1. PROTAC Protein Tyrosine Kinase/RTK
  2. Ligands for Target Protein for PROTAC Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase
  3. Crizotinib

クリゾチニブ  (Synonyms: Crizotinib; PF-02341066)

製品番号: HY-50878 純度: 99.74%
COA 取扱説明書 Technical Support

Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.

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CAS 番号 : 877399-52-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 38 在庫あり
Solution
10 mM * 1 mL in DMSO USD 38 在庫あり
Solid
5 mg $35 在庫あり
10 mg $55 在庫あり
50 mg $77 在庫あり
100 mg $110 在庫あり
200 mg $132 在庫あり
500 mg $209 在庫あり
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カスタマーレビュー

Based on 86 publication(s) in Google Scholar

Other Forms of Crizotinib:

Top Publications Citing Use of Products

顧客検証

WB

    Crizotinib purchased from MedChemExpress. Usage Cited in: Evid Based Complement Alternat Med. 2019 Nov 7;2019:4253846.  [Abstract]

    Western blot analysis of cleaved caspase 3, Bax, and Bcl-2 expression after serum-free culture for 72 h with or without Crizotinib.

    Crizotinib purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.  [Abstract]

    Resistant cells are treated with 200 nM Afatinib alone or in combination with 1 μM Crizotinib for 48 h.

    Crizotinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369.  [Abstract]

    At 50mg/kg, Crizotinib inhibits MET phosphorylation and downstream signaling pathway activation.

    Crizotinib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 May 28:422:19-28.  [Abstract]

    CD74-ROS1 or CD74-ROS1 G2032R mutation cells are treated with Crizotinib for 24 h, the expression of ROS1 or p-ROS1 is determined by western blot.

    Crizotinib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):996-1006.  [Abstract]

    Dose-response and time course comparison of ALK inhibition by Crizotinib or Ceritinib.

    Crizotinib purchased from MedChemExpress. Usage Cited in: Dis Model Mech. 2016 Sep 1;9(9):941-52.  [Abstract]

    CLB-BAR, CLB-GE neuroblastoma cells are treated for 6 h with either Crizotinib or PF-04643922. Cells are harvested and pre-cleared cell lysates are analyzed on SDS PAGE followed by western blotting for ALK, phospho-ALK-Y1278, phospho-ERK5, pan-ERK5 phospho-ERK1/2 and pan-ERK. Actin is employed as a loading control. Protein band intensities are quantified by Image Studio Lite 3.1 and normalized to untreated samples.

    Crizotinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 17;7(20):29011-22.  [Abstract]

    A, B. CLB-BAR (ALK-Δ4-11) and CLB-GE (ALK-F1174V), both ALK addicted cell lines, are treated with increasing doses of Brigatinib for 6 hours. Crizotinib (250 nM) is employed as a positive control. Cells lysates are resolved on SDS/PAGE followed by immunoblotting for pALK (Y1604) and additional downstream targets as indicated.

    Crizotinib purchased from MedChemExpress. Usage Cited in: Sci Signal. 2014 Oct 28;7(349):ra102.  [Abstract]

    Activation of ERK5 in neuroblastoma cell lines expressing activated ALK. (A to C) Immunoblotting for the indicated proteins in neuroblastoma cells CLB-BAR (A), CLB-GE (B), and IMR32 (C) cultured on six-well plates in complete growth medium and treated with inhibitors as indicated for 6 hours alone (A and B) or before (C) stimulation with mAb46 for 30 min.

    Crizotinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2014 May 15;5(9):2688-702.  [Abstract]

    The Ret expression level is investigated by Western blot in MYCN/KI AlkR1279Q and MYCN/KI AlkF1178L treated tumors and controls using the anti-Ret antibody EPR2871. Actin is used as a standard for quantification.
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    製品説明

    Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition[1][2][3].

    IC50 & Target

    IC50: 20 nM (ALK), 8 nM (c-Met)[3]

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    0.008 3
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of human recombinant c-MET kinase expressed in A549 cells assessed as inhibition of HGF-induced autophosphorylation by ELISA method
    Inhibition of human recombinant c-MET kinase expressed in A549 cells assessed as inhibition of HGF-induced autophosphorylation by ELISA method
    [PMID: 21812414]
    A549 IC50
    0.1343 3
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells after 72 hrs by Alamarblue assay relative to control
    Antiproliferative activity against human A549 cells after 72 hrs by Alamarblue assay relative to control
    [PMID: 29202410]
    A549 IC50
    0.1343 3
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells after 72 hrs by Alamarblue assay relative to control
    Antiproliferative activity against human A549 cells after 72 hrs by Alamarblue assay relative to control
    [PMID: 29202410]
    A549 IC50
    >1 3
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 30223120]
    A549 IC50
    0.41 3
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34237620]
    A549 IC50
    0.41 3
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34237620]
    A549 IC50
    1.06 3
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31260890]
    A549 IC50
    1.06 3
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31260890]
    A549 IC50
    1.17 3
    Compound: Crizotinib
    Cytotoxicity against human A549 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay
    Cytotoxicity against human A549 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    A549 IC50
    >1 3
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells harboring EGFR after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells harboring EGFR after 72 hrs by MTT assay
    [PMID: 29174809]
    A549 IC50
    2.31 3
    Compound: Crizotinib
    Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    A549 IC50
    5.7 3
    Compound: PF-02341066
    Cytotoxicity against EGFR-positive human A549 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against EGFR-positive human A549 cells incubated for 72 hrs by MTT assay
    [PMID: 33069075]
    A549 IC50
    4.084 3
    Compound: Crizotinib
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    [PMID: 24900830]
    A549 IC50
    4.084 3
    Compound: Crizotinib
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    [PMID: 24900830]
    A549 IC50
    >10 3
    Compound: Crizotinib
    Cytotoxicity against human A549 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    [PMID: 27474925]
    A549 IC50
    5.7 3
    Compound: PF-02341066
    Cytotoxicity against EGFR-positive human A549 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against EGFR-positive human A549 cells incubated for 72 hrs by MTT assay
    [PMID: 33069075]
    A549 IC50
    > 1 1
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 24785465]
    A549 IC50
    1.17 3
    Compound: Crizotinib
    Cytotoxicity against human A549 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay
    Cytotoxicity against human A549 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    A549 IC50
    2.31 3
    Compound: Crizotinib
    Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    A549 IC50
    > 1 3
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells harboring EGFR after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells harboring EGFR after 72 hrs by MTT assay
    [PMID: 29174809]
    A549 IC50
    > 1 3
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 30223120]
    A549 IC50
    0.008 3
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of human recombinant c-MET kinase expressed in A549 cells assessed as inhibition of HGF-induced autophosphorylation by ELISA method
    Inhibition of human recombinant c-MET kinase expressed in A549 cells assessed as inhibition of HGF-induced autophosphorylation by ELISA method
    [PMID: 21812414]
    A549 IC50
    > 10 3
    Compound: Crizotinib
    Cytotoxicity against human A549 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    [PMID: 27474925]
    ASPC1 GI50
    2.38 3
    Compound: 2
    Antiproliferative activity against human ASPC1 cells harbouring KRAS G12D mutant and RON delta 165 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human ASPC1 cells harbouring KRAS G12D mutant and RON delta 165 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    ASPC1 GI50
    2.38 3
    Compound: 2
    Antiproliferative activity against human ASPC1 cells harbouring KRAS G12D mutant and RON delta 165 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human ASPC1 cells harbouring KRAS G12D mutant and RON delta 165 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    BaF3 GI50
    1.1 3
    Compound: 9
    Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
    [PMID: 28850922]
    BaF3 IC50
    >1 3
    Compound: Crizotinib
    Antiproliferative activity against mouse BAF3 cells harboring G1202R mutation after 72 hrs by MTT assay
    Antiproliferative activity against mouse BAF3 cells harboring G1202R mutation after 72 hrs by MTT assay
    [PMID: 30223120]
    BaF3 IC50
    >5 3
    Compound: Crizotinib
    Cytotoxicity against mouse BA/F3 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay
    Cytotoxicity against mouse BA/F3 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    BaF3 IC50
    0.98 3
    Compound: Crizotinib
    Cytotoxicity against mouse BAF3 cells assessed as growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    Cytotoxicity against mouse BAF3 cells assessed as growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    [PMID: 24468632]
    BaF3 GI50
    1.1 3
    Compound: 9
    Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
    [PMID: 28850922]
    BaF3 IC50
    0.62 3
    Compound: 2, PF-2341066
    Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 after 48 hrs by MTS assay
    Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 after 48 hrs by MTS assay
    [PMID: 21572589]
    BaF3 IC50
    2.2 3
    Compound: 2, PF-2341066
    Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 after 48 hrs by MTS assay
    Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 after 48 hrs by MTS assay
    [PMID: 21572589]
    BaF3 IC50
    0.051 3
    Compound: Crizotinib
    Inhibition of NPM/ALK (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    Inhibition of NPM/ALK (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    [PMID: 24468632]
    BaF3 IC50
    0.28 3
    Compound: 2, PF-2341066
    Cytotoxicity against mouse BAF3 cells expressing EML4-ALK after 48 hrs by MTS assay
    Cytotoxicity against mouse BAF3 cells expressing EML4-ALK after 48 hrs by MTS assay
    [PMID: 21572589]
    BaF3 IC50
    0.19 3
    Compound: 2, PF-2341066
    Cytotoxicity against mouse BAF3 cells expressing Tel-ALK after 48 hrs by CellTiter-Glo assay
    Cytotoxicity against mouse BAF3 cells expressing Tel-ALK after 48 hrs by CellTiter-Glo assay
    [PMID: 21572589]
    BaF3 IC50
    0.19 3
    Compound: 2, PF-2341066
    Cytotoxicity against mouse BAF3 cells expressing Tel-ALK after 48 hrs by CellTiter-Glo assay
    Cytotoxicity against mouse BAF3 cells expressing Tel-ALK after 48 hrs by CellTiter-Glo assay
    [PMID: 21572589]
    BaF3 IC50
    0.26 3
    Compound: Crizotinib
    Inhibition of NPM/ALK L1196M mutant (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    Inhibition of NPM/ALK L1196M mutant (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    [PMID: 24468632]
    BaF3 IC50
    0.051 3
    Compound: Crizotinib
    Inhibition of NPM/ALK (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    Inhibition of NPM/ALK (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    [PMID: 24468632]
    BaF3 IC50
    0.28 3
    Compound: 2, PF-2341066
    Cytotoxicity against mouse BAF3 cells expressing EML4-ALK after 48 hrs by MTS assay
    Cytotoxicity against mouse BAF3 cells expressing EML4-ALK after 48 hrs by MTS assay
    [PMID: 21572589]
    BaF3 IC50
    0.26 3
    Compound: Crizotinib
    Inhibition of NPM/ALK L1196M mutant (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    Inhibition of NPM/ALK L1196M mutant (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    [PMID: 24468632]
    BaF3 IC50
    0.62 3
    Compound: 2, PF-2341066
    Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 after 48 hrs by MTS assay
    Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 after 48 hrs by MTS assay
    [PMID: 21572589]
    CAPAN-1 GI50
    5.12 3
    Compound: 2
    Antiproliferative activity against human CAPAN-1 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human CAPAN-1 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    BaF3 IC50
    0.98 3
    Compound: Crizotinib
    Cytotoxicity against mouse BAF3 cells assessed as growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    Cytotoxicity against mouse BAF3 cells assessed as growth inhibition after 72 hrs by [3H]-thymidine incorporation assay
    [PMID: 24468632]
    CHO GI50
    3.2 3
    Compound: 9
    Antiproliferative activity against CHO cells after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against CHO cells after 72 hrs by CellTiter-Glo assay
    [PMID: 28850922]
    COLO 205 IC50
    2.449 3
    Compound: Crizotinib
    Antiproliferative activity against human COLO205 cells after 72 hrs by Alamarblue assay
    Antiproliferative activity against human COLO205 cells after 72 hrs by Alamarblue assay
    [PMID: 29202410]
    BaF3 IC50
    111 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BaF3 cells harbouring ALK wild type assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    Antiproliferative activity against mouse BaF3 cells harbouring ALK wild type assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    [PMID: 35421578]
    BaF3 IC50
    4.336 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BAF3 cells expressing wild type CD74/ROS1 assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BAF3 cells expressing wild type CD74/ROS1 assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 31260890]
    BaF3 IC50
    1237 1
    Compound: Crizotinib
    Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth in presence of IL-3
    Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth in presence of IL-3
    [PMID: 27780853]
    BaF3 IC50
    127.4 1
    Compound: 1
    Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs
    Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs
    [PMID: 26005523]
    EBC-1 IC50
    0.021 3
    Compound: Crizotinib
    Antiproliferative activity against human EBC1 cells after 72 hrs
    Antiproliferative activity against human EBC1 cells after 72 hrs
    [PMID: 25537530]
    BaF3 IC50
    144 1
    Compound: 4
    Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    EBC-1 IC50
    0.023 3
    Compound: Crizotinib
    Antiproliferative activity against human EBC1 cells after 72 hrs
    Antiproliferative activity against human EBC1 cells after 72 hrs
    [PMID: 23993328]
    BaF3 IC50
    150.8 1
    Compound: 1, PF-02341066
    Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    [PMID: 23742252]
    EBC-1 IC50
    0.013 3
    Compound: Crizotinib
    Antiproliferative activity against human EBC1 cells after 72 hrs by Alamarblue assay
    Antiproliferative activity against human EBC1 cells after 72 hrs by Alamarblue assay
    [PMID: 29202410]
    EBC-1 IC50
    0.053 3
    Compound: 1
    Antiproliferative activity against human EBC1 cells expressing elevated levels of constitutively active c-Met after 72 hrs by SRB assay
    Antiproliferative activity against human EBC1 cells expressing elevated levels of constitutively active c-Met after 72 hrs by SRB assay
    [PMID: 22863529]
    BaF3 IC50
    1643 1
    Compound: 1, PF-02341066
    Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    [PMID: 23742252]
    EBC-1 IC50
    0.044 3
    Compound: Crizotinib
    Cytotoxicity against human EBC1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human EBC1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    [PMID: 27017548]
    BaF3 IC50
    18 1
    Compound: PF-02341066
    Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
    [PMID: 25733882]
    BaF3 IC50
    2.2 3
    Compound: 2, PF-2341066
    Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 after 48 hrs by MTS assay
    Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 after 48 hrs by MTS assay
    [PMID: 21572589]
    GBM EC50
    4.3 3
    Compound: 5
    Cytotoxicity against patient-derived GBM cells assessed as LDH release after 96 hrs by spectrophotometric method
    Cytotoxicity against patient-derived GBM cells assessed as LDH release after 96 hrs by spectrophotometric method
    [PMID: 31378572]
    GL261 IC50
    3.43 3
    Compound: Cri
    Anti-proliferative activity against mouse GL261 cells assessed as cell viability incubated for 2 hrs by CCK8 assay
    Anti-proliferative activity against mouse GL261 cells assessed as cell viability incubated for 2 hrs by CCK8 assay
    [PMID: 37861443]
    BaF3 IC50
    259 1
    Compound: PF-02341066
    Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
    [PMID: 25733882]
    HCC78 IC50
    2 3
    Compound: Crizotinib
    Antiproliferative activity against human HCC78 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HCC78 cells after 48 hrs by MTT assay
    [PMID: 29174814]
    BaF3 IC50
    284 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BaF3 cells harbouring ALK C1156Y mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    Antiproliferative activity against mouse BaF3 cells harbouring ALK C1156Y mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    [PMID: 35421578]
    HCC78 IC50
    0.17 3
    Compound: Crizotinib
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
    [PMID: 29174809]
    BaF3 IC50
    328 1
    Compound: 4
    Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    340 1
    Compound: 1
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    HCC78 IC50
    0.17 3
    Compound: Crizotinib
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
    [PMID: 30223120]
    BaF3 IC50
    3479 1
    Compound: 1, PF-02341066
    Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    [PMID: 23742252]
    HCC78 IC50
    19.19 3
    Compound: Crizotinib
    Antiproliferative activity against ROS1-addicted human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against ROS1-addicted human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31260890]
    HCC78 IC50
    0.34 3
    Compound: Crizotinib
    Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay
    [PMID: 27474925]
    BaF3 IC50
    4.336 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BAF3 cells expressing wild type CD74/ROS1 assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BAF3 cells expressing wild type CD74/ROS1 assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 31260890]
    HCC78 IC50
    0.17 3
    Compound: PF-02341066
    Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 incubated for 72 hrs by MTT assay
    Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 incubated for 72 hrs by MTT assay
    [PMID: 33069075]
    BaF3 IC50
    48.6 1
    Compound: 1
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    HCC78 IC50
    0.23 3
    Compound: Crizotinib
    Cytotoxicity against human HCC78 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human HCC78 cells incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    BaF3 IC50
    512 1
    Compound: 4
    Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    HCC827 IC50
    >10 3
    Compound: Crizotinib
    Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay
    Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay
    [PMID: 24900830]
    BaF3 IC50
    549 1
    Compound: 4
    Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    56 1
    Compound: 4
    Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    HCC827 IC50
    7.25 3
    Compound: Crizotinib
    Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27396929]
    BaF3 IC50
    564 1
    Compound: 1
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    HCT-116 IC50
    14.82 3
    Compound: Crizotinib
    Antiproliferative activity against human HCT116 cells after 72 hrs
    Antiproliferative activity against human HCT116 cells after 72 hrs
    [PMID: 23993328]
    BaF3 IC50
    57.5 1
    Compound: 1
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    HCT-116 IC50
    0.2536 3
    Compound: Crizotinib
    Antiproliferative activity against human HCT116 cells after 72 hrs by Alamarblue assay relative to control
    Antiproliferative activity against human HCT116 cells after 72 hrs by Alamarblue assay relative to control
    [PMID: 29202410]
    EBC-1 IC50
    6.9 1
    Compound: Crizotinib, PF2341066
    Antiproliferative activity against cMET-amplified human EBC1 cells after 72 hrs
    Antiproliferative activity against cMET-amplified human EBC1 cells after 72 hrs
    [PMID: 24900831]
    BaF3 IC50
    58.5 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 31260890]
    MKN-45 IC50
    9.1 1
    Compound: 1; PF-0234106
    Antiproliferative activity against human MKN45 cells overexpressing c-MET assessed as reduction in cell proliferation
    Antiproliferative activity against human MKN45 cells overexpressing c-MET assessed as reduction in cell proliferation
    [PMID: 32371098]
    BaF3 IC50
    594 1
    Compound: 1
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    HEL IC50
    4.725 3
    Compound: 4
    Antiproliferative activity against HEL cells harboring JAK2 V617F mutant measured after 3 days by CCK8 assay
    Antiproliferative activity against HEL cells harboring JAK2 V617F mutant measured after 3 days by CCK8 assay
    [PMID: 30981578]
    BaF3 IC50
    643.5 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 31260890]
    BaF3 IC50
    644 1
    Compound: 1
    Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    MKN-45 IC50
    15 1
    Compound: 2
    Antiproliferative activity against human MKN-45 cells incubated for 72 hrs
    Antiproliferative activity against human MKN-45 cells incubated for 72 hrs
    [PMID: 33957388]
    BaF3 IC50
    645 1
    Compound: 4
    Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    EBC-1 IC50
    19 1
    Compound: Crizotinib
    Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
    Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
    [PMID: 26698536]
    BaF3 IC50
    65 1
    Compound: 4
    Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    HepG2 IC50
    0.32 3
    Compound: Crizotinib
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34237620]
    BaF3 IC50
    704 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BaF3 cells harbouring ALK L1196M mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    Antiproliferative activity against mouse BaF3 cells harbouring ALK L1196M mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    [PMID: 35421578]
    HepG2 IC50
    3.7 3
    Compound: Crizotinib
    Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27396929]
    BaF3 IC50
    81 1
    Compound: 4
    Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    KARPAS-299 IC50
    20 1
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of ALK in human KARPAS299 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    Inhibition of ALK in human KARPAS299 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    [PMID: 21812414]
    SNU-5 IC50
    20.4 1
    Compound: 1
    Antiproliferative activity against human SNU5 cells after 72 hrs
    Antiproliferative activity against human SNU5 cells after 72 hrs
    [PMID: 26005523]
    BaF3 IC50
    857 1
    Compound: 4
    Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    927 1
    Compound: 4
    Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    EBC-1 IC50
    21.8 1
    Compound: 1
    Antiproliferative activity against human EBC1 cells after 72 hrs
    Antiproliferative activity against human EBC1 cells after 72 hrs
    [PMID: 26005523]
    HT-29 GI50
    4 3
    Compound: 2
    Antiproliferative activity against human HT-29 cells harbouring wild-type KRAS and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human HT-29 cells harbouring wild-type KRAS and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    BaF3 IC50
    > 1 3
    Compound: Crizotinib
    Antiproliferative activity against mouse BAF3 cells harboring G1202R mutation after 72 hrs by MTT assay
    Antiproliferative activity against mouse BAF3 cells harboring G1202R mutation after 72 hrs by MTT assay
    [PMID: 30223120]
    BaF3 IC50
    > 2000 1
    Compound: PF-02341066
    Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
    [PMID: 25733882]
    HT-29 IC50
    >10 3
    Compound: Crizotinib
    Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    [PMID: 27474925]
    BaF3 IC50
    > 5 3
    Compound: Crizotinib
    Cytotoxicity against mouse BA/F3 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay
    Cytotoxicity against mouse BA/F3 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    Jurkat IC50
    >40 3
    Compound: 70
    Anti-neprotic activity in human Jurkat cells FADD defient assessed as reduction in TNFalpha-induced necroptosis preincubated for 30 mins followed by addition of TNFalpha-stimulation and further incubated for over night by Cell Titer Glo assay
    Anti-neprotic activity in human Jurkat cells FADD defient assessed as reduction in TNFalpha-induced necroptosis preincubated for 30 mins followed by addition of TNFalpha-stimulation and further incubated for over night by Cell Titer Glo assay
    [PMID: 31622096]
    BaF3 IC50
    > 5 3
    Compound: Crizotinib
    Cytotoxicity against mouse BA/F3 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against mouse BA/F3 cells incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    NCI-H3122 EC50
    32 1
    Compound: 4
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    KARPAS-299 IC50
    0.03 3
    Compound: 1; PF-02341066
    Antiproliferative activity against human KARPAS299 cells expressing NMP-ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human KARPAS299 cells expressing NMP-ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31569004]
    KARPAS-299 IC50
    0.087 3
    Compound: Crizotinib
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay
    [PMID: 29174809]
    KARPAS-299 IC50
    0.24 3
    Compound: Crizotinib
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay
    [PMID: 30223120]
    KARPAS-299 IC50
    0.087 3
    Compound: PF-02341066
    Cytotoxicity against human KARPAS299 cells harboring NMP-ALK incubated for 72 hrs by MTT assay
    Cytotoxicity against human KARPAS299 cells harboring NMP-ALK incubated for 72 hrs by MTT assay
    [PMID: 33069075]
    KARPAS-299 IC50
    0.068 3
    Compound: Crizotinib
    Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay
    [PMID: 27474925]
    CAPAN-1 GI50
    5.12 3
    Compound: 2
    Antiproliferative activity against human CAPAN-1 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human CAPAN-1 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    KARPAS-299 IC50
    0.097 3
    Compound: Crizotinib
    Cytotoxicity against human KARPAS299 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human KARPAS299 cells incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    CHO GI50
    3.2 3
    Compound: 9
    Antiproliferative activity against CHO cells after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against CHO cells after 72 hrs by CellTiter-Glo assay
    [PMID: 28850922]
    HEK293 IC50
    37 1
    Compound: Crizotinib
    Inhibition of recombinant human ALK expressed in HEK293 cells assessed as reduction in ALK autophosphorylation at Tyr1604 residue incubated for 60 mins by sandwich ELISA
    Inhibition of recombinant human ALK expressed in HEK293 cells assessed as reduction in ALK autophosphorylation at Tyr1604 residue incubated for 60 mins by sandwich ELISA
    [PMID: 31009559]
    MKN-45 IC50
    38.1 1
    Compound: 1
    Antiproliferative activity against human MKN45 cells after 72 hrs
    Antiproliferative activity against human MKN45 cells after 72 hrs
    [PMID: 26005523]
    COLO 205 IC50
    2.449 3
    Compound: Crizotinib
    Antiproliferative activity against human COLO205 cells after 72 hrs by Alamarblue assay
    Antiproliferative activity against human COLO205 cells after 72 hrs by Alamarblue assay
    [PMID: 29202410]
    EBC-1 IC50
    39 1
    Compound: Crizotinib
    Antiproliferative activity against human EBC1 cells after 72 hrs by Cell Titer-Glo assay
    Antiproliferative activity against human EBC1 cells after 72 hrs by Cell Titer-Glo assay
    [PMID: 29602036]
    Kelly IC50
    >1 3
    Compound: Crizotinib
    Antiproliferative activity against crizotinib-resistant human Kelly cells harboring ALK F1174L mutant after 72 hrs by MTT assay
    Antiproliferative activity against crizotinib-resistant human Kelly cells harboring ALK F1174L mutant after 72 hrs by MTT assay
    [PMID: 24785465]
    Kelly IC50
    0.42 3
    Compound: 2, PF-2341066
    Cytotoxicity against human Kelly cells expressing ALK F1174L mutant
    Cytotoxicity against human Kelly cells expressing ALK F1174L mutant
    [PMID: 21572589]
    BaF3 IC50
    48.6 1
    Compound: 1
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    BaF3 IC50
    56 1
    Compound: 4
    Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    57.5 1
    Compound: 1
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    DEL GI50
    309 1
    Compound: Crizotinib
    Growth inhibition of human DEL cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay
    Growth inhibition of human DEL cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay
    [PMID: 27780853]
    BaF3 IC50
    58.5 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 31260890]
    MCF7 IC50
    9.58 3
    Compound: Crizotinib
    Antiproliferative activity against human MCF7 cells after 72 hrs
    Antiproliferative activity against human MCF7 cells after 72 hrs
    [PMID: 23993328]
    MCF7 IC50
    0.045 3
    Compound: Crizotinib
    Antiproliferative activity against human MCF7 cells after 72 hrs by Alamarblue assay relative to control
    Antiproliferative activity against human MCF7 cells after 72 hrs by Alamarblue assay relative to control
    [PMID: 29202410]
    EBC-1 IC50
    0.013 3
    Compound: Crizotinib
    Antiproliferative activity against human EBC1 cells after 72 hrs by Alamarblue assay
    Antiproliferative activity against human EBC1 cells after 72 hrs by Alamarblue assay
    [PMID: 29202410]
    KARPAS-299 IC50
    62 1
    Compound: 1, Xalkori
    Inhibition of ALK-fusion driven cell proliferation in human KARPAS299 cells after 72 hrs by CellTiter Glo assay
    Inhibition of ALK-fusion driven cell proliferation in human KARPAS299 cells after 72 hrs by CellTiter Glo assay
    [PMID: 24432909]
    KARPAS-299 IC50
    64.2 1
    Compound: 1, PF-02341066
    Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay
    Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay
    [PMID: 23742252]
    EBC-1 IC50
    0.021 3
    Compound: Crizotinib
    Antiproliferative activity against human EBC1 cells after 72 hrs
    Antiproliferative activity against human EBC1 cells after 72 hrs
    [PMID: 25537530]
    BaF3 IC50
    65 1
    Compound: 4
    Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    EBC-1 IC50
    0.023 3
    Compound: Crizotinib
    Antiproliferative activity against human EBC1 cells after 72 hrs
    Antiproliferative activity against human EBC1 cells after 72 hrs
    [PMID: 23993328]
    MDA-MB-231 IC50
    10.8 3
    Compound: Crizotinib
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs
    [PMID: 23993328]
    EBC-1 IC50
    0.044 3
    Compound: Crizotinib
    Cytotoxicity against human EBC1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human EBC1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    [PMID: 27017548]
    EBC-1 IC50
    0.053 3
    Compound: 1
    Antiproliferative activity against human EBC1 cells expressing elevated levels of constitutively active c-Met after 72 hrs by SRB assay
    Antiproliferative activity against human EBC1 cells expressing elevated levels of constitutively active c-Met after 72 hrs by SRB assay
    [PMID: 22863529]
    MDA-MB-231 IC50
    0.79 3
    Compound: Crizotinib
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34237620]
    EBC-1 IC50
    19 1
    Compound: Crizotinib
    Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
    Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
    [PMID: 26698536]
    NIH3T3 IC50
    80 1
    Compound: 1, Xalkori
    Inhibition of human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
    Inhibition of human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NIH3T3 IC50
    80 1
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of RON in mouse 3T3 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    Inhibition of RON in mouse 3T3 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    [PMID: 21812414]
    EBC-1 IC50
    21.8 1
    Compound: 1
    Antiproliferative activity against human EBC1 cells after 72 hrs
    Antiproliferative activity against human EBC1 cells after 72 hrs
    [PMID: 26005523]
    EBC-1 IC50
    39 1
    Compound: Crizotinib
    Antiproliferative activity against human EBC1 cells after 72 hrs by Cell Titer-Glo assay
    Antiproliferative activity against human EBC1 cells after 72 hrs by Cell Titer-Glo assay
    [PMID: 29602036]
    NIH3T3 IC50
    80 1
    Compound: 1, PF-02341066
    Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
    Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    BaF3 IC50
    81 1
    Compound: 4
    Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    EBC-1 IC50
    6.9 1
    Compound: Crizotinib
    Antiproliferative activity against human EBC-1 cells
    Antiproliferative activity against human EBC-1 cells
    [PMID: 38733884]
    SU-DHL-1 IC50
    92.3 1
    Compound: Crizotinib
    Antiproliferative activity against ALK constitutively activated human SU-DHL1 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against ALK constitutively activated human SU-DHL1 cells after 72 hrs by SRB or CCK8 assay
    [PMID: 27769623]
    EBC-1 IC50
    6.9 1
    Compound: Crizotinib, PF2341066
    Antiproliferative activity against cMET-amplified human EBC1 cells after 72 hrs
    Antiproliferative activity against cMET-amplified human EBC1 cells after 72 hrs
    [PMID: 24900831]
    NIH3T3 IC50
    95.4 1
    Compound: Crizotinib
    Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1 after 72 hrs by MTT assay
    Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1 after 72 hrs by MTT assay
    [PMID: 24785465]
    MIA PaCa-2 GI50
    1.457 3
    Compound: 2
    Antiproliferative activity against human MIA PaCa-2 cells harbouring KRAS G12C mutant and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human MIA PaCa-2 cells harbouring KRAS G12C mutant and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    GBM EC50
    3200 1
    Compound: 5
    Synergistic antiproliferative activity against patient-derived GBM cells assessed as cell viability after 48 hrs in presence of temozolomide by 5-Ethynyl-2'-deoxyuridine incorporation assay
    Synergistic antiproliferative activity against patient-derived GBM cells assessed as cell viability after 48 hrs in presence of temozolomide by 5-Ethynyl-2'-deoxyuridine incorporation assay
    [PMID: 31378572]
    GBM EC50
    4.3 3
    Compound: 5
    Cytotoxicity against patient-derived GBM cells assessed as LDH release after 96 hrs by spectrophotometric method
    Cytotoxicity against patient-derived GBM cells assessed as LDH release after 96 hrs by spectrophotometric method
    [PMID: 31378572]
    MIA PaCa-2 IC50
    7.16 3
    Compound: Crizotinib
    Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27396929]
    GBM EC50
    5600 1
    Compound: 5
    Antiproliferative activity against patient-derived GBM cells assessed as cell viability after 48 hrs by 5-Ethynyl-2'-deoxyuridine incorporation assay
    Antiproliferative activity against patient-derived GBM cells assessed as cell viability after 48 hrs by 5-Ethynyl-2'-deoxyuridine incorporation assay
    [PMID: 31378572]
    MKN-45 IC50
    0.013 3
    Compound: Crizotinib
    Antiproliferative activity against human MKN45 cells after 72 hrs
    Antiproliferative activity against human MKN45 cells after 72 hrs
    [PMID: 23993328]
    MKN-45 IC50
    0.022 3
    Compound: Crizotinib
    Antiproliferative activity against human MKN45 cells after 72 hrs by Alamarblue assay
    Antiproliferative activity against human MKN45 cells after 72 hrs by Alamarblue assay
    [PMID: 29202410]
    GBM IC50
    480 1
    Compound: 5
    Synergistic antiproliferative activity against patient-derived GBM cells assessed as reduction in cell viability after 48 hrs in presence of temozolomide by 5-Ethynyl-2'-deoxyuridine incorporation assay
    Synergistic antiproliferative activity against patient-derived GBM cells assessed as reduction in cell viability after 48 hrs in presence of temozolomide by 5-Ethynyl-2'-deoxyuridine incorporation assay
    [PMID: 31378572]
    GBM IC50
    540 1
    Compound: 5
    Antiproliferative activity against patient-derived GBM cells assessed as reduction in cell viability after 48 hrs by 5-Ethynyl-2'-deoxyuridine incorporation assay
    Antiproliferative activity against patient-derived GBM cells assessed as reduction in cell viability after 48 hrs by 5-Ethynyl-2'-deoxyuridine incorporation assay
    [PMID: 31378572]
    NCI-H3122 IC50
    100.9 1
    Compound: Crizotinib
    Antiproliferative activity against ALK constitutively activated human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against ALK constitutively activated human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
    [PMID: 27769623]
    KARPAS-299 IC50
    103 1
    Compound: 1; PF-2341066
    Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    GL261 IC50
    3.43 3
    Compound: Cri
    Anti-proliferative activity against mouse GL261 cells assessed as cell viability incubated for 2 hrs by CCK8 assay
    Anti-proliferative activity against mouse GL261 cells assessed as cell viability incubated for 2 hrs by CCK8 assay
    [PMID: 37861443]
    KARPAS-299 IC50
    104.9 1
    Compound: Crizotinib
    Antiproliferative activity against ALK constitutively activated human KARPAS299 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against ALK constitutively activated human KARPAS299 cells after 72 hrs by SRB or CCK8 assay
    [PMID: 27769623]
    NCI-H3122 IC50
    108 1
    Compound: 1, Xalkori
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells after 72 hrs by CellTiter Glo assay
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells after 72 hrs by CellTiter Glo assay
    [PMID: 24432909]
    BaF3 IC50
    111 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BaF3 cells harbouring ALK wild type assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    Antiproliferative activity against mouse BaF3 cells harbouring ALK wild type assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    [PMID: 35421578]
    NCI-H2228 IC50
    118 1
    Compound: 1, Xalkori
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H2228 cells after 72 hrs by CellTiter Glo assay
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H2228 cells after 72 hrs by CellTiter Glo assay
    [PMID: 24432909]
    BaF3 IC50
    127.4 1
    Compound: 1
    Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs
    Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs
    [PMID: 26005523]
    SU-DHL-1 IC50
    136 1
    Compound: 1; PF-2341066
    Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    KARPAS-299 IC50
    138 1
    Compound: Crizotinib
    Antiproliferative activity against human KARPAS-299 cells harbouring wild type ALK assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    Antiproliferative activity against human KARPAS-299 cells harbouring wild type ALK assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    [PMID: 35421578]
    BaF3 IC50
    144 1
    Compound: 4
    Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    HCC78 IC50
    0.17 3
    Compound: Crizotinib
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
    [PMID: 29174809]
    HCC78 IC50
    0.17 3
    Compound: Crizotinib
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
    [PMID: 30223120]
    BaF3 IC50
    150.8 1
    Compound: 1, PF-02341066
    Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    [PMID: 23742252]
    HCC78 IC50
    0.17 3
    Compound: PF-02341066
    Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 incubated for 72 hrs by MTT assay
    Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 incubated for 72 hrs by MTT assay
    [PMID: 33069075]
    SU-DHL-1 IC50
    155 1
    Compound: 1
    Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    NIH3T3 IC50
    165 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    HCC78 IC50
    0.23 3
    Compound: Crizotinib
    Cytotoxicity against human HCC78 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human HCC78 cells incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    HCC78 IC50
    0.34 3
    Compound: Crizotinib
    Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay
    [PMID: 27474925]
    NIH3T3 IC50
    165 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    HCC78 IC50
    19.19 3
    Compound: Crizotinib
    Antiproliferative activity against ROS1-addicted human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against ROS1-addicted human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31260890]
    KARPAS-299 IC50
    176 1
    Compound: 1
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    NCI-H3122 IC50
    180 1
    Compound: 1; PF2341066
    Cytotoxicity against human NCI-H3122 cells harboring EML4-ALK E13;A20 mutant incubated for 72 hrs by Cell titer blue assay
    Cytotoxicity against human NCI-H3122 cells harboring EML4-ALK E13;A20 mutant incubated for 72 hrs by Cell titer blue assay
    [PMID: 31419130]
    HCC78 IC50
    2 3
    Compound: Crizotinib
    Antiproliferative activity against human HCC78 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HCC78 cells after 48 hrs by MTT assay
    [PMID: 29174814]
    KARPAS-299 IC50
    200 1
    Compound: Crizotinib, PF2341066
    Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs
    Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs
    [PMID: 24900831]
    HCC78 IC50
    21 1
    Compound: PF-02341066
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
    [PMID: 25733882]
    HCC78 IC50
    47 1
    Compound: PF-02341066
    Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
    [PMID: 25733882]
    NCI-H2228 IC50
    202 1
    Compound: Crizotinib
    Inhibition of E6a/b;A20 EML4-ALK (unknown origin) expressed in human NCI-H2228 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    Inhibition of E6a/b;A20 EML4-ALK (unknown origin) expressed in human NCI-H2228 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    [PMID: 26844689]
    NCI-H3122 IC50
    210 1
    Compound: 1; PF-2341066
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    HCC78 IC50
    889 1
    Compound: 1
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    Kelly EC50
    211 1
    Compound: 4
    Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    HCC827 IC50
    7.25 3
    Compound: Crizotinib
    Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27396929]
    HCC827 IC50
    > 10 3
    Compound: Crizotinib
    Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay
    Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay
    [PMID: 24900830]
    NCI-H1975 IC50
    >10 3
    Compound: PF-02341066
    Cytotoxicity against EGFR-positive human H1975 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against EGFR-positive human H1975 cells incubated for 72 hrs by MTT assay
    [PMID: 33069075]
    HCT-116 IC50
    0.2536 3
    Compound: Crizotinib
    Antiproliferative activity against human HCT116 cells after 72 hrs by Alamarblue assay relative to control
    Antiproliferative activity against human HCT116 cells after 72 hrs by Alamarblue assay relative to control
    [PMID: 29202410]
    NCI-H1975 IC50
    7.551 3
    Compound: Crizotinib
    Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay
    Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay
    [PMID: 24900830]
    HCT-116 IC50
    14.82 3
    Compound: Crizotinib
    Antiproliferative activity against human HCT116 cells after 72 hrs
    Antiproliferative activity against human HCT116 cells after 72 hrs
    [PMID: 23993328]
    NCI-H1993 IC50
    0.061 3
    Compound: Crizotinib
    Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay
    Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay
    [PMID: 24900830]
    NCI-H1993 IC50
    3 3
    Compound: 12
    Cytotoxicity against human NCI-H1993 cells assessed as inhibition of cell growth
    Cytotoxicity against human NCI-H1993 cells assessed as inhibition of cell growth
    [PMID: 32858470]
    HEK293 IC50
    2887 1
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of IR in human HEK293 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    Inhibition of IR in human HEK293 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    [PMID: 21812414]
    NCI-H2228 GI50
    0.073 3
    Compound: 9
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-fused ALK varian3 after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-fused ALK varian3 after 72 hrs by CellTiter-Glo assay
    [PMID: 28850922]
    HEK293 IC50
    294 1
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of AXL in human HEK293 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    Inhibition of AXL in human HEK293 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    [PMID: 21812414]
    HEK293 IC50
    37 1
    Compound: Crizotinib
    Inhibition of recombinant human ALK expressed in HEK293 cells assessed as reduction in ALK autophosphorylation at Tyr1604 residue incubated for 60 mins by sandwich ELISA
    Inhibition of recombinant human ALK expressed in HEK293 cells assessed as reduction in ALK autophosphorylation at Tyr1604 residue incubated for 60 mins by sandwich ELISA
    [PMID: 31009559]
    NCI-H2228 IC50
    2.5 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H2228 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H2228 cells after 72 hrs by MTT assay
    [PMID: 29091425]
    NCI-H2228 IC50
    0.64 3
    Compound: 1; PF-02341066
    Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31569004]
    HEL IC50
    4.725 3
    Compound: 4
    Antiproliferative activity against HEL cells harboring JAK2 V617F mutant measured after 3 days by CCK8 assay
    Antiproliferative activity against HEL cells harboring JAK2 V617F mutant measured after 3 days by CCK8 assay
    [PMID: 30981578]
    NCI-H2228 IC50
    2.62 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H2228 cells harboring EML4/ALK L1196M mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H2228 cells harboring EML4/ALK L1196M mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34237620]
    HT-29 GI50
    4 3
    Compound: 2
    Antiproliferative activity against human HT-29 cells harbouring wild-type KRAS and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human HT-29 cells harbouring wild-type KRAS and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    NCI-H2228 IC50
    0.087 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay
    [PMID: 30223120]
    NCI-H2228 IC50
    0.24 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay
    [PMID: 29174809]
    HT-29 IC50
    > 10 3
    Compound: Crizotinib
    Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    [PMID: 27474925]
    NCI-H2228 IC50
    1.92 3
    Compound: Crizotinib
    Cytotoxicity against human NCI-H2228 cells harboring EML4-ALK fusion protein assessed as decrease in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human NCI-H2228 cells harboring EML4-ALK fusion protein assessed as decrease in cell viability after 72 hrs by MTT assay
    [PMID: 30108712]
    NCI-H2228 IC50
    0.27 3
    Compound: Crizotinib
    Cytotoxicity against human NCI-H2228 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human NCI-H2228 cells incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    NCI-H2228 IC50
    2.8 3
    Compound: PF-02341066
    Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay
    Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay
    [PMID: 31425908]
    NCI-H3122 GI50
    0.037 3
    Compound: 9
    Antiproliferative activity against human NCI-H3122 cells harboring EML4-fused ALK varian1 after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human NCI-H3122 cells harboring EML4-fused ALK varian1 after 72 hrs by CellTiter-Glo assay
    [PMID: 28850922]
    NCI-H3122 IC50
    6.27 3
    Compound: Crizotinib
    Antiproliferative activity against ALK-addicted human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against ALK-addicted human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31260890]
    NCI-H3122 IC50
    0.8 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H3122 cells after 48 hrs by MTT assay
    Antiproliferative activity against human NCI-H3122 cells after 48 hrs by MTT assay
    [PMID: 29174814]
    HepG2 IC50
    0.32 3
    Compound: Crizotinib
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34237620]
    NCI-H3122 IC50
    0.092 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell proliferation
    Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell proliferation
    [PMID: 30114660]
    HepG2 IC50
    3.7 3
    Compound: Crizotinib
    Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27396929]
    NCI-H441 IC50
    17.25 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H441 cells after 72 hrs
    Antiproliferative activity against human NCI-H441 cells after 72 hrs
    [PMID: 23993328]
    NCI-H460 IC50
    2.244 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by Alamarblue assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by Alamarblue assay
    [PMID: 29202410]
    NCI-H460 IC50
    >1 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    [PMID: 29174809]
    Jurkat IC50
    2.38 3
    Compound: F11
    Anti-necroptosis activity against TNFalpha-induced human Jurkat cells assessed as reduction in cell viability
    Anti-necroptosis activity against TNFalpha-induced human Jurkat cells assessed as reduction in cell viability
    [PMID: 38199165]
    Jurkat IC50
    2741 1
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of LCK in human Jurkat cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    Inhibition of LCK in human Jurkat cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    [PMID: 21812414]
    NCI-H3122 IC50
    261.2 1
    Compound: 1
    Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs
    Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs
    [PMID: 26476749]
    Jurkat IC50
    > 40 3
    Compound: 70
    Anti-neprotic activity in human Jurkat cells FADD defient assessed as reduction in TNFalpha-induced necroptosis preincubated for 30 mins followed by addition of TNFalpha-stimulation and further incubated for over night by Cell Titer Glo assay
    Anti-neprotic activity in human Jurkat cells FADD defient assessed as reduction in TNFalpha-induced necroptosis preincubated for 30 mins followed by addition of TNFalpha-stimulation and further incubated for over night by Cell Titer Glo assay
    [PMID: 31622096]
    NCI-H460 IC50
    >10 3
    Compound: Crizotinib
    Cytotoxicity against human NCI-H460 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human NCI-H460 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    [PMID: 27474925]
    KARPAS-299 GI50
    119 1
    Compound: Crizotinib
    Growth inhibition of human Karpas-299 cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay
    Growth inhibition of human Karpas-299 cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay
    [PMID: 27780853]
    NCI-H661 IC50
    11.47 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H661 cells after 72 hrs
    Antiproliferative activity against human NCI-H661 cells after 72 hrs
    [PMID: 23993328]
    NIH3T3 IC50
    283 1
    Compound: 1; PF-2341066
    Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    KARPAS-299 IC50
    0.03 3
    Compound: 1; PF-02341066
    Antiproliferative activity against human KARPAS299 cells expressing NMP-ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human KARPAS299 cells expressing NMP-ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31569004]
    KARPAS-299 IC50
    0.068 3
    Compound: Crizotinib
    Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay
    [PMID: 27474925]
    BaF3 IC50
    284 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BaF3 cells harbouring ALK C1156Y mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    Antiproliferative activity against mouse BaF3 cells harbouring ALK C1156Y mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    [PMID: 35421578]
    KARPAS-299 IC50
    0.087 3
    Compound: Crizotinib
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay
    [PMID: 29174809]
    HEK293 IC50
    294 1
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of AXL in human HEK293 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    Inhibition of AXL in human HEK293 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    [PMID: 21812414]
    KARPAS-299 IC50
    0.087 3
    Compound: PF-02341066
    Cytotoxicity against human KARPAS299 cells harboring NMP-ALK incubated for 72 hrs by MTT assay
    Cytotoxicity against human KARPAS299 cells harboring NMP-ALK incubated for 72 hrs by MTT assay
    [PMID: 33069075]
    NCI-H3122 IC50
    300 1
    Compound: Crizotinib
    Inhibition of E13;A20 EML4-ALK variant (unknown origin) expressed in human NCI-H3122 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    Inhibition of E13;A20 EML4-ALK variant (unknown origin) expressed in human NCI-H3122 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    [PMID: 26844689]
    KARPAS-299 IC50
    0.097 3
    Compound: Crizotinib
    Cytotoxicity against human KARPAS299 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human KARPAS299 cells incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    NCI-H3122 IC50
    303 1
    Compound: 1
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    NIH3T3 IC50
    0.364 3
    Compound: Crizotinib
    Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay
    Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay
    [PMID: 24900830]
    KARPAS-299 IC50
    0.24 3
    Compound: Crizotinib
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay
    [PMID: 30223120]
    KARPAS-299 IC50
    103 1
    Compound: 1; PF-2341066
    Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    BaF3 IC50
    328 1
    Compound: 4
    Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    KARPAS-299 IC50
    104.9 1
    Compound: Crizotinib
    Antiproliferative activity against ALK constitutively activated human KARPAS299 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against ALK constitutively activated human KARPAS299 cells after 72 hrs by SRB or CCK8 assay
    [PMID: 27769623]
    BaF3 IC50
    340 1
    Compound: 1
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    KARPAS-299 IC50
    365 1
    Compound: Crizotinib
    Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
    Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
    [PMID: 27144831]
    KARPAS-299 IC50
    1331.74 1
    Compound: Crizotinib
    Antiproliferative activity against human KARPAS299 cells after 3 days by MTT assay
    Antiproliferative activity against human KARPAS299 cells after 3 days by MTT assay
    [PMID: 30777610]
    KARPAS-299 IC50
    138 1
    Compound: Crizotinib
    Antiproliferative activity against human KARPAS-299 cells harbouring wild type ALK assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    Antiproliferative activity against human KARPAS-299 cells harbouring wild type ALK assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    [PMID: 35421578]
    SK-N-SH EC50
    370 1
    Compound: 4
    Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    KARPAS-299 IC50
    176 1
    Compound: 1
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    PANC-03-27 GI50
    6.348 3
    Compound: 2
    Antiproliferative activity against human Panc 03.27 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human Panc 03.27 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    KARPAS-299 IC50
    20 1
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of ALK in human KARPAS299 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    Inhibition of ALK in human KARPAS299 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    [PMID: 21812414]
    PANC-1 GI50
    2.559 3
    Compound: 2
    Antiproliferative activity against human PANC-1 cells harbouring KRAS G12D mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human PANC-1 cells harbouring KRAS G12D mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    KARPAS-299 IC50
    200 1
    Compound: Crizotinib
    Antiproliferative activity against human KARPAS-299 cells
    Antiproliferative activity against human KARPAS-299 cells
    [PMID: 38733884]
    NCI-H2228 IC50
    437.9 1
    Compound: 1
    Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    [PMID: 36332597]
    NIH3T3 IC50
    478 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    KARPAS-299 IC50
    200 1
    Compound: Crizotinib, PF2341066
    Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs
    Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs
    [PMID: 24900831]
    KARPAS-299 IC50
    365 1
    Compound: Crizotinib
    Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
    Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
    [PMID: 27144831]
    NIH3T3 IC50
    478 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    KARPAS-299 IC50
    62 1
    Compound: 1, Xalkori
    Inhibition of ALK-fusion driven cell proliferation in human KARPAS299 cells after 72 hrs by CellTiter Glo assay
    Inhibition of ALK-fusion driven cell proliferation in human KARPAS299 cells after 72 hrs by CellTiter Glo assay
    [PMID: 24432909]
    GBM IC50
    480 1
    Compound: 5
    Synergistic antiproliferative activity against patient-derived GBM cells assessed as reduction in cell viability after 48 hrs in presence of temozolomide by 5-Ethynyl-2'-deoxyuridine incorporation assay
    Synergistic antiproliferative activity against patient-derived GBM cells assessed as reduction in cell viability after 48 hrs in presence of temozolomide by 5-Ethynyl-2'-deoxyuridine incorporation assay
    [PMID: 31378572]
    KARPAS-299 IC50
    64.2 1
    Compound: 1, PF-02341066
    Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay
    Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay
    [PMID: 23742252]
    PC-3 IC50
    9.787 3
    Compound: Crizotinib
    Antiproliferative activity against human PC3 cells after 72 hrs by Alamarblue assay
    Antiproliferative activity against human PC3 cells after 72 hrs by Alamarblue assay
    [PMID: 29202410]
    BaF3 IC50
    512 1
    Compound: 4
    Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    SH-SY5Y EC50
    523 1
    Compound: 4
    Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    GBM IC50
    540 1
    Compound: 5
    Antiproliferative activity against patient-derived GBM cells assessed as reduction in cell viability after 48 hrs by 5-Ethynyl-2'-deoxyuridine incorporation assay
    Antiproliferative activity against patient-derived GBM cells assessed as reduction in cell viability after 48 hrs by 5-Ethynyl-2'-deoxyuridine incorporation assay
    [PMID: 31378572]
    BaF3 IC50
    549 1
    Compound: 4
    Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    564 1
    Compound: 1
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    Kelly EC50
    211 1
    Compound: 4
    Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    Kelly IC50
    0.42 3
    Compound: 2, PF-2341066
    Cytotoxicity against human Kelly cells expressing ALK F1174L mutant
    Cytotoxicity against human Kelly cells expressing ALK F1174L mutant
    [PMID: 21572589]
    BaF3 IC50
    594 1
    Compound: 1
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    Kelly IC50
    > 1000 1
    Compound: Crizotinib
    Antiproliferative activity against crizotinib-resistant human Kelly cells harboring ALK F1174L mutant after 72 hrs by MTT assay
    Antiproliferative activity against crizotinib-resistant human Kelly cells harboring ALK F1174L mutant after 72 hrs by MTT assay
    [PMID: 24785465]
    NIH3T3 IC50
    605 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    605 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    MCF7 IC50
    0.045 3
    Compound: Crizotinib
    Antiproliferative activity against human MCF7 cells after 72 hrs by Alamarblue assay relative to control
    Antiproliferative activity against human MCF7 cells after 72 hrs by Alamarblue assay relative to control
    [PMID: 29202410]
    NIH3T3 IC50
    606 1
    Compound: Crizotinib
    Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1/L1196M mutant after 72 hrs by MTT assay
    Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1/L1196M mutant after 72 hrs by MTT assay
    [PMID: 24785465]
    MCF7 IC50
    9.58 3
    Compound: Crizotinib
    Antiproliferative activity against human MCF7 cells after 72 hrs
    Antiproliferative activity against human MCF7 cells after 72 hrs
    [PMID: 23993328]
    NCI-H3122 IC50
    623 1
    Compound: 1, Xalkori
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK G1269A mutant after 72 hrs by CellTiter Glo assay
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK G1269A mutant after 72 hrs by CellTiter Glo assay
    [PMID: 24432909]
    NIH3T3 IC50
    626 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    626 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    BaF3 IC50
    643.5 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 31260890]
    BaF3 IC50
    644 1
    Compound: 1
    Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    BaF3 IC50
    645 1
    Compound: 4
    Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    704 1
    Compound: Crizotinib
    Antiproliferative activity against mouse BaF3 cells harbouring ALK L1196M mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    Antiproliferative activity against mouse BaF3 cells harbouring ALK L1196M mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay
    [PMID: 35421578]
    RD CC50
    >10 3
    Compound: 21
    Cytotoxicity against human RD cells
    Cytotoxicity against human RD cells
    [PMID: 33539089]
    MDA-MB-231 IC50
    0.79 3
    Compound: Crizotinib
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34237620]
    NCI-H3122 IC50
    838 1
    Compound: 1, Xalkori
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK L1196M mutant after 72 hrs by CellTiter Glo assay
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK L1196M mutant after 72 hrs by CellTiter Glo assay
    [PMID: 24432909]
    NIH3T3 IC50
    843 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    MDA-MB-231 IC50
    10.8 3
    Compound: Crizotinib
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs
    [PMID: 23993328]
    MDA-MB-231 IC50
    8.37 3
    Compound: Crizotinib
    Antiproliferative activity against human MDA-MB-231 cells harboring wild type BRCA and c-Met amplification assessed as inhibition of cell growth incubated for 7 days by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells harboring wild type BRCA and c-Met amplification assessed as inhibition of cell growth incubated for 7 days by MTT assay
    [PMID: 38477575]
    NIH3T3 IC50
    843 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    BaF3 IC50
    857 1
    Compound: 4
    Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    HCC78 IC50
    889 1
    Compound: 1
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    BaF3 IC50
    927 1
    Compound: 4
    Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    MDA-MB-468 IC50
    4.54 3
    Compound: Crizotinib
    Antiproliferative activity against human MDA-MB-468 cells harboring wild type BRCA1/2, HR-proficient and non-c-Met amplification assessed as inhibition of cell growth incubated for 7 days by MTT assay
    Antiproliferative activity against human MDA-MB-468 cells harboring wild type BRCA1/2, HR-proficient and non-c-Met amplification assessed as inhibition of cell growth incubated for 7 days by MTT assay
    [PMID: 38477575]
    NIH3T3 IC50
    1026 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    1026 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NIH3T3 IC50
    1148 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    1160 1
    Compound: 1; PF-2341066
    Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    Sf9 IC50
    1.36 3
    Compound: 4
    Inhibition of human recombinant C-terminal hexahistidine tagged JAK3 JH1 catalytic domain (811 to 1124 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    Inhibition of human recombinant C-terminal hexahistidine tagged JAK3 JH1 catalytic domain (811 to 1124 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    [PMID: 30981578]
    MIA PaCa-2 GI50
    1.457 3
    Compound: 2
    Antiproliferative activity against human MIA PaCa-2 cells harbouring KRAS G12C mutant and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human MIA PaCa-2 cells harbouring KRAS G12C mutant and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    MIA PaCa-2 IC50
    7.16 3
    Compound: Crizotinib
    Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27396929]
    KARPAS-299 IC50
    1331.74 1
    Compound: Crizotinib
    Antiproliferative activity against human KARPAS299 cells after 3 days by MTT assay
    Antiproliferative activity against human KARPAS299 cells after 3 days by MTT assay
    [PMID: 30777610]
    Sf9 IC50
    0.563 3
    Compound: 4
    Inhibition of human recombinant N-terminal hexahistidine tagged JAK1 JH1 catalytic domain (854 to 1154 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    Inhibition of human recombinant N-terminal hexahistidine tagged JAK1 JH1 catalytic domain (854 to 1154 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    [PMID: 30981578]
    Sf9 IC50
    0.027 3
    Compound: 4
    Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    [PMID: 30981578]
    SK-N-FI EC50
    1469 1
    Compound: 4
    Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    MKN-45 IC50
    0.013 3
    Compound: Crizotinib
    Antiproliferative activity against human MKN45 cells after 72 hrs
    Antiproliferative activity against human MKN45 cells after 72 hrs
    [PMID: 23993328]
    SK-N-AS EC50
    1473 1
    Compound: 4
    Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    MKN-45 IC50
    0.022 3
    Compound: Crizotinib
    Antiproliferative activity against human MKN45 cells after 72 hrs by Alamarblue assay
    Antiproliferative activity against human MKN45 cells after 72 hrs by Alamarblue assay
    [PMID: 29202410]
    BaF3 IC50
    1643 1
    Compound: 1, PF-02341066
    Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    [PMID: 23742252]
    SGC-7901 IC50
    0.3213 3
    Compound: Crizotinib
    Antiproliferative activity against human SGC7901 cells after 72 hrs by Alamarblue assay relative to control
    Antiproliferative activity against human SGC7901 cells after 72 hrs by Alamarblue assay relative to control
    [PMID: 29202410]
    MKN-45 IC50
    15 1
    Compound: 2
    Antiproliferative activity against human MKN-45 cells incubated for 72 hrs
    Antiproliferative activity against human MKN-45 cells incubated for 72 hrs
    [PMID: 33957388]
    SH-SY5Y IC50
    0.92 3
    Compound: Crizotinib
    Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    [PMID: 36208544]
    MKN-45 IC50
    38.1 1
    Compound: 1
    Antiproliferative activity against human MKN45 cells after 72 hrs
    Antiproliferative activity against human MKN45 cells after 72 hrs
    [PMID: 26005523]
    SH-SY5Y IC50
    0.85 3
    Compound: 1; PF-02341066
    Antiproliferative activity against human SH-SY5Y cells expressing ALK F1174L mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human SH-SY5Y cells expressing ALK F1174L mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31569004]
    MKN-45 IC50
    9.1 1
    Compound: 1; PF-0234106
    Antiproliferative activity against human MKN45 cells overexpressing c-MET assessed as reduction in cell proliferation
    Antiproliferative activity against human MKN45 cells overexpressing c-MET assessed as reduction in cell proliferation
    [PMID: 32371098]
    SH-SY5Y IC50
    0.32 3
    Compound: Crizotinib
    Antiproliferative activity against human SH-SY5Y cells harboring ALK F1174L mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human SH-SY5Y cells harboring ALK F1174L mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34237620]
    SH-SY5Y IC50
    0.53 3
    Compound: 2, PF-2341066
    Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant
    Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant
    [PMID: 21572589]
    NCI-H1975 IC50
    7.551 3
    Compound: Crizotinib
    Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay
    Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay
    [PMID: 24900830]
    NCI-H1975 IC50
    > 10 3
    Compound: PF-02341066
    Cytotoxicity against EGFR-positive human H1975 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against EGFR-positive human H1975 cells incubated for 72 hrs by MTT assay
    [PMID: 33069075]
    U-937 IC50
    2286 1
    Compound: Crizotinib
    Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
    Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
    [PMID: 27144831]
    SK-MEL-28 IC50
    10.97 3
    Compound: Crizotinib
    Antiproliferative activity against human SK-MEL-28 cells after 72 hrs
    Antiproliferative activity against human SK-MEL-28 cells after 72 hrs
    [PMID: 23993328]
    NCI-H1993 IC50
    0.061 3
    Compound: Crizotinib
    Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay
    Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay
    [PMID: 24900830]
    NCI-H1993 IC50
    3 3
    Compound: 12
    Cytotoxicity against human NCI-H1993 cells assessed as inhibition of cell growth
    Cytotoxicity against human NCI-H1993 cells assessed as inhibition of cell growth
    [PMID: 32858470]
    SK-N-AS IC50
    12.12 3
    Compound: Crizotinib
    Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    [PMID: 36208544]
    Jurkat IC50
    2741 1
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of LCK in human Jurkat cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    Inhibition of LCK in human Jurkat cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    [PMID: 21812414]
    NCI-H2228 GI50
    0.073 3
    Compound: 9
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-fused ALK varian3 after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-fused ALK varian3 after 72 hrs by CellTiter-Glo assay
    [PMID: 28850922]
    SK-OV-3 IC50
    12.85 3
    Compound: Crizotinib
    Antiproliferative activity against human SKOV3 cells after 72 hrs
    Antiproliferative activity against human SKOV3 cells after 72 hrs
    [PMID: 23993328]
    NCI-H2228 GI50
    121 1
    Compound: Crizotinib
    Growth inhibition of human NCI-H2228 cells harboring EML4-ALK v3a/3b incubated for 72 hrs by CyQuant cell proliferation assay
    Growth inhibition of human NCI-H2228 cells harboring EML4-ALK v3a/3b incubated for 72 hrs by CyQuant cell proliferation assay
    [PMID: 27780853]
    HEK293 IC50
    2887 1
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of IR in human HEK293 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    Inhibition of IR in human HEK293 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    [PMID: 21812414]
    NCI-H2228 IC50
    0.087 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay
    [PMID: 30223120]
    NIH3T3 IC50
    3039 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    3039 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NCI-H2228 IC50
    0.24 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay
    [PMID: 29174809]
    GBM EC50
    3200 1
    Compound: 5
    Synergistic antiproliferative activity against patient-derived GBM cells assessed as cell viability after 48 hrs in presence of temozolomide by 5-Ethynyl-2'-deoxyuridine incorporation assay
    Synergistic antiproliferative activity against patient-derived GBM cells assessed as cell viability after 48 hrs in presence of temozolomide by 5-Ethynyl-2'-deoxyuridine incorporation assay
    [PMID: 31378572]
    NCI-H2228 IC50
    0.27 3
    Compound: Crizotinib
    Cytotoxicity against human NCI-H2228 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human NCI-H2228 cells incubated for 72 hrs by MTT assay
    [PMID: 30927566]
    NCI-H2228 IC50
    0.64 3
    Compound: 1; PF-02341066
    Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31569004]
    SNU-5 IC50
    0.016 3
    Compound: Crizotinib
    Antiproliferative activity against human SNU5 cells after 72 hrs
    Antiproliferative activity against human SNU5 cells after 72 hrs
    [PMID: 23993328]
    NCI-H2228 IC50
    1.92 3
    Compound: Crizotinib
    Cytotoxicity against human NCI-H2228 cells harboring EML4-ALK fusion protein assessed as decrease in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human NCI-H2228 cells harboring EML4-ALK fusion protein assessed as decrease in cell viability after 72 hrs by MTT assay
    [PMID: 30108712]
    BaF3 IC50
    3479 1
    Compound: 1, PF-02341066
    Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
    [PMID: 23742252]
    NCI-H2228 IC50
    118 1
    Compound: 1, Xalkori
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H2228 cells after 72 hrs by CellTiter Glo assay
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H2228 cells after 72 hrs by CellTiter Glo assay
    [PMID: 24432909]
    SU-DHL-1 IC50
    0.01 3
    Compound: 2, PF-2341066
    Cytotoxicity against human SU-DHL1 cells expressing ALK coexpressing NPM
    Cytotoxicity against human SU-DHL1 cells expressing ALK coexpressing NPM
    [PMID: 21572589]
    NCI-H2228 IC50
    2.5 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H2228 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H2228 cells after 72 hrs by MTT assay
    [PMID: 29091425]
    SW480 GI50
    >10 3
    Compound: 2
    Antiproliferative activity against human SW480 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human SW480 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    NCI-H2228 IC50
    2.62 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H2228 cells harboring EML4/ALK L1196M mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H2228 cells harboring EML4/ALK L1196M mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34237620]
    GBM EC50
    5600 1
    Compound: 5
    Antiproliferative activity against patient-derived GBM cells assessed as cell viability after 48 hrs by 5-Ethynyl-2'-deoxyuridine incorporation assay
    Antiproliferative activity against patient-derived GBM cells assessed as cell viability after 48 hrs by 5-Ethynyl-2'-deoxyuridine incorporation assay
    [PMID: 31378572]
    NCI-H2228 IC50
    2.8 3
    Compound: PF-02341066
    Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay
    Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay
    [PMID: 31425908]
    U-87MG ATCC IC50
    7.29 3
    Compound: Cri
    Anti-proliferative activity against human U-87 MG cells assessed as cell viability incubated for 2 hrs by CCK8 assay
    Anti-proliferative activity against human U-87 MG cells assessed as cell viability incubated for 2 hrs by CCK8 assay
    [PMID: 37861443]
    NCI-H2228 IC50
    202 1
    Compound: Crizotinib
    Inhibition of E6a/b;A20 EML4-ALK (unknown origin) expressed in human NCI-H2228 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    Inhibition of E6a/b;A20 EML4-ALK (unknown origin) expressed in human NCI-H2228 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    [PMID: 26844689]
    A549 IC50
    >1 1
    Compound: Crizotinib
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 24785465]
    Vero CC50
    4.23 3
    Compound: 51
    Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by coulter counter method
    Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by coulter counter method
    [PMID: 32883635]
    NCI-H2228 IC50
    437.9 1
    Compound: 1
    Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H2228 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    [PMID: 36332597]
    NCI-H23 GI50
    1773 1
    Compound: Crizotinib
    Growth inhibition of ALK-negative human NCI-H23 cells incubated for 72 hrs by CyQuant cell proliferation assay
    Growth inhibition of ALK-negative human NCI-H23 cells incubated for 72 hrs by CyQuant cell proliferation assay
    [PMID: 27780853]
    NCI-H3122 EC50
    32 1
    Compound: 4
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    NCI-H3122 GI50
    0.037 3
    Compound: 9
    Antiproliferative activity against human NCI-H3122 cells harboring EML4-fused ALK varian1 after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human NCI-H3122 cells harboring EML4-fused ALK varian1 after 72 hrs by CellTiter-Glo assay
    [PMID: 28850922]
    NCI-H3122 GI50
    62 1
    Compound: Crizotinib
    Growth inhibition of human NCI-H3122 cells harboring EML4-ALK v1 incubated for 72 hrs by CyQuant cell proliferation assay
    Growth inhibition of human NCI-H3122 cells harboring EML4-ALK v1 incubated for 72 hrs by CyQuant cell proliferation assay
    [PMID: 27780853]
    NCI-H3122 IC50
    0.092 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell proliferation
    Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell proliferation
    [PMID: 30114660]
    NCI-H3122 IC50
    0.8 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H3122 cells after 48 hrs by MTT assay
    Antiproliferative activity against human NCI-H3122 cells after 48 hrs by MTT assay
    [PMID: 29174814]
    NCI-H3122 IC50
    100.9 1
    Compound: Crizotinib
    Antiproliferative activity against ALK constitutively activated human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against ALK constitutively activated human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
    [PMID: 27769623]
    NCI-H3122 IC50
    108 1
    Compound: 1, Xalkori
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells after 72 hrs by CellTiter Glo assay
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells after 72 hrs by CellTiter Glo assay
    [PMID: 24432909]
    NCI-H3122 IC50
    180 1
    Compound: 1; PF2341066
    Cytotoxicity against human NCI-H3122 cells harboring EML4-ALK E13;A20 mutant incubated for 72 hrs by Cell titer blue assay
    Cytotoxicity against human NCI-H3122 cells harboring EML4-ALK E13;A20 mutant incubated for 72 hrs by Cell titer blue assay
    [PMID: 31419130]
    NCI-H3122 IC50
    210 1
    Compound: 1; PF-2341066
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    NCI-H3122 IC50
    261.2 1
    Compound: 1
    Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs
    Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs
    [PMID: 26476749]
    NCI-H3122 IC50
    300 1
    Compound: Crizotinib
    Inhibition of E13;A20 EML4-ALK variant (unknown origin) expressed in human NCI-H3122 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    Inhibition of E13;A20 EML4-ALK variant (unknown origin) expressed in human NCI-H3122 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    [PMID: 26844689]
    NCI-H3122 IC50
    303 1
    Compound: 1
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    NCI-H3122 IC50
    6.27 3
    Compound: Crizotinib
    Antiproliferative activity against ALK-addicted human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against ALK-addicted human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31260890]
    NCI-H3122 IC50
    623 1
    Compound: 1, Xalkori
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK G1269A mutant after 72 hrs by CellTiter Glo assay
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK G1269A mutant after 72 hrs by CellTiter Glo assay
    [PMID: 24432909]
    NCI-H3122 IC50
    838 1
    Compound: 1, Xalkori
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK L1196M mutant after 72 hrs by CellTiter Glo assay
    Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK L1196M mutant after 72 hrs by CellTiter Glo assay
    [PMID: 24432909]
    NCI-H441 IC50
    17.25 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H441 cells after 72 hrs
    Antiproliferative activity against human NCI-H441 cells after 72 hrs
    [PMID: 23993328]
    NCI-H460 IC50
    2.244 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by Alamarblue assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by Alamarblue assay
    [PMID: 29202410]
    NCI-H460 IC50
    > 1 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    [PMID: 29174809]
    NCI-H460 IC50
    > 10 3
    Compound: Crizotinib
    Cytotoxicity against human NCI-H460 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human NCI-H460 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
    [PMID: 27474925]
    NCI-H661 IC50
    11.47 3
    Compound: Crizotinib
    Antiproliferative activity against human NCI-H661 cells after 72 hrs
    Antiproliferative activity against human NCI-H661 cells after 72 hrs
    [PMID: 23993328]
    NCI-H838 GI50
    1307 1
    Compound: Crizotinib
    Growth inhibition of ALK-negative human NCI-H838 cells incubated for 72 hrs by CyQuant cell proliferation assay
    Growth inhibition of ALK-negative human NCI-H838 cells incubated for 72 hrs by CyQuant cell proliferation assay
    [PMID: 27780853]
    NIH3T3 IC50
    0.364 3
    Compound: Crizotinib
    Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay
    Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay
    [PMID: 24900830]
    NIH3T3 IC50
    1026 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    1026 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NIH3T3 IC50
    1148 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    1160 1
    Compound: 1; PF-2341066
    Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    NIH3T3 IC50
    165 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    165 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NIH3T3 IC50
    283 1
    Compound: 1; PF-2341066
    Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    NIH3T3 IC50
    3039 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    3039 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NIH3T3 IC50
    478 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    478 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NIH3T3 IC50
    605 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    605 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NIH3T3 IC50
    606 1
    Compound: Crizotinib
    Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1/L1196M mutant after 72 hrs by MTT assay
    Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1/L1196M mutant after 72 hrs by MTT assay
    [PMID: 24785465]
    NIH3T3 IC50
    626 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    626 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NIH3T3 IC50
    80 1
    Compound: 1, PF-02341066
    Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
    Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    80 1
    Compound: 1, Xalkori
    Inhibition of human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
    Inhibition of human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NIH3T3 IC50
    80 1
    Compound: 63, Crizotinib, PF-02341066
    Inhibition of RON in mouse 3T3 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    Inhibition of RON in mouse 3T3 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method
    [PMID: 21812414]
    NIH3T3 IC50
    843 1
    Compound: 1, PF-02341066
    Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24819116]
    NIH3T3 IC50
    843 1
    Compound: 1, Xalkori
    Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    [PMID: 24432909]
    NIH3T3 IC50
    95.4 1
    Compound: Crizotinib
    Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1 after 72 hrs by MTT assay
    Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1 after 72 hrs by MTT assay
    [PMID: 24785465]
    PANC-03-27 GI50
    6.348 3
    Compound: 2
    Antiproliferative activity against human Panc 03.27 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human Panc 03.27 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    PANC-1 GI50
    2.559 3
    Compound: 2
    Antiproliferative activity against human PANC-1 cells harbouring KRAS G12D mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human PANC-1 cells harbouring KRAS G12D mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    PC-3 IC50
    9.787 3
    Compound: Crizotinib
    Antiproliferative activity against human PC3 cells after 72 hrs by Alamarblue assay
    Antiproliferative activity against human PC3 cells after 72 hrs by Alamarblue assay
    [PMID: 29202410]
    RD CC50
    > 10 3
    Compound: 21
    Cytotoxicity against human RD cells
    Cytotoxicity against human RD cells
    [PMID: 33539089]
    SGC-7901 IC50
    0.3213 3
    Compound: Crizotinib
    Antiproliferative activity against human SGC7901 cells after 72 hrs by Alamarblue assay relative to control
    Antiproliferative activity against human SGC7901 cells after 72 hrs by Alamarblue assay relative to control
    [PMID: 29202410]
    SH-SY5Y EC50
    523 1
    Compound: 4
    Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    SH-SY5Y IC50
    0.32 3
    Compound: Crizotinib
    Antiproliferative activity against human SH-SY5Y cells harboring ALK F1174L mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human SH-SY5Y cells harboring ALK F1174L mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 34237620]
    SH-SY5Y IC50
    0.53 3
    Compound: 2, PF-2341066
    Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant
    Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant
    [PMID: 21572589]
    SH-SY5Y IC50
    0.85 3
    Compound: 1; PF-02341066
    Antiproliferative activity against human SH-SY5Y cells expressing ALK F1174L mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human SH-SY5Y cells expressing ALK F1174L mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31569004]
    SH-SY5Y IC50
    0.92 3
    Compound: Crizotinib
    Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    [PMID: 36208544]
    SK-MEL-28 IC50
    10.97 3
    Compound: Crizotinib
    Antiproliferative activity against human SK-MEL-28 cells after 72 hrs
    Antiproliferative activity against human SK-MEL-28 cells after 72 hrs
    [PMID: 23993328]
    SK-N-AS EC50
    1473 1
    Compound: 4
    Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    SK-N-AS IC50
    12.12 3
    Compound: Crizotinib
    Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    [PMID: 36208544]
    SK-N-FI EC50
    1469 1
    Compound: 4
    Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    SK-N-SH EC50
    370 1
    Compound: 4
    Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    SK-OV-3 IC50
    12.85 3
    Compound: Crizotinib
    Antiproliferative activity against human SKOV3 cells after 72 hrs
    Antiproliferative activity against human SKOV3 cells after 72 hrs
    [PMID: 23993328]
    SNU-5 IC50
    0.016 3
    Compound: Crizotinib
    Antiproliferative activity against human SNU5 cells after 72 hrs
    Antiproliferative activity against human SNU5 cells after 72 hrs
    [PMID: 23993328]
    SNU-5 IC50
    20.4 1
    Compound: 1
    Antiproliferative activity against human SNU5 cells after 72 hrs
    Antiproliferative activity against human SNU5 cells after 72 hrs
    [PMID: 26005523]
    SU-DHL-1 GI50
    99 1
    Compound: Crizotinib
    Growth inhibition of human SU-DHL-1 cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay
    Growth inhibition of human SU-DHL-1 cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay
    [PMID: 27780853]
    SU-DHL-1 IC50
    0.01 3
    Compound: 2, PF-2341066
    Cytotoxicity against human SU-DHL1 cells expressing ALK coexpressing NPM
    Cytotoxicity against human SU-DHL1 cells expressing ALK coexpressing NPM
    [PMID: 21572589]
    SU-DHL-1 IC50
    136 1
    Compound: 1; PF-2341066
    Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    SU-DHL-1 IC50
    155 1
    Compound: 1
    Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    [PMID: 29288940]
    SU-DHL-1 IC50
    92.3 1
    Compound: Crizotinib
    Antiproliferative activity against ALK constitutively activated human SU-DHL1 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against ALK constitutively activated human SU-DHL1 cells after 72 hrs by SRB or CCK8 assay
    [PMID: 27769623]
    SW480 GI50
    > 10 3
    Compound: 2
    Antiproliferative activity against human SW480 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    Antiproliferative activity against human SW480 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay
    [PMID: 37736180]
    Sf9 IC50
    0.027 3
    Compound: 4
    Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    [PMID: 30981578]
    Sf9 IC50
    0.563 3
    Compound: 4
    Inhibition of human recombinant N-terminal hexahistidine tagged JAK1 JH1 catalytic domain (854 to 1154 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    Inhibition of human recombinant N-terminal hexahistidine tagged JAK1 JH1 catalytic domain (854 to 1154 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    [PMID: 30981578]
    Sf9 IC50
    1.36 3
    Compound: 4
    Inhibition of human recombinant C-terminal hexahistidine tagged JAK3 JH1 catalytic domain (811 to 1124 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    Inhibition of human recombinant C-terminal hexahistidine tagged JAK3 JH1 catalytic domain (811 to 1124 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr
    [PMID: 30981578]
    U-87MG ATCC IC50
    7.29 3
    Compound: Cri
    Anti-proliferative activity against human U-87 MG cells assessed as cell viability incubated for 2 hrs by CCK8 assay
    Anti-proliferative activity against human U-87 MG cells assessed as cell viability incubated for 2 hrs by CCK8 assay
    [PMID: 37861443]
    U-937 GI50
    928 1
    Compound: Crizotinib
    Growth inhibition of ALK-negative human U-937 cells incubated for 72 hrs by CyQuant cell proliferation assay
    Growth inhibition of ALK-negative human U-937 cells incubated for 72 hrs by CyQuant cell proliferation assay
    [PMID: 27780853]
    U-937 IC50
    2286 1
    Compound: Crizotinib
    Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
    Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
    [PMID: 27144831]
    Vero CC50
    4.23 3
    Compound: 51
    Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by coulter counter method
    Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by coulter counter method
    [PMID: 32883635]
    体外実験

    Crizotinib (PF-02341066) displays similar potency against c-Met phosphorylation in mIMCD3 mouse or MDCK canine epithelial cells with IC50 of 5 nM and 20 nM, respectivly. PF-2341066 shows improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I or H1094R or the P-loop mutant M1250T with IC50 of 19 nM, 2 nM and 15 nM, respectively, compared with NIH3T3 cells expressing wild-type receptor with IC50 of 13 nM. In contrast, a marked shift in potency of PF-2341066 is observed against cells engineered to express c-Met activation loop mutants Y1230C and Y1235D with IC50 of 127 nM and 92 nM, respectively, compared with wild-type receptor. PF-2341066 also potently prevents the phosphorylation of c-Met in NCI-H69 and HOP92 cells, with IC50 of 13 nM and 16 nM, respectively, which express the endogenous c-Met variants R988C and T1010I, respectively[1].
    Crizotinib (PF-02341066) also potently inhibits NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells with an IC50 of 24 nM. PF-2341066 potently prevents cell proliferation, which is associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells with IC50 of 30 nM, but not ALK-negative lymphoma cells[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    体内実験

    Crizotinib (PF-02341066) reveals the ability to cause marked regression of large established tumors (> 600 mm3) in both the 50 mg/kg/day and 75 mg/kg/day treatment cohorts, with a 60% decrease in mean tumor volume over the 43-day administration schedule in the GTL-16 model. In an another study, PF-2341066 displays the ability to completely inhibits GTL-16 tumor growth for >3 months, with only 1 of 12 mice exhibiting a significant increase in tumor growth over the 3-month treatment schedule at 50 mg/kg/day. A significant dose-dependent reduction of CD31-positive endothelial cells is observed at 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day in GTL-16 tumors, indicating that inhibition of MVD shows a dose-dependent correlation to antitumor efficacy. PF-2341066 displays a significant dose-dependent reduction of human VEGFA and IL-8 plasma levels in both the GTL-16 and U87MG models. Marked inhibition of phosphorylated c-Met, Akt, Erk, PLCλ1, and STAT5 levels is observed in GTL-16 tumors following p.o. administration of PF-2341066[1].
    Treatment of c-MET-amplified GTL-16 xenografts with 50 mg/kg PF-2341066 elicits tumor regression that is associated with a slow reduction in 18F-FDG uptake and decreases expression of the glucose transporter 1, GLUT-1[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    臨床実験
    分子量

    450.34

    分子式

    C21H22Cl2FN5O

    CAS 番号
    Appearance

    Solid

    Color

    White to light brown

    SMILES

    ClC1=C(F)C=CC(Cl)=C1[C@H](OC2=CC(C3=CN(N=C3)C4CCNCC4)=CN=C2N)C

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 20 mg/mL (44.41 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2205 mL 11.1027 mL 22.2054 mL
    5 mM 0.4441 mL 2.2205 mL 4.4411 mL
    10 mM 0.2221 mL 1.1103 mL 2.2205 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

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    一般には略語で表示されます:C1V1 = C2V2

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    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
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    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 1.25 mg/mL (2.78 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1 mg/mL (2.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 20 mg/mL (44.41 mM); Suspended solution; Need ultrasonic and warming and heat to 40°C

    In Vivo Dissolution Calculator
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    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.97% ee.: 99.63%

    参考文献
    キナーゼ実験
    [1]

    Cells are seeded in 96-well plates in media supplemented with 10% fetal bovine serum (FBS) and transferred to serum-free media [with 0.04% bovine serum albumin (BSA)] after 24 h. In experiments investigating ligand-dependent RTK phosphorylation, corresponding growth factors are added for up to 20 min. After incubation of cells with PF-2341066 for 1 h and/or appropriate ligands for the designated times, cells are washed once with HBSS supplemented with 1 mM Na3VO4, and protein lysates are generated from cells. Subsequently, phosphorylation of selected protein kinases is assessed by a sandwich ELISA method using specific capture antibodies used to coat 96-well plates and a detection antibody specific for phosphorylated tyrosine residues. Antibody-coated plates are (a) incubated in the presence of protein lysates at 4°C overnight; (b) washed seven times in 1% Tween 20 in PBS; (c) incubated in a horseradish peroxidase-conjugated anti-total-phosphotyrosine (PY-20) antibody (1:500) for 30 min; (d) washed seven times again; (e) incubated in 3,3′,5,5′-tetramethyl benzidine peroxidase substrate to initiate a colorimetric reaction that is stopped by adding 0.09 N H2SO4; and (f) measured for absorbance in 450 nm using a spectrophotometer.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    細胞実験
    [1]

    Tumor cells are seeded in 96-well plates at low density in media supplemented with 10% FBS (growth media) and transferred to serum-free media (0% FBS and 0.04% BSA) after 24 h. Appropriate controls or designated concentrations of PF-2341066 are added to each well, and cells are incubated for 24 to 72 h. Human umbilical vascular endothelial cells (HUVEC) are seeded in 96-well plates in EGM2 media for 5 to 6 h at > 20,000 cells per well and transferred to serum-free media overnight. The following day, appropriate controls or designated concentrations of PF-2341066 are added to each well, and after 1 h incubation, HGF is added to designated wells at 100 ng/mL. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay is done to determine the relative tumor cell or HUVEC numbers.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [1]

    Athymic mice bearing xenografts (300-800 mm3) are given PF-2341066 in water by oral gavage at designated dose levels. At designated times following PF-2341066 administration, mice are humanely euthanized, and tumors are resected. Tumors are snap frozen and pulverized using a liquid nitrogen-cooled cryomortar and pestle, protein lysates are generated, and protein concentrations are determined using a BSA assay. The level of total and phosphorylated protein is determined using a capture ELISA or immunoprecipitation-immunoblotting method.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2205 mL 11.1027 mL 22.2054 mL 55.5136 mL
    5 mM 0.4441 mL 2.2205 mL 4.4411 mL 11.1027 mL
    10 mM 0.2221 mL 1.1103 mL 2.2205 mL 5.5514 mL
    15 mM 0.1480 mL 0.7402 mL 1.4804 mL 3.7009 mL
    20 mM 0.1110 mL 0.5551 mL 1.1103 mL 2.7757 mL
    25 mM 0.0888 mL 0.4441 mL 0.8882 mL 2.2205 mL
    30 mM 0.0740 mL 0.3701 mL 0.7402 mL 1.8505 mL
    40 mM 0.0555 mL 0.2776 mL 0.5551 mL 1.3878 mL
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    製品名:
    Crizotinib
    製品番号:
    HY-50878
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