Crizotinib acetate
Based on 84 publication(s) in Google Scholar
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate 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 acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition.
For research use only. We do not sell to patients.
- CAS No.: 877399-53-6
- Formula: C23H26Cl2FN5O3
- Molecular Weight:510.39
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Crizotinib acetate
More- Signal Transduct Target Ther. 2024 Mar 9;9(1):65. [Abstract]
- Cancer Discov. 2024 Sep 13:OF1-OF20. [Abstract]
- Cancer Discov. 2023 Mar 1;13(3):598-615. [Abstract]
- Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Blood. 2022 Feb 3;139(5):717-731. [Abstract]
- Cancer Res. 2015 Nov 1;75(21):4548-59. [Abstract]
- Nat Commun. 2025 Jul 17;16(1):6587. [Abstract]
- Acta Pharm Sin B. 2026 Mar 2.
- Sci Transl Med. 2021 Sep;13(609):eabb3738. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Leukemia. 2025 Aug 14. [Abstract]
- J Exp Clin Cancer Res. 2025 Jul 19;44(1):215. [Abstract]
- J Exp Clin Cancer Res. 2022 Mar 29;41(1):113. [Abstract]
- Biomark Res. 2024 Jan 25;12(1):13. [Abstract]
- EBioMedicine. 2023 Jan:87:104410. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Cell Rep Med. 2024 Mar 19;5(3):101472. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Cancer Lett. 2026 May 29:656:218624. [Abstract]
- Cancer Lett. 2018 May 28:422:19-28. [Abstract]
- J Pharm Anal. 2021 Dec;11(6):799-807. [Abstract]
- Int J Biol Macromol. 2025 Jun 4;318(Pt 1):144963. [Abstract]
- J Transl Med. 2023 Aug 5;21(1):530. [Abstract]
- Oncogene. 2024 Sep;43(40):2995-3002. [Abstract]
- Oncogene. 2018 Mar;37(11):1417-1429. [Abstract]
- Blood Adv. 2025 Jul 2:bloodadvances.2024015322. [Abstract]
- Blood Adv. 2023 Aug 8;7(15):4049-4063. [Abstract]
- Clin Transl Med. 2025 May;15(5):e70338. [Abstract]
- J Med Chem. 2024 Oct 24;67(20):18098-18123. [Abstract]
- J Med Chem. 2021 Oct 14;64(19):14344-14357. [Abstract]
- J Med Chem. 2021 Mar 11;64(5):2725-2738. [Abstract]
- Sci Signal. 2015 Dec 8;8(406):ra125. [Abstract]
- Sci Signal. 2014 Oct 28;7(349):ra102. [Abstract]
- Talanta. 2019 Aug 15:201:217-225. [Abstract]
- Eur J Med Chem. 2017 Oct 20:139:674-697. [Abstract]
- Mol Cancer Ther. 2025 Jul 2;24(7):1005-1019. [Abstract]
- J Pharm Investig. 2025 Dec 29.
- Stem Cell Reports. 2017 Dec 12;9(6):1948-1960. [Abstract]
- Int J Mol Sci. 2022 Sep 17;23(18):10895. [Abstract]
- Pharmaceuticals (Basel). 2026 Feb 27;19(3):381. [Abstract]
- Spectrochim Acta A Mol Biomol Spectrosc. 2021 Oct 5:259:119884. [Abstract]
- Spectrochim Acta A Mol Biomol Spectrosc. 2014 Oct 15;131:347-54. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Mol Oncol. 2017 Aug;11(8):996-1006. [Abstract]
- Cancers (Basel). 2024
- Cancers (Basel). 2017 Oct 30;9(11). pii: E149. [Abstract]
- Cancer Sci. 2025 Jul 23. [Abstract]
- ACS Omega. 2023 Jun 14;8(25):22603-22612. [Abstract]
- Transl Oncol. 2022 Jan;15(1):101272. [Abstract]
- Transl Oncol. 2021 Jan;14(1):100887. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2020 Jul;1867(7):118712. [Abstract]
- Proteomes. 2023 Jun 2;11(2):20. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Saudi Pharm J. 2015 Jan;23(1):75-84. [Abstract]
- Front Oncol. 2020 May 12;10:696. [Abstract]
- Dis Model Mech. 2016 Sep 1;9(9):941-52. [Abstract]
- Cancer Med. 2020 Jun;9(12):4350-4359. [Abstract]
- Arch Biochem Biophys. 2024 Mar:753:109905. [Abstract]
- J Cancer Res Clin Oncol. 2021 Jan;147(1):167-175. [Abstract]
- Invest New Drugs. 2023 Apr;41(2):254-266. [Abstract]
- PLoS One. 2025 Jan 21;20(1):e0308747. [Abstract]
- PLoS One. 2021 Jun 8;16(6):e0252907. [Abstract]
- PLoS One. 2019 Feb 11;14(2):e0212048. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Biomed Chromatogr. 2024 Oct;38(10):e5986. [Abstract]
- Biomed Chromatogr. 2019 Oct;33(10):e4611. [Abstract]
- Biol Methods Protoc. 2025 Feb 13;10(1):bpaf012. [Abstract]
- J Solution Chem. 2014 Jul;43(7):1282-1295.
- Braz J Pharm Sci. 2015 Jun;51(2):2175-9790.
- bioRxiv. 2025 Dec 5.
- Patent. US20250269018A1.
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- Eberhard Karls Universität Tübingen. 2023 Sep 18.
- Research Square Print. 26 Oct, 2022
- Research Square Print. September 14th, 2022.
- Research Square Preprint. 2022 Feb.
- Evid Based Complement Alternat Med. 2019 Nov 7;2019:4253846. [Abstract]
- Oncotarget. 2019 Aug 13;10(48):4937-4950. [Abstract]
- Technical University of Munich. 24.01.2018.
- Oncotarget. 2016 May 17;7(20):29011-22. [Abstract]
- Oncotarget. 2014 May 15;5(9):2688-702. [Abstract]
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Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>1 nM
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 μM
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 μM
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 |
>10 μM
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 |
0.008 μM
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 μM
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 |
0.41 μM
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 μM
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 μM
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 μM
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 |
4.084 μM
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 |
5.7 μM
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] |
| BaF3 | GI50 |
1.1 μM
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 μM
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 μM
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 |
>5 μM
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] |
| BaF3 | IC50 |
0.051 μM
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 |
0.19 μM
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 μM
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 |
0.28 μM
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 |
0.62 μM
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 |
0.98 μM
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 | IC50 |
111 nM
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 |
127.4 nM
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] |
| BaF3 | IC50 |
144 nM
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] |
| BaF3 | IC50 |
150.8 nM
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] |
| BaF3 | IC50 |
1643 nM
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] |
| BaF3 | IC50 |
2.2 μM
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 |
284 nM
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] |
| BaF3 | IC50 |
328 nM
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 nM
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] |
| BaF3 | IC50 |
3479 nM
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] |
| BaF3 | IC50 |
4.336 nM
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 |
48.6 nM
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 |
512 nM
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] |
| BaF3 | IC50 |
549 nM
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 nM
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 |
564 nM
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] |
| BaF3 | IC50 |
57.5 nM
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] |
| BaF3 | IC50 |
58.5 nM
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] |
| BaF3 | IC50 |
594 nM
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] |
| BaF3 | IC50 |
643.5 nM
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 nM
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 nM
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 |
65 nM
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] |
| BaF3 | IC50 |
704 nM
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] |
| BaF3 | IC50 |
81 nM
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] |
| BaF3 | IC50 |
857 nM
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 nM
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] |
| CHO | GI50 |
3.2 μM
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 μM
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 |
0.013 μM
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 |
0.021 μM
Compound: Crizotinib
|
Antiproliferative activity against human EBC1 cells after 72 hrs
Antiproliferative activity against human EBC1 cells after 72 hrs
|
[PMID: 25537530] |
| EBC-1 | IC50 |
0.023 μM
Compound: Crizotinib
|
Antiproliferative activity against human EBC1 cells after 72 hrs
Antiproliferative activity against human EBC1 cells after 72 hrs
|
[PMID: 23993328] |
| EBC-1 | IC50 |
0.044 μM
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 μM
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] |
| EBC-1 | IC50 |
19 nM
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] |
| EBC-1 | IC50 |
21.8 nM
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 nM
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] |
| EBC-1 | IC50 |
6.9 nM
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] |
| GBM | EC50 |
3200 nM
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 μM
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] |
| GBM | EC50 |
5600 nM
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] |
| GBM | IC50 |
480 nM
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 nM
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] |
| HCC78 | IC50 |
0.17 μM
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 μM
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] |
| HCC78 | IC50 |
0.17 μM
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] |
| HCC78 | IC50 |
0.23 μM
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 μM
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] |
| HCC78 | IC50 |
19.19 μM
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 |
2 μM
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] |
| HCC78 | IC50 |
889 nM
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] |
| HCC827 | IC50 |
>10 μM
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] |
| HCC827 | IC50 |
7.25 μM
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] |
| HCT-116 | IC50 |
0.2536 μM
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] |
| HCT-116 | IC50 |
14.82 μM
Compound: Crizotinib
|
Antiproliferative activity against human HCT116 cells after 72 hrs
Antiproliferative activity against human HCT116 cells after 72 hrs
|
[PMID: 23993328] |
| HEK293 | IC50 |
2887 nM
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] |
| HEK293 | IC50 |
294 nM
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 nM
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] |
| HEL | IC50 |
4.725 μM
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] |
| HepG2 | IC50 |
0.32 μM
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] |
| HepG2 | IC50 |
3.7 μM
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] |
| HT-29 | IC50 |
>10 μM
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] |
| Jurkat | IC50 |
>40 μM
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] |
| Jurkat | IC50 |
2741 nM
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] |
| KARPAS-299 | IC50 |
0.03 μM
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 μM
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] |
| KARPAS-299 | IC50 |
0.087 μM
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 |
0.087 μM
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 |
0.097 μM
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] |
| KARPAS-299 | IC50 |
0.24 μM
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 nM
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] |
| KARPAS-299 | IC50 |
104.9 nM
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] |
| KARPAS-299 | IC50 |
1331.74 nM
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 nM
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] |
| KARPAS-299 | IC50 |
176 nM
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] |
| KARPAS-299 | IC50 |
20 nM
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] |
| KARPAS-299 | IC50 |
200 nM
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 nM
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 |
62 nM
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 nM
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] |
| Kelly | EC50 |
211 nM
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 |
>1000 nM
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] |
| MCF7 | IC50 |
0.045 μM
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] |
| MCF7 | IC50 |
9.58 μM
Compound: Crizotinib
|
Antiproliferative activity against human MCF7 cells after 72 hrs
Antiproliferative activity against human MCF7 cells after 72 hrs
|
[PMID: 23993328] |
| MDA-MB-231 | IC50 |
0.79 μM
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] |
| MDA-MB-231 | IC50 |
10.8 μM
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] |
| MIA PaCa-2 | IC50 |
7.16 μM
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] |
| MKN-45 | IC50 |
0.013 μM
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 μM
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] |
| MKN-45 | IC50 |
15 nM
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] |
| MKN-45 | IC50 |
38.1 nM
Compound: 1
|
Antiproliferative activity against human MKN45 cells after 72 hrs
Antiproliferative activity against human MKN45 cells after 72 hrs
|
[PMID: 26005523] |
| NCI-H1975 | IC50 |
>10 μM
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] |
| NCI-H1975 | IC50 |
7.551 μM
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-H1993 | IC50 |
0.061 μM
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-H2228 | GI50 |
0.073 μM
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] |
| NCI-H2228 | IC50 |
0.087 μM
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 μM
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] |
| NCI-H2228 | IC50 |
0.27 μM
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 μM
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] |
| NCI-H2228 | IC50 |
1.92 μM
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 |
118 nM
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] |
| NCI-H2228 | IC50 |
2.5 μM
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 |
2.62 μM
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] |
| NCI-H2228 | IC50 |
2.8 μM
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-H2228 | IC50 |
202 nM
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-H2228 | IC50 |
437.9 nM
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-H3122 | EC50 |
32 nM
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 μM
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 |
0.8 μM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 μM
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 nM
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 nM
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 μM
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 |
>1 μM
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 μM
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-H460 | IC50 |
2.244 μM
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-H661 | IC50 |
11.47 μM
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 |
0.364 μM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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 nM
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] |
| PC-3 | IC50 |
9.787 μM
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] |
| Sf9 | IC50 |
0.027 μM
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 μM
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 μM
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] |
| SGC-7901 | IC50 |
0.3213 μM
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 nM
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 μM
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 |
0.85 μM
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 μM
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 μM
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 nM
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 μM
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 nM
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 nM
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 μM
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 μM
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 nM
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 | IC50 |
136 nM
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 nM
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 nM
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] |
| U-937 | IC50 |
2286 nM
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 μM
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] |
Chemical Information
-
CAS No. 877399-53-6
-
Molecular Weight 510.39
-
Formula C23H26Cl2FN5O3
-
SMILES
NC1=NC=C(C=C1O[C@H](C)C2=C(C=CC(F)=C2Cl)Cl)C3=CN(N=C3)C4CCNCC4.CC(O)=O
-
Synonyms
PF-02341066 acetate
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (84)
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Journal Impact Factor
-
Most Recent
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Signal Transduct Target Ther
Tet methylcytosine dioxygenase 2 (TET2) deficiency elicits EGFR-TKI (tyrosine kinase inhibitors) resistance in non-small cell lung cancer. [Abstract]2024 Mar 9;9(1):65. PMID: 38461173 -
Cancer Discov
NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations. [Abstract]2024 Sep 13:OF1-OF20. PMID: 39269178 -
Cancer Discov
NVL-520 is a selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations. [Abstract]2023 Mar 1;13(3):598-615. PMID: 36511802 -
Cancer Discov
Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple-Negative Breast Cancer. [Abstract]2018 Mar;8(3):354-369. PMID: 29203461
Crizotinib acetate 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.
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Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Blood
Tyrosine phosphatases regulate resistance to ALK inhibitors in ALK+ anaplastic large cell lymphoma. [Abstract]2022 Feb 3;139(5):717-731. PMID: 34657149 -
Cancer Res
c-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers. [Abstract]2015 Nov 1;75(21):4548-59. PMID: 26483207 -
Nat Commun
Engineering bi-directional chemically-modulated synthetic condensates for cellular control. [Abstract]2025 Jul 17;16(1):6587. PMID: 40675979 -
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Sci Transl Med
Oncogenic switch and single-agent MET inhibitor sensitivity in a subset of EGFR-mutant lung cancer. [Abstract]2021 Sep;13(609):eabb3738. PMID: 34516823 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Leukemia
Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]2025 Aug 14. PMID: 40813622 -
J Exp Clin Cancer Res
MiR-181a-driven downregulation of cholesterol biosynthesis through SREBP2 inhibition suppresses uveal melanoma metastasis. [Abstract]2025 Jul 19;44(1):215. PMID: 40684202 -
J Exp Clin Cancer Res
The autocrine loop of ALK receptor and ALKAL2 ligand is an actionable target in consensus molecular subtype 1 colon cancer. [Abstract]2022 Mar 29;41(1):113. PMID: 35351152 -
Biomark Res
Simultaneous inhibition of FAK and ROS1 synergistically repressed triple-negative breast cancer by upregulating p53 signalling. [Abstract]2024 Jan 25;12(1):13. PMID: 38273343 -
EBioMedicine
Immunological profiles of human oligodendrogliomas define two distinct molecular subtypes. [Abstract]2023 Jan:87:104410. PMID: 36525723 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Cell Rep Med
STAT3 couples activated tyrosine kinase signaling to the oncogenic core transcriptional regulatory circuitry of anaplastic large cell lymphoma. [Abstract]2024 Mar 19;5(3):101472. PMID: 38508140 -
Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
Cancer Lett
Integrated clinical, genomic and functional characterization of a novel ALK variant in neuroblastoma. [Abstract]2026 May 29:656:218624. PMID: 42217560 -
Cancer Lett
CD74-ROS1 G2032R mutation transcriptionally up-regulates Twist1 in non-small cell lung cancer cells leading to increased migration, invasion, and resistance to crizotinib. [Abstract]2018 May 28:422:19-28. PMID: 29477381
Crizotinib acetate 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.
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J Pharm Anal
Synergistic effects of methyl 2-cyano-3,11-dioxo-18beta-olean-1,-12-dien-30-oate and erlotinib on erlotinib-resistant non-small cell lung cancer cells. [Abstract]2021 Dec;11(6):799-807. PMID: 35028186 -
Int J Biol Macromol
Regulation of shelterin proteins TERF2IP and TRF2 by the MLL2-H3K4me3-p65 axis drives hyperglycemia-dependent endothelial senescence. [Abstract]2025 Jun 4;318(Pt 1):144963. PMID: 40480577 -
J Transl Med
Epithelial cell adhesion molecule (EpCAM) regulates HGFR signaling to promote colon cancer progression and metastasis. [Abstract]2023 Aug 5;21(1):530. PMID: 37543570 -
Oncogene
Synergistic effects of combined BET and FAK inhibition against Vestibular Schwannomas in NF2-related Schwannomatosis. [Abstract]2024 Sep;43(40):2995-3002. PMID: 39209965 -
Oncogene
Activated ALK signals through the ERK-ETV5-RET pathway to drive neuroblastoma oncogenesis. [Abstract]2018 Mar;37(11):1417-1429. PMID: 29321660 -
Blood Adv
BH3 mimetic drugs overcome the microenvironment-induced resistance to crizotinib in ALK+ anaplastic large cell lymphoma. [Abstract]2025 Jul 2:bloodadvances.2024015322. PMID: 40601898 -
Blood Adv
Aberrant expression of GOLM1 protects ALK+ anaplastic large cell lymphoma from apoptosis by enhancing BCL-XL stability. [Abstract]2023 Aug 8;7(15):4049-4063. PMID: 36763539 -
Clin Transl Med
2025 May;15(5):e70338. PMID: 40437874 -
J Med Chem
Discovery of Oral Degraders of the ROS1 Fusion Protein with Potent Activity against Secondary Resistance Mutations. [Abstract]2024 Oct 24;67(20):18098-18123. PMID: 39361251 -
J Med Chem
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. [Abstract]2021 Oct 14;64(19):14344-14357. PMID: 34547896 -
J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967 -
Sci Signal
Pleiotrophin promotes vascular abnormalization in gliomas and correlates with poor survival in patients with astrocytomas. [Abstract]2015 Dec 8;8(406):ra125. PMID: 26645582 -
Sci Signal
The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. [Abstract]2014 Oct 28;7(349):ra102. PMID: 25351247
Crizotinib acetate 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.
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Talanta
Development and comparative evaluation of two immunoassay platforms for bioanalysis of crizotinib: A potent drug used for the treatment of non-small cell lung cancer. [Abstract]2019 Aug 15:201:217-225. PMID: 31122414 -
Eur J Med Chem
Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR associated drug resistant mutants in NSCLC. [Abstract]2017 Oct 20:139:674-697. PMID: 28850922 -
Mol Cancer Ther
2025 Jul 2;24(7):1005-1019. PMID: 40299789 -
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Stem Cell Reports
Inhibition of Farnesyltransferase Potentiates NOTCH-Targeted Therapy against Glioblastoma Stem Cells. [Abstract]2017 Dec 12;9(6):1948-1960. PMID: 29198824 -
Int J Mol Sci
Doxorubicin-Induced TrkAIII Activation: A Selection Mechanism for Resistant Dormant Neuroblastoma Cells. [Abstract]2022 Sep 17;23(18):10895. PMID: 36142807 -
Pharmaceuticals (Basel)
Synthesis and Development of 3-((2,4-Difluorophenyl)Amino)Propanoic Acid Derivatives as an Antiproliferative Medicinal Chemistry Scaffold Targeting Growth Factor Receptors. [Abstract]2026 Feb 27;19(3):381. PMID: 41901229 -
Spectrochim Acta A Mol Biomol Spectrosc
Innovative use of σ and π electron acceptors in the development of three high throughput 96-microwell spectrophotometric assays for crizotinib. [Abstract]2021 Oct 5:259:119884. PMID: 33971436 -
Spectrochim Acta A Mol Biomol Spectrosc
Charge-transfer reaction of 1,4-benzoquinone with crizotinib: spectrophotometric study, computational molecular modeling and use in development of microwell assay for crizotinib. [Abstract]2014 Oct 15;131:347-54. PMID: 24835938 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Mol Oncol
Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. [Abstract]2017 Aug;11(8):996-1006. PMID: 28432815
Crizotinib acetate 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.
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Cancers (Basel)
Novel Mechanisms of ALK Activation Revealed by Analysis of the Y1278S Neuroblastoma Mutation. [Abstract]2017 Oct 30;9(11). pii: E149. PMID: 29084134 -
Cancer Sci
APE1 Attenuates ALK Tyrosine Kinase Inhibitors Sensitivity in NPM1-ALK Positive Anaplastic Large Cell Lymphoma. [Abstract]2025 Jul 23. PMID: 40702700 -
ACS Omega
2023 Jun 14;8(25):22603-22612. PMID: 37387790 -
Transl Oncol
2022 Jan;15(1):101272. PMID: 34823094 -
Transl Oncol
Anti-epidermal growth factor vaccine antibodies increase the antitumor activity of kinase inhibitors in ALK and RET rearranged lung cancer cells. [Abstract]2021 Jan;14(1):100887. PMID: 33129112 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Biochim Biophys Acta Mol Cell Res
ZX-29, a novel ALK inhibitor, induces apoptosis via ER stress in ALK rearrangement NSCLC cells and overcomes cell resistance caused by an ALK mutation. [Abstract]2020 Jul;1867(7):118712. PMID: 32224191 -
Proteomes
Mass Spectrometry and Pharmacological Approaches to Measuring Cooption and Reciprocal Activation of Receptor Tyrosine Kinases. [Abstract]2023 Jun 2;11(2):20. PMID: 37368466 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Saudi Pharm J
Charge-transfer reaction of 2,3-dichloro-1,4-naphthoquinone with crizotinib: Spectrophotometric study, computational molecular modeling and use in development of microwell assay for crizotinib. [Abstract]2015 Jan;23(1):75-84. PMID: 25685046 -
Front Oncol
Low-Dose Crizotinib, a Tyrosine Kinase Inhibitor, Highly and Specifically Sensitizes P-Glycoprotein-Overexpressing Chemoresistant Cancer Cells Through Induction of Late Apoptosis in vivo and in vitro. [Abstract]2020 May 12;10:696. PMID: 32528877 -
Dis Model Mech
The ALK inhibitor PF-06463922 is effective as a single agent in neuroblastoma driven by expression of ALK and MYCN. [Abstract]2016 Sep 1;9(9):941-52. PMID: 27483357
Crizotinib acetate 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.
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Cancer Med
The underlying mechanisms of lorlatinib penetration across the blood-brain barrier and the distribution characteristics of lorlatinib in the brain. [Abstract]2020 Jun;9(12):4350-4359. PMID: 32347012 -
Arch Biochem Biophys
Collagen I protects human keratinocytes HaCaT against UVB injury via restoring PINK1/parkin-mediated mitophagy. [Abstract]2024 Mar:753:109905. PMID: 38281543 -
J Cancer Res Clin Oncol
MET canonical transcript expression is a predictive biomarker for chemo-sensitivity to MET-inhibitors in hepatocellular carcinoma cell lines. [Abstract]2021 Jan;147(1):167-175. PMID: 32980960 -
Invest New Drugs
Iruplinalkib (WX‑0593), a novel ALK/ROS1 inhibitor, overcomes crizotinib resistance in preclinical models for non-small cell lung cancer. [Abstract]2023 Apr;41(2):254-266. PMID: 37036582 -
PLoS One
Inhibition of the anti-apoptotic protein BCL2 in EML4-ALK cell models as a second proposed therapeutic target for non-small cell lung cancer. [Abstract]2025 Jan 21;20(1):e0308747. PMID: 39836700 -
PLoS One
A new method for the study of biophysical and morphological parameters in 3D cell cultures: Evaluation in LoVo spheroids treated with crizotinib. [Abstract]2021 Jun 8;16(6):e0252907. PMID: 34101765 -
PLoS One
Synthesis of hapten, generation of specific polyclonal antibody and development of ELISA with high sensitivity for therapeutic monitoring of crizotinib. [Abstract]2019 Feb 11;14(2):e0212048. PMID: 30742664 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
Biomed Chromatogr
Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method to quantify the small molecule inhibitors adagrasib, alectinib, brigatinib, capmatinib, crizotinib, lorlatinib, selpercatinib, and sotorasib in human plasma. [Abstract]2024 Oct;38(10):e5986. PMID: 39136165 -
Biomed Chromatogr
Pharmacokinetics of cligosiban in dog plasma after oral administration by liquid chromatography electrospray ionization tandem mass spectrometry. [Abstract]2019 Oct;33(10):e4611. PMID: 31145820 -
Biol Methods Protoc
Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]2025 Feb 13;10(1):bpaf012. PMID: 40060949 -
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bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
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Evid Based Complement Alternat Med
In a Rat Model of Acute Liver Failure, Icaritin Improved the Therapeutic Effect of Mesenchymal Stem Cells by Activation of the Hepatocyte Growth Factor/c-Met Pathway. [Abstract]2019 Nov 7;2019:4253846. PMID: 31915446
Crizotinib acetate 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.
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Oncotarget
ALK mutation dynamics and clonal evolution in a neuroblastoma model exhibiting two ALK mutations. [Abstract]2019 Aug 13;10(48):4937-4950. PMID: 31452835 -
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Oncotarget
Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. [Abstract]2016 May 17;7(20):29011-22. PMID: 27049722
Crizotinib acetate 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.
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Oncotarget
Activated Alk triggers prolonged neurogenesis and Ret upregulation providing a therapeutic target in ALK-mutated neuroblastoma. [Abstract]2014 May 15;5(9):2688-702. PMID: 24811913
Crizotinib acetate 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.
Purity & Documentation
References
[1]. Zou HY, et al. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 2007, 67(9), 4408-4417. [Content Brief]
[2]. Christensen JG, et al. Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma. Mol Cancer Ther. 2007, 6(12 Pt 1), 3314-3322. [Content Brief]
[3]. Cui JJ, et al. Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J Med Chem. 2011 Sep 22;54(18):6342-63. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)