Cat. No.: HY-50878

Crizotinib

(Synonyms: PF-02341066)

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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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Pureté: 99.74%
CAS No.: 877399-52-5
Formule: C₂₁H₂₂Cl₂FN₅O
Masse moléculaire:450.34

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Crizotinib Chemical Structure

CAS No.: 877399-52-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
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- IC₅₀ & Target
- Cellular Effect
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- In Vivo
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Publications (89)
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Activité biologique

Description

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
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	>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	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	>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	>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	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	>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	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	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	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]
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]
ASPC1	GI₅₀	2.38 μM 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	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	0.28 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	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	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	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	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	0.26 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	0.98 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	>2000 nM 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]
BaF3	IC₅₀	18 nM 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	259 nM 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]
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	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	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	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	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]
BaF3	IC₅₀	1237 nM 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	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	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	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	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	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	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	>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	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	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	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	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	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	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]
CAPAN-1	GI₅₀	5.12 μM 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]
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]
DEL	GI₅₀	309 nM 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]
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	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	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]
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	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	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	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	0.013 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	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	Antiproliferative activity against human EBC-1 cells Antiproliferative activity against human EBC-1 cells	[PMID: 38733884]
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]
GL261	IC₅₀	3.43 μM 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]
HCC78	IC₅₀	21 nM 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 nM 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]
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	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	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]
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	0.23 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	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	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]
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	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]
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]
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	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]
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]
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]
HT-29	GI₅₀	4 μM 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]
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]
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	2.38 μM 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]
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	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]
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	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	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	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	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	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	GI₅₀	119 nM 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]
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	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	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	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	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	0.03 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	0.087 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	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	200 nM Compound: Crizotinib	Antiproliferative activity against human KARPAS-299 cells Antiproliferative activity against human KARPAS-299 cells	[PMID: 38733884]
Kelly	IC₅₀	0.42 μM Compound: 2, PF-2341066	Cytotoxicity against human Kelly cells expressing ALK F1174L mutant Cytotoxicity against human Kelly cells expressing ALK F1174L mutant	[PMID: 21572589]
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]
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]
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]
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]
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]
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	8.37 μM 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]
MDA-MB-468	IC₅₀	4.54 μM 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]
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]
MIA PaCa-2	GI₅₀	1.457 μM 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]
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	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]
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	9.1 nM 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]
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]
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-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-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-H1993	IC₅₀	3 μM 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]
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	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	GI₅₀	121 nM 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]
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	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	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	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	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	0.27 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	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	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	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	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-H23	GI₅₀	1773 nM 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	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	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-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	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	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	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	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	GI₅₀	62 nM 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	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	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	0.092 μM 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	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	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-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	>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	>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	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]
NCI-H838	GI₅₀	1307 nM 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	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	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	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	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, 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, 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	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, 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	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	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	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]
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	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	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	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	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	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	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	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	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	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	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	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]
PANC-03-27	GI₅₀	6.348 μM 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 μM 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 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]
RD	CC₅₀	>10 μM Compound: 21	Cytotoxicity against human RD cells Cytotoxicity against human RD cells	[PMID: 33539089]
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	IC₅₀	0.53 μM 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	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	0.85 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	0.32 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	0.92 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	0.01 μM 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 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	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]
SU-DHL-1	GI₅₀	99 nM 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	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]
SW480	GI₅₀	>10 μM 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]
U-87MG ATCC	IC₅₀	7.29 μM 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	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]
U-937	GI₅₀	928 nM 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]
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]

In Vitro

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.

In Vivo

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 877399-52-5
Appearance Solid
Masse moléculaire 450.34
Formule C₂₁H₂₂Cl₂FN₅O
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
Synonyms

PF-02341066
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (89)

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Journal Impact Factor

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 Cell

JYP0322, a highly selective and brain-penetrant ROS1 inhibitor, overcomes ROS1G2032R resistance mutation in NSCLC: The first-in-human phase 1 trial. [Abstract]

2026 May 11;44(5):983-994.e5. PMID: 42030931
J Hematol Oncol

Mouse avatar models of esophageal squamous cell carcinoma proved the potential for EGFR-TKI afatinib and uncovered Src family kinases involved in acquired resistance. [Abstract]

2018 Aug 29;11(1):109. PMID: 30157900

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.
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 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.
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
Acta Pharm Sin B

2026 Mar 2.
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
MedComm (2020)

Crizotinib: A Novel Strategy to Reverse Immunosuppression in Melanoma by Targeting Lactate Transport. [Abstract]

2025 Jul 21;6(8):e70286. PMID: 40692663
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 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.
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

Responsiveness of different MET tumour alterations to type I and type II MET inhibitors. [Abstract]

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 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.
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
Anal Chim Acta

2026 May 12;1412:345649.
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

Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations. [Abstract]

2025 Jul 2;24(7):1005-1019. PMID: 40299789
J Pharm Investig

2025 Dec 29.
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
Int J Antimicrob Agents

A new perspective on the antimicrobial mechanism of linezolid against Staphylococcus aureus revealed by proteomics and metabolomics analysis. [Abstract]

2025 Jun;65(6):107470. PMID: 40049374
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 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.
Cancers (Basel)

2024
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

Discovery of PLpro and Mpro Inhibitors for SARS-CoV-2. [Abstract]

2023 Jun 14;8(25):22603-22612. PMID: 37387790
Transl Oncol

BX-795 inhibits neuroblastoma growth and enhances sensitivity towards chemotherapy. [Abstract]

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 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.
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

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

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
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

PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]

2024 Nov 6:2024.11.04.621884. PMID: 39574568
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

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 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.
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
Technical University of Munich

24.01.2018.
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 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.
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 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 Alk^R1279Q and MYCN/KI Alk^F1178L treated tumors and controls using the anti-Ret antibody EPR2871. Actin is used as a standard for quantification.

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Working 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

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Kinase Assay^[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) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[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) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[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) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
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- Italian - IT (623 KB)
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- Portuguese - PT (623 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

[4]. Cullinane C, et al. Differential (18)F-FDG and 3'-deoxy-3'-(18)F-fluorothymidine PET responses to pharmacologic inhibition of the c-MET receptor in preclinical tumor models. J Nucl Med. 2011 Aug;52(8):1261-7 [Content Brief]

[5]. Shen A, et al. c-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers. Cancer Res. 2015 Nov 1;75(21):4548-59. [Content Brief]

[6]. Umapathy G, et al. The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. Sci Signal. 2014 Oct 28;7(349):ra102. [Content Brief]

[7]. Tucker ER, et al. Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. Mol Oncol. 2017 Aug;11(8):996-1006. [Content Brief]

[8]. Liu H, et al. Identifying and Targeting Sporadic Oncogenic GeneticLiu H, et al. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple Negative Breast Cancer. Cancer Discov. 2018 Mar;8(3):354-369. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Crizotinib

89 Cited Publications

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Crizotinib

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Publications Citing Use of MedChemExpress (MCE) Crizotinib

Activité biologique

Chemical Information

Publications (89)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Crizotinib Related Classifications

HY-50878 Related Classifications