Crizotinib acetate (Synonyms: PF-02341066 acetate)

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

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Crizotinib acetate Chemical Structure

CAS No. : 877399-53-6

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Other In-stock Forms of Crizotinib acetate:

Crizotinib Crizotinib hydrochloride

Other Forms of Crizotinib acetate:

66 Publications Citing Use of MCE Crizotinib acetate

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Evid Based Complement Alternat Med. 2019 Nov 7;2019:4253846. [Abstract]; Western blot analysis of cleaved caspase 3, Bax, and Bcl-2 expression after serum-free culture for 72 h with or without Crizotinib.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109. [Abstract]; Resistant cells are treated with 200 nM Afatinib alone or in combination with 1 μM Crizotinib for 48 h.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]; At 50mg/kg, Crizotinib inhibits MET phosphorylation and downstream signaling pathway activation.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 May 28;422:19-28. [Abstract]; CD74-ROS1 or CD74-ROS1 G2032R mutation cells are treated with Crizotinib for 24 h, the expression of ROS1 or p-ROS1 is determined by western blot.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):996-1006. [Abstract]; Dose-response and time course comparison of ALK inhibition by Crizotinib or Ceritinib.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Dis Model Mech. 2016 Sep 1;9(9):941-52. [Abstract]; CLB-BAR, CLB-GE neuroblastoma cells are treated for 6 h with either Crizotinib or PF-04643922. Cells are harvested and pre-cleared cell lysates are analyzed on SDS PAGE followed by western blotting for ALK, phospho-ALK-Y1278, phospho-ERK5, pan-ERK5 phospho-ERK1/2 and pan-ERK. Actin is employed as a loading control. Protein band intensities are quantified by Image Studio Lite 3.1 and normalized to untreated samples.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 17;7(20):29011-22. [Abstract]; A, B. CLB-BAR (ALK-Δ4-11) and CLB-GE (ALK-F1174V), both ALK addicted cell lines, are treated with increasing doses of Brigatinib for 6 hours. Crizotinib (250 nM) is employed as a positive control. Cells lysates are resolved on SDS/PAGE followed by immunoblotting for pALK (Y1604) and additional downstream targets as indicated.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Sci Signal. 2014 Oct 28;7(349):ra102. [Abstract]; Activation of ERK5 in neuroblastoma cell lines expressing activated ALK. (A to C) Immunoblotting for the indicated proteins in neuroblastoma cells CLB-BAR (A), CLB-GE (B), and IMR32 (C) cultured on six-well plates in complete growth medium and treated with inhibitors as indicated for 6 hours alone (A and B) or before (C) stimulation with mAb46 for 30 min.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2014 May 15;5(9):2688-702. [Abstract]; The Ret expression level is investigated by Western blot in MYCN/KI 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.

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Biological Activity
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Description

Cellular Effect

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

Molecular Weight

510.39

Formula

C₂₃H₂₆Cl₂FN₅O₃

CAS No.

877399-53-6

SMILES

NC1=NC=C(C=C1O[C@H](C)C2=C(C=CC(F)=C2Cl)Cl)C3=CN(N=C3)C4CCNCC4.CC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zou HY, et al. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 2007, 67(9), 4408-4417. [Content Brief]

[2]. Christensen JG, et al. Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma. Mol Cancer Ther. 2007, 6(12 Pt 1), 3314-3322. [Content Brief]

[3]. Cui JJ, et al. Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J Med Chem. 2011 Sep 22;54(18):6342-63. [Content Brief]

Crizotinib acetate Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Crizotinib877399-53-6PF-02341066PF02341066PF 02341066c-Met/HGFRROS KinaseAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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Crizotinib acetate (Synonyms: PF-02341066 acetate)

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Crizotinib acetate Related Antibodies

66 Publications Citing Use of MCE Crizotinib acetate

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