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PF-02341066 (Crizotinib) ALK/c-Met/ROS1 억제제

Name: PF-02341066 (Crizotinib)
Brand: Selleck Chemicals
SKU: S1068
Rating: 5 (466 reviews)

제품 번호S1068

Crizotinib은 세포 기반 분석에서 각각 11 nM 및 24 nM의 IC50을 갖는 c-Met 및 ALK의 강력한 억제제입니다. 또한 Ki 값 0.025 nM 미만인 강력한 ROS1 억제제입니다. Crizotinib은 여러 폐암 세포주에서 STAT3 경로 억제를 통해 자가포식을 유도합니다.

PF-02341066 (Crizotinib) c-Met 억제제 Chemical Structure

화학 구조

분자량: 450.34

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품질 관리

배치: 순도: 99.92%

99.92

관련 타겟	EGFR VEGFR PDGFR FGFR Src MEK CSF-1R FLT3 HER2 c-Kit
기타 c-Met 억제제	Tepotinib Dihexa SGX-523 PHA-665752 Foretinib SU11274 BMS-777607 JNJ-38877605 Tivantinib PF-04217903

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
SU-DHL1	Cytotoxic Assay				Cytotoxicity against human SU-DHL1 cells expressing ALK coexpressing NPM with IC50 of 0.01 μM	21572589
BAF3	Cytotoxic Assay		48 h	DMSO	Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 with IC50 of 0.62 μM	21572589
BAF3	Cytotoxic Assay		48 h	DMSO	Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 with IC50 of 2.2 μM	21572589
BAF3	Cytotoxic Assay		48 h	DMSO	Cytotoxicity against mouse BAF3 cells expressing EML4-ALK with IC50 of 0.28 μM	21572589
Kelly	Cytotoxic Assay			DMSO	Cytotoxicity against human Kelly cells expressing ALK F1174L mutant with IC50 of 0.42 μM	21572589
SH-SY5Y	Cytotoxic Assay			DMSO	Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant with IC50 of 0.53 μM	21572589
SMS-KCN	Cytotoxic Assay			DMSO	Cytotoxicity against human SMS-KCN cells expressing ALK R1275Q mutant with IC50 of 0.91 μM	21572589
BAF3	Cytotoxic Assay		48 h	DMSO	Cytotoxicity against mouse BAF3 cells expressing Tel-ALK with IC50 of 0.19 μM	21572589
3T3	Function Assay		1 h	DMSO	Inhibition of RON assessed as growth factor-induced autophosphorylation with IC50 of 0.08 μM	21812414
3T3-E	Function Assay		1 h	DMSO	Inhibition of TIE2 assessed growth factor-induced autophosphorylation with IC50 of 0.448 μM	21812414
A549	Kinase Assay		1 h	DMSO	Inhibition of human recombinant c-MET kinase expressed assessed as inhibition of HGF-induced autophosphorylation with IC50 of 0.008 μM	21812414
BAF3-BCL	Function Assay		1 h	DMSO	Inhibition of ABL assessed as growth factor-induced autophosphorylation with IC50 of 1.159 μM	21812414
HEK293	Function Assay		1 h	DMSO	Inhibition of AXL assessed as growth factor-induced autophosphorylation with IC50 of 0.294 μM	21812414
HEK293	Function Assay		1 h	DMSO	Inhibition of IR assessed as growth factor-induced autophosphorylation with IC50 of 2.887 μM	21812414
Jurkat	Function Assay		1 h	DMSO	Inhibition of LCK assessed as growth factor-induced autophosphorylation with IC50 of 2.741 μM	21812414
KARPAS299	Kinase Assay		1 h	DMSO	Inhibition of ALK assessed as growth factor-induced autophosphorylation with IC50 of 0.02 μM	21812414
PAE	Function Assay		1 h	DMSO	Inhibition of TRKB assessed as growth factor-induced autophosphorylation with IC50 of 0.399 μM	21812414
PAE	Function Assay		1 h	DMSO	Inhibition of TRKA assessed as growth factor-induced autophosphorylation with IC50 of 0.58 μM	21812414
BAF3	Function Assay		2-3 d	DMSO	Inhibition of TEL-fused insulin receptor expressed with IC50 of 1.643 μM	23742252
BAF3	Function Assay		2-3 d	DMSO	Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay with IC50 of 0.1508 μM	23742252
BAF3	Function Assay		2-3 d	DMSO	Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay with IC50 of 3.479 μM	23742252
KARPAS299	Cytotoxic Assay		2-3 d	DMSO	IC50=0.0642 μM	23742252
EBC1	Growth Inhibition Assay		72 h	DMSO	IC50=0.023 μM	23993328
HCT116	Growth Inhibition Assay		72 h	DMSO	IC50=14.82 μM	23993328
MCF7	Growth Inhibition Assay		72 h	DMSO	IC50=9.58 μM	23993328
MDA-MB-231	Growth Inhibition Assay		72 h	DMSO	IC50=10.8 μM	23993328
MKN45	Growth Inhibition Assay		72 h	DMSO	IC50=0.013 μM	23993328
NCI-H441	Growth Inhibition Assay		72 h	DMSO	IC50=17.25 μM	23993328
NCI-H661	Growth Inhibition Assay		72 h	DMSO	IC50=11.47 μM	23993328
SK-MEL-28	Growth Inhibition Assay		72 h	DMSO	IC50=10.97 μM	23993328
SKOV3	Growth Inhibition Assay		72 h	DMSO	IC50=12.85 μM	23993328
SNU5	Growth Inhibition Assay		72 h	DMSO	IC50=0.016 μM	23993328
Antiproliferative assay	EBC1		72 hrs		Antiproliferative activity against human EBC1 cells expressing elevated levels of constitutively active c-Met after 72 hrs by SRB assay, IC50 = 0.053 μM.	22863529
Function assay	KARPAS299		72 hrs		Inhibition of ALK-fusion driven cell proliferation in human KARPAS299 cells after 72 hrs by CellTiter Glo assay, IC50 = 0.062 μM.	24432909
Function assay	NIH-3T3		1 hr		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, IC50 = 0.08 μM.	24432909
Function assay	NCI-H3122		72 hrs		Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells after 72 hrs by CellTiter Glo assay, IC50 = 0.108 μM.	24432909
Function assay	NCI-H2228		72 hrs		Inhibition of ALK-fusion driven cell proliferation in human NCI-H2228 cells after 72 hrs by CellTiter Glo assay, IC50 = 0.118 μM.	24432909
Function assay	NIH-3T3		1 hr		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, IC50 = 0.165 μM.	24432909
Function assay	NIH-3T3		1 hr		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, IC50 = 0.478 μM.	24432909
Function assay	NIH-3T3		1 hr		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, IC50 = 0.605 μM.	24432909
Function assay	NCI-H3122		72 hrs		Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK G1269A mutant after 72 hrs by CellTiter Glo assay, IC50 = 0.623 μM.	24432909
Function assay	NIH-3T3		1 hr		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, IC50 = 0.626 μM.	24432909
Function assay	NCI-H3122		72 hrs		Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK L1196M mutant after 72 hrs by CellTiter Glo assay, IC50 = 0.838 μM.	24432909
Function assay	NIH-3T3		1 hr		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, IC50 = 0.843 μM.	24432909
Function assay	NIH-3T3		1 hr		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, IC50 = 1.026 μM.	24432909
Function assay	NIH-3T3		1 hr		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, IC50 = 3.039 μM.	24432909
Function assay	BAF3		72 hrs		Inhibition of NPM/ALK (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay, IC50 = 0.051 μM.	24468632
Function assay	BAF3		72 hrs		Inhibition of NPM/ALK (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay, IC50 = 0.051 μM.	24468632
Function assay	BAF3		72 hrs		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, IC50 = 0.26 μM.	24468632
Cytotoxicity assay	BAF3		72 hrs		Cytotoxicity against mouse BAF3 cells assessed as growth inhibition after 72 hrs by [3H]-thymidine incorporation assay, IC50 = 0.98 μM.	24468632
Antiproliferative assay	NIH/3T3		72 hrs		Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1 after 72 hrs by MTT assay, IC50 = 0.0954 μM.	24785465
Antiproliferative assay	SUP-M2		72 hrs		Antiproliferative activity against human SUP-M2 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.174 μM.	24785465
Antiproliferative assay	NIH/3T3		72 hrs		Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1/L1196M mutant after 72 hrs by MTT assay, IC50 = 0.606 μM.	24785465
Function assay	NIH-3T3		1 hr		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, IC50 = 0.08 μM.	24819116
Function assay	NIH-3T3		1 hr		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, IC50 = 0.165 μM.	24819116
Function assay	NIH-3T3		1 hr		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, IC50 = 0.478 μM.	24819116
Function assay	NIH-3T3		1 hr		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, IC50 = 0.605 μM.	24819116
Function assay	NIH-3T3		1 hr		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, IC50 = 0.626 μM.	24819116
Function assay	NIH-3T3		1 hr		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, IC50 = 0.843 μM.	24819116
Function assay	NIH-3T3		1 hr		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, IC50 = 1.026 μM.	24819116
Function assay	NIH-3T3		1 hr		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, IC50 = 1.148 μM.	24819116
Function assay	NIH-3T3		1 hr		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, IC50 = 3.039 μM.	24819116
Function assay	MKN845		1 hr		Inhibition of c-Met phosphorylation in human MKN845 cells after 1 hr by western blotting, IC50 = 0.02 μM.	24900750
Function assay	MKN845		90 mins		Inhibition of c-Met phosphorylation in human MKN845 cells after 90 mins by Sandwich-ELISA, IC50 = 0.02 μM.	24900750
Function assay	karpas 299		90 mins		Inhibition of NPM-fused ALK phosphorylation (unknown origin) expressed in human karpas 299 cells after 90 mins by Sandwich-ELISA, IC50 = 0.11 μM.	24900750
Cytotoxicity assay	NCI-H1993		48 hrs		Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay, IC50 = 0.061 μM.	24900830
Cytotoxicity assay	NIH/3T3		48 hrs		Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay, IC50 = 0.364 μM.	24900830
Cytotoxicity assay	A549		48 hrs		Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 4.084 μM.	24900830
Cytotoxicity assay	NCI-H1975		48 hrs		Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay, IC50 = 7.551 μM.	24900830
Antiproliferative assay	EBC1		72 hrs		Antiproliferative activity against cMET-amplified human EBC1 cells after 72 hrs, IC50 = 0.0069 μM.	24900831
Antiproliferative assay	KARPAS299		72 hrs		Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs, IC50 = 0.2 μM.	24900831
Antitumor assay	BAF3	50 mg/kg	2 weeks		Antitumor activity against mouse BAF3 cells expressing EML4-ALK fusion protein allografted in nude mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 2 weeks relative to vehicle-treated control	24900831
Antiproliferative assay	EBC1		72 hrs		Antiproliferative activity against human EBC1 cells after 72 hrs, IC50 = 0.021 μM.	25537530
Antiproliferative assay	SNU5		72 hrs		Antiproliferative activity against human SNU5 cells after 72 hrs, IC50 = 0.0204 μM.	26005523
Antiproliferative assay	EBC1		72 hrs		Antiproliferative activity against human EBC1 cells after 72 hrs, IC50 = 0.0218 μM.	26005523
Antiproliferative assay	MKN45		72 hrs		Antiproliferative activity against human MKN45 cells after 72 hrs, IC50 = 0.0381 μM.	26005523
Antiproliferative assay	BAF3/TPR-Met		72 hrs		Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs, IC50 = 0.1274 μM.	26005523
Antiproliferative assay	NCI-H3122		72 hrs		Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs, IC50 = 0.2612 μM.	26476749
Antiproliferative assay	NCI-H3122		72 hrs		Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.032 μM.	26568289
Function assay	Ba/F3		72 hrs		Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.056 μM.	26568289
Function assay	Ba/F3		72 hrs		Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.056 μM.	26568289
Function assay	Ba/F3		72 hrs		Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.065 μM.	26568289
Function assay	Ba/F3		72 hrs		Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.081 μM.	26568289
Function assay	Ba/F3		72 hrs		Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.144 μM.	26568289
Antiproliferative assay	SMS-KCNR		72 hrs		Antiproliferative activity against human SMS-KCNR cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.179 μM.	26568289
Antiproliferative assay	Kelly		72 hrs		Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.211 μM.	26568289
Antiproliferative assay	LAN5		72 hrs		Antiproliferative activity against human LAN5 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.232 μM.	26568289
Antiproliferative assay	DFCI76		72 hrs		Antiproliferative activity against human DFCI76 cells expressing EML4-ALK L1152R mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.233 μM.	26568289
Function assay	Ba/F3		72 hrs		Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.328 μM.	26568289
Antiproliferative assay	SK-N-SH		72 hrs		Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.37 μM.	26568289
Antiproliferative assay	CHLA20		72 hrs		Antiproliferative activity against human CHLA20 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.439 μM.	26568289
Function assay	Ba/F3		72 hrs		Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.512 μM.	26568289
Antiproliferative assay	SH-SY5Y		72 hrs		Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.523 μM.	26568289
Function assay	Ba/F3		72 hrs		Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.549 μM.	26568289
Function assay	Ba/F3		72 hrs		Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.645 μM.	26568289
Antiproliferative assay	SK-N-BE(2)		72 hrs		Antiproliferative activity against human SK-N-BE(2) cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.71 μM.	26568289
Function assay	Ba/F3		72 hrs		Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.857 μM.	26568289
Cytotoxicity assay	BA/F3		72 hrs		Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.927 μM.	26568289
Antiproliferative assay	LAN1		72 hrs		Antiproliferative activity against human LAN1 cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.346 μM.	26568289
Antiproliferative assay	SK-N-FI		72 hrs		Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.469 μM.	26568289
Antiproliferative assay	SK-N-AS		72 hrs		Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.473 μM.	26568289
Antiproliferative assay	DFCI114		72 hrs		Antiproliferative activity against human DFCI114 cells expressing EML4-ALK G1269A mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.615 μM.	26568289
Antiproliferative assay	EBC1		72 hrs		Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay, IC50 = 0.019 μM.	26698536
Cytotoxicity assay	EBC1		72 hrs		Cytotoxicity against human EBC1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50 = 0.044 μM.	27017548
Antiproliferative assay	KARPAS299		72 hrs		Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.103 μM.	27131066
Antiproliferative assay	SUP-M2		72 hrs		Antiproliferative activity against human SUP-M2 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.112 μM.	27131066
Antiproliferative assay	SU-DHL1		72 hrs		Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.136 μM.	27131066
Antiproliferative assay	NCI-H3122		72 hrs		Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.21 μM.	27131066
Function assay	NCI-H3122		72 hrs		Inhibition of ALK expressed in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB/CCK-8 assay, IC50 = 0.261 μM.	27131066
Antiproliferative assay	NIH/3T3		72 hrs		Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay, IC50 = 0.283 μM.	27131066
Antiproliferative assay	NIH/3T3		72 hrs		Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay, IC50 = 1.16 μM.	27131066
Antiproliferative assay	ALK-positive KARPAS299		72 hrs		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, IC50 = 0.365 μM.	27144831
Antiproliferative assay	ALK-negative U937		72 hrs		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, IC50 = 2.286 μM.	27144831
Cytotoxicity assay	HepG2		72 hrs		Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 3.7 μM.	27396929
Cytotoxicity assay	MIAPaCa2		72 hrs		Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 7.16 μM.	27396929
Cytotoxicity assay	HCC827		72 hrs		Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 7.25 μM.	27396929
Cytotoxicity assay	KARPAS299		72 hrs		Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay, IC50 = 0.068 μM.	27474925
Cytotoxicity assay	HCC78		72 hrs		Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay, IC50 = 0.34 μM.	27474925
Antiproliferative assay	SU-DHL1		72 hrs		Antiproliferative activity against ALK constitutively activated human SU-DHL1 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.0923 μM.	27769623
Antiproliferative assay	NCI-H3122		72 hrs		Antiproliferative activity against ALK constitutively activated human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.1009 μM.	27769623
Antiproliferative assay	KARPAS299		72 hrs		Antiproliferative activity against ALK constitutively activated human KARPAS299 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.1049 μM.	27769623
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.08 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.08 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK F1174L mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.165 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK F1174L mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.165 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK C1156Y mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.478 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK C1156Y mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.478 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK G1269A mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.605 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK G1269A mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.605 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK S1206Y mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.626 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK S1206Y mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.626 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK L1196M mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.843 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK L1196M mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.843 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK L1152R mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 1.026 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK L1152R mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 1.026 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK G1202R mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 1.148 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK G1202R mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 1.148 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK 1151Tins mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 3.039 μM.	28431340
Function assay	NIH/3T3				Inhibition of wild type EML4/ALK 1151Tins mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 3.039 μM.	28431340
Cytotoxicity assay	EBC1		72 hrs		Cytotoxicity against human EBC1 cells assessed as decrease in cell viability after 72 hrs by Cell Titer-Glo assay, Activity = 0.013 μM.	28755635
Cytotoxicity assay	MKN45		72 hrs		Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 72 hrs by Cell Titer-Glo assay, Activity = 0.022 μM.	28755635
Cytotoxicity assay	PC3		72 hrs		Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 72 hrs by Cell Titer-Glo assay, Activity = 2.244 μM.	28755635
Function assay	BAF3		72 hrs		Inhibition of EML4-fused ALK (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28850922
Function assay	BAF3		72 hrs		Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28850922
Function assay	BAF3		72 hrs		Inhibition of TEL-fused ALK (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28850922
Antiproliferative assay	NCI-H3122		72 hrs		Antiproliferative activity against human NCI-H3122 cells harboring EML4-fused ALK varian1 after 72 hrs by CellTiter-Glo assay, GI50 = 0.037 μM.	28850922
Antiproliferative assay	NCI-H2228		72 hrs		Antiproliferative activity against human NCI-H2228 cells harboring EML4-fused ALK varian3 after 72 hrs by CellTiter-Glo assay, GI50 = 0.073 μM.	28850922
Function assay	BAF3		72 hrs		Inhibition of TEL-fused ALK C1156Y mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.15 μM.	28850922
Function assay	BAF3		72 hrs		Inhibition of full length ALK F1174L mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.32 μM.	28850922
Function assay	BAF3		72 hrs		Inhibition of TEL-fused ALK G1202R mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.43 μM.	28850922
Antiproliferative assay	CHL		72 hrs		Antiproliferative activity against CHL cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.45 μM.	28850922
Function assay	BAF3		72 hrs		Inhibition of TEL-fused ALK L1196M mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay, GI50 = 0.59 μM.	28850922
Antiproliferative assay	BAF3		72 hrs		Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 1.1 μM.	28850922
Antiproliferative assay	CHO		72 hrs		Antiproliferative activity against CHO cells after 72 hrs by CellTiter-Glo assay, GI50 = 3.2 μM.	28850922
Antiproliferative assay	NCI-H2228		72 hrs		Antiproliferative activity against human NCI-H2228 cells after 72 hrs by MTT assay, IC50 = 2.5 μM.	29091425
Antiproliferative assay	H2228/CR		72 hrs		Antiproliferative activity against human H2228/CR cells after 72 hrs by MTT assay, IC50 = 10 μM.	29091425
Function assay	H2228	0.5 uM	3 hrs		Inhibition of ALK in human H2228 cells assessed as decrease in AKT phosphorylation at 0.5 uM after 3 hrs by Western blot method	29091425
Function assay	Ba/F3	0.1 to 1 uM	72 hrs		Inhibition of human wild type EML4 fused ALK expressed in mouse Ba/F3 cells assessed as decrease in cell proliferation at 0.1 to 1 uM preincubated for 72 hrs followed by methyl-3H-thymidine incorporation measured after 8 hrs by filter scintillation counte	29091425
Antiproliferative assay	KARPAS299		72 hrs		Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.087 μM.	29174809
Antiproliferative assay	HCC78		72 hrs		Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay, IC50 = 0.17 μM.	29174809
Antiproliferative assay	NCI-H2228		72 hrs		Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay, IC50 = 0.24 μM.	29174809
Antiproliferative assay	NCI-H3122		48 hrs		Antiproliferative activity against human NCI-H3122 cells after 48 hrs by MTT assay, IC50 = 0.8 μM.	29174814
Antiproliferative assay	HCC78		48 hrs		Antiproliferative activity against human HCC78 cells after 48 hrs by MTT assay, IC50 = 2 μM.	29174814
Antiproliferative assay	EBC1		72 hrs		Antiproliferative activity against human EBC1 cells after 72 hrs by Alamarblue assay, IC50 = 0.013 μM.	29202410
Antiproliferative assay	MKN45		72 hrs		Antiproliferative activity against human MKN45 cells after 72 hrs by Alamarblue assay, IC50 = 0.022 μM.	29202410
Antiproliferative assay	MCF7		72 hrs		Antiproliferative activity against human MCF7 cells after 72 hrs by Alamarblue assay relative to control, IC50 = 0.045 μM.	29202410
Antiproliferative assay	A549		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by Alamarblue assay relative to control, IC50 = 0.1343 μM.	29202410
Antiproliferative assay	HCT116		72 hrs		Antiproliferative activity against human HCT116 cells after 72 hrs by Alamarblue assay relative to control, IC50 = 0.2536 μM.	29202410
Antiproliferative assay	SGC7901		72 hrs		Antiproliferative activity against human SGC7901 cells after 72 hrs by Alamarblue assay relative to control, IC50 = 0.3213 μM.	29202410
Antiproliferative assay	NCI-H460		72 hrs		Antiproliferative activity against human NCI-H460 cells after 72 hrs by Alamarblue assay, IC50 = 2.244 μM.	29202410
Antiproliferative assay	COLO205		72 hrs		Antiproliferative activity against human COLO205 cells after 72 hrs by Alamarblue assay, IC50 = 2.449 μM.	29202410
Antiproliferative assay	PC3		72 hrs		Antiproliferative activity against human PC3 cells after 72 hrs by Alamarblue assay, IC50 = 9.787 μM.	29202410
Antiproliferative assay	BAF3		72 hrs		Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay, IC50 = 0.0486 μM.	29288940
Antiproliferative assay	BAF3		72 hrs		Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.0575 μM.	29288940
Antiproliferative assay	SU-DHL1		72 hrs		Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.155 μM.	29288940
Antiproliferative assay	KARPAS299		72 hrs		Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.176 μM.	29288940
Antiproliferative assay	NCI-H3122		72 hrs		Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.303 μM.	29288940
Antiproliferative assay	BAF3		72 hrs		Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.34 μM.	29288940
Antiproliferative assay	BAF3		72 hrs		Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.564 μM.	29288940
Antiproliferative assay	BAF3		72 hrs		Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.594 μM.	29288940
Antiproliferative assay	BAF3		72 hrs		Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.644 μM.	29288940
Antiproliferative assay	HCC78		72 hrs		Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay, IC50 = 0.889 μM.	29288940
qHTS assay	TC32				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
qHTS assay	A673				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
qHTS assay	Saos-2				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
qHTS assay	RD				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
qHTS assay	SK-N-SH				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
qHTS assay	BT-12				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
qHTS assay	MG 63 (6-TG R)				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
qHTS assay	NB1643				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
qHTS assay	OHS-50				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
qHTS assay	LAN-5				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
qHTS assay	NB-EBc1				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
qHTS assay	SK-N-SH				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
qHTS assay	Rh41				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
qHTS assay	A673				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
qHTS assay	Rh30				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
qHTS assay	BT-37				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
qHTS assay	MG 63 (6-TG R)				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
qHTS assay	Rh30				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
qHTS assay	OHS-50				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
qHTS assay	SJ-GBM2				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
qHTS assay	SK-N-MC				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
qHTS assay	NB-EBc1				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
qHTS assay	LAN-5				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
qHTS assay	Rh18				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
qHTS assay	NB1643				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
qHTS assay	SK-N-MC				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
qHTS assay	TC32				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
qHTS assay	Rh18				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
qHTS assay	Saos-2				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
Antiproliferative assay	EBC1		72 hrs		Antiproliferative activity against human EBC1 cells after 72 hrs by Cell Titer-Glo assay, IC50 = 0.039 μM.	29602036
Function assay	Hs578T	100 nM	30 mins		Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human Hs578T cells assessed as decrease in MET phosphorylation at 100 nM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot m	29701962
Function assay	HCC1937	100 nM	30 mins		Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human HCC1937 cells assessed as decrease in MET phosphorylation at 100 nM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot	29701962
Antiproliferative assay	NCI-H2228		72 hrs		Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay, IC50 = 0.087 μM.	30223120
Antiproliferative assay	HCC78		72 hrs		Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay, IC50 = 0.17 μM.	30223120
Antiproliferative assay	KARPAS299		72 hrs		Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.24 μM.	30223120
NB1	Growth Inhibition Assay				IC50=91.98 nM	SANGER
NCI-SNU-5	Growth Inhibition Assay				IC50=105.75 nM	SANGER
SR	Growth Inhibition Assay				IC50=126.31 nM	SANGER
SF539	Growth Inhibition Assay				IC50=204.24 nM	SANGER
SU-DHL-1	Growth Inhibition Assay				IC50=336.82 nM	SANGER
SCC-3	Growth Inhibition Assay				IC50=356.76 nM	SANGER
DEL	Growth Inhibition Assay				IC50=369.9 nM	SANGER
CTV-1	Growth Inhibition Assay				IC50=596.48 nM	SANGER
EM-2	Growth Inhibition Assay				IC50=601.34 nM	SANGER
MHH-CALL-2	Growth Inhibition Assay				IC50=682.57 nM	SANGER
KM12	Growth Inhibition Assay				IC50=706.9 nM	SANGER
KINGS-1	Growth Inhibition Assay				IC50=749.75 nM	SANGER
MEG-01	Growth Inhibition Assay				IC50=857.66 nM	SANGER
BV-173	Growth Inhibition Assay				IC50=1.05997 μM	SANGER
LAMA-84	Growth Inhibition Assay				IC50=1.38282 μM	SANGER
KARPAS-299	Growth Inhibition Assay				IC50=1.40861 μM	SANGER
K-562	Growth Inhibition Assay				IC50=1.72269 μM	SANGER
SK-LMS-1	Growth Inhibition Assay				IC50=1.76867 μM	SANGER
MOLT-16	Growth Inhibition Assay				IC50=1.95575 μM	SANGER
CMK	Growth Inhibition Assay				IC50=1.96159 μM	SANGER
ST486	Growth Inhibition Assay				IC50=2.43073 μM	SANGER
CI-1	Growth Inhibition Assay				IC50=2.49659 μM	SANGER
KP-N-RT-BM-1	Growth Inhibition Assay				IC50=2.70122 μM	SANGER
ALL-PO	Growth Inhibition Assay				IC50=3.18207 μM	SANGER
KS-1	Growth Inhibition Assay				IC50=3.21225 μM	SANGER
Becker	Growth Inhibition Assay				IC50=4.2393 μM	SANGER
GDM-1	Growth Inhibition Assay				IC50=4.24617 μM	SANGER
BC-1	Growth Inhibition Assay				IC50=4.49277 μM	SANGER
NB14	Growth Inhibition Assay				IC50=4.83524 μM	SANGER
NOS-1	Growth Inhibition Assay				IC50=5.33874 μM	SANGER
MZ1-PC	Growth Inhibition Assay				IC50=5.82151 μM	SANGER
A498	Growth Inhibition Assay				IC50=6.08473 μM	SANGER
EW-16	Growth Inhibition Assay				IC50=6.37773 μM	SANGER
NALM-6	Growth Inhibition Assay				IC50=6.68387 μM	SANGER
EB-3	Growth Inhibition Assay				IC50=7.07233 μM	SANGER
697	Growth Inhibition Assay				IC50=9.24329 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay				IC50=9.59842 μM	SANGER
KNS-81-FD	Growth Inhibition Assay				IC50=9.69653 μM	SANGER
HUTU-80	Growth Inhibition Assay				IC50=9.74642 μM	SANGER
LS-411N	Growth Inhibition Assay				IC50=10.0567 μM	SANGER
RPMI-8402	Growth Inhibition Assay				IC50=10.116 μM	SANGER
KU812	Growth Inhibition Assay				IC50=10.2991 μM	SANGER
EW-1	Growth Inhibition Assay				IC50=10.4425 μM	SANGER
HC-1	Growth Inhibition Assay				IC50=10.4844 μM	SANGER
NB69	Growth Inhibition Assay				IC50=10.5043 μM	SANGER
MFH-ino	Growth Inhibition Assay				IC50=10.8303 μM	SANGER
CCRF-CEM	Growth Inhibition Assay				IC50=11.597 μM	SANGER
SK-N-DZ	Growth Inhibition Assay				IC50=12.0436 μM	SANGER
NCI-H720	Growth Inhibition Assay				IC50=12.1705 μM	SANGER
HCC1187	Growth Inhibition Assay				IC50=12.2041 μM	SANGER
IST-SL2	Growth Inhibition Assay				IC50=12.4872 μM	SANGER
KE-37	Growth Inhibition Assay				IC50=12.7966 μM	SANGER
HCC1599	Growth Inhibition Assay				IC50=12.9069 μM	SANGER
A4-Fuk	Growth Inhibition Assay				IC50=12.9586 μM	SANGER
NKM-1	Growth Inhibition Assay				IC50=13.2925 μM	SANGER
BE-13	Growth Inhibition Assay				IC50=13.7989 μM	SANGER
MV-4-11	Growth Inhibition Assay				IC50=14.0324 μM	SANGER
OPM-2	Growth Inhibition Assay				IC50=14.4085 μM	SANGER
KARPAS-422	Growth Inhibition Assay				IC50=14.5126 μM	SANGER
RPMI-8226	Growth Inhibition Assay				IC50=14.8915 μM	SANGER
KARPAS-45	Growth Inhibition Assay				IC50=15.7716 μM	SANGER
SK-PN-DW	Growth Inhibition Assay				IC50=15.8631 μM	SANGER
LC-2	Growth Inhibition Assay				IC50=16.1506 μM	SANGER
NCI-H1648	Growth Inhibition Assay				IC50=16.254 μM	SANGER
RL95-2	Growth Inhibition Assay				IC50=16.3978 μM	SANGER
KNS-42	Growth Inhibition Assay				IC50=16.7274 μM	SANGER
RPMI-6666	Growth Inhibition Assay				IC50=16.9211 μM	SANGER
SIG-M5	Growth Inhibition Assay				IC50=17.1903 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay				IC50=17.7451 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay				IC50=17.9312 μM	SANGER
LAN-6	Growth Inhibition Assay				IC50=18.7557 μM	SANGER
A388	Growth Inhibition Assay				IC50=19.3059 μM	SANGER
SK-NEP-1	Growth Inhibition Assay				IC50=20.2132 μM	SANGER
TE-10	Growth Inhibition Assay				IC50=20.5221 μM	SANGER
HL-60	Growth Inhibition Assay				IC50=20.9099 μM	SANGER
MC116	Growth Inhibition Assay				IC50=21.7221 μM	SANGER
SW962	Growth Inhibition Assay				IC50=21.7915 μM	SANGER
NOMO-1	Growth Inhibition Assay				IC50=22.6564 μM	SANGER
CTB-1	Growth Inhibition Assay				IC50=22.8671 μM	SANGER
MRK-nu-1	Growth Inhibition Assay				IC50=22.9074 μM	SANGER
GR-ST	Growth Inhibition Assay				IC50=23.76 μM	SANGER
HH	Growth Inhibition Assay				IC50=24.003 μM	SANGER
NCI-H1963	Growth Inhibition Assay				IC50=24.0782 μM	SANGER
QIMR-WIL	Growth Inhibition Assay				IC50=24.8772 μM	SANGER
CGTH-W-1	Growth Inhibition Assay				IC50=25.0723 μM	SANGER
LP-1	Growth Inhibition Assay				IC50=25.6551 μM	SANGER
NCI-H748	Growth Inhibition Assay				IC50=26.5137 μM	SANGER
PF-382	Growth Inhibition Assay				IC50=27.2223 μM	SANGER
ATN-1	Growth Inhibition Assay				IC50=27.3732 μM	SANGER
L-540	Growth Inhibition Assay				IC50=27.6459 μM	SANGER
LXF-289	Growth Inhibition Assay				IC50=27.7519 μM	SANGER
LS-513	Growth Inhibition Assay				IC50=28.1807 μM	SANGER
NCI-H1581	Growth Inhibition Assay				IC50=30.3976 μM	SANGER
ES6	Growth Inhibition Assay				IC50=30.6899 μM	SANGER
SW982	Growth Inhibition Assay				IC50=30.8566 μM	SANGER
DOHH-2	Growth Inhibition Assay				IC50=31.5893 μM	SANGER
DB	Growth Inhibition Assay				IC50=33.9431 μM	SANGER
MPP-89	Growth Inhibition Assay				IC50=34.1756 μM	SANGER
LB831-BLC	Growth Inhibition Assay				IC50=34.5184 μM	SANGER
NB5	Growth Inhibition Assay				IC50=34.8535 μM	SANGER
GB-1	Growth Inhibition Assay				IC50=35.0469 μM	SANGER
TE-15	Growth Inhibition Assay				IC50=35.2238 μM	SANGER
LC4-1	Growth Inhibition Assay				IC50=35.3847 μM	SANGER
NCI-H747	Growth Inhibition Assay				IC50=36.1369 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay				IC50=38.7347 μM	SANGER
SK-MM-2	Growth Inhibition Assay				IC50=40.1146 μM	SANGER
TGW	Growth Inhibition Assay				IC50=41.0563 μM	SANGER
ONS-76	Growth Inhibition Assay				IC50=42.4883 μM	SANGER
CPC-N	Growth Inhibition Assay				IC50=42.9971 μM	SANGER
ES4	Growth Inhibition Assay				IC50=44.4153 μM	SANGER
Daudi	Growth Inhibition Assay				IC50=45.0827 μM	SANGER
MOLT-4	Growth Inhibition Assay				IC50=45.0853 μM	SANGER
HT-144	Growth Inhibition Assay				IC50=46.726 μM	SANGER
SW872	Growth Inhibition Assay				IC50=48.1933 μM	SANGER
D-283MED	Growth Inhibition Assay				IC50=48.3542 μM	SANGER
NCI-H2126	Growth Inhibition Assay				IC50=48.8476 μM	SANGER
NCI-SNU-16	Growth Inhibition Assay				IC50=49.2143 μM	SANGER
CESS	Growth Inhibition Assay				IC50=49.5088 μM	SANGER
A101D	Growth Inhibition Assay				IC50=49.9736 μM	SANGER
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화학 정보, 보관 및 안정성

분자량	450.34	화학식	C₂₁H₂₂Cl₂FN₅O	보관 (수령일로부터)	3년-20°C분말
CAS 번호	877399-52-5	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	PF-02341066			Smiles	CC(C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N

용해도

In vitro
배치:

DMSO : 9 mg/mL (19.98 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 45 mg/mL (99.92 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 23 mg/mL (51.07 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 90 mg/mL (199.84 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 25 mg/mL (55.51 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	4.500mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 90%Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.500mg/ml (5.55mM)	Taking the 1 mL working solution as an example, add 100 μL of 25 mg/ml clear DMSO stock solution to 900 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 10%Tween80 3 45%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.500mg/ml (5.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 100 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

Targets/IC₅₀/Ki	ROS1 (Cell-free assay) <0.025 nM(Ki) c-Met (A549, MDA-MB-231, GTL-16, HT29, 786-O, Colo-205, A498 cells) 11 nM ALK (Karpas299 cells) 24 nM
시험관 내(In vitro)	PF-2341066은 mIMCD3 마우스 또는 MDCK 개 상피 세포에서 c-Met 인산화에 대해 유사한 효능을 보이며, IC50은 각각 5 nM 및 20 nM입니다. 이 화합물은 야생형 수용체를 발현하는 NIH3T3 세포(IC50 13 nM)와 비교하여 c-Met ATP 결합 부위 돌연변이 V1092I 또는 H1094R 또는 P-루프 돌연변이 M1250T를 발현하도록 조작된 NIH3T3 세포에 대해 IC50이 각각 19 nM, 2 nM 및 15 nM로 개선되거나 유사한 활성을 보입니다. 대조적으로, c-Met 활성화 루프 돌연변이 Y1230C 및 Y1235D를 발현하도록 조작된 세포에 대해서는 야생형 수용체와 비교하여 IC50이 각각 127 nM 및 92 nM로 이 화합물의 효능에 현저한 변화가 관찰됩니다. 또한 NCI-H69 및 HOP92 세포에서 c-Met 인산화를 강력하게 억제하며, IC50은 각각 13 nM 및 16 nM이고, 이들 세포는 내인성 c-Met 변이체 R988C 및 T1010I를 각각 발현합니다. 이 화합물은 VEGFR2 및 PDGFRβ RTK에 대해 >1,000배, IRK 및 Lck에 대해 >250배, Tie2, TrkA 및 TrkB에 대해 ~40~60배 선택성을 보이며, 모두 c-Met과 비교한 것입니다. RON 및 Axl RTK에 대해서는 20~30배 선택성을 보입니다. 대조적으로, 이 화합물은 KARPAS299 인간 역형성 대세포 림프종(ALCL) 세포주에 의해 발현되는 ALK RTK의 뉴클레오포스민(NPM)-역형성 림프종 키나제(ALK) 종양유전성 융합 변이체에 대해 거의 동일한 IC50인 24 nM을 보입니다. 암세포의 c-Met 의존성 신생물 표현형 및 내피 세포의 혈관신생 표현형을 억제합니다. 이 화학 물질은 인간 GTL-16 위암 세포 성장을 IC50 9.7 nM로 억제합니다. GTL-16 세포에서 IC50 8.4 nM로 세포자멸사를 유도합니다. HGF로 자극된 인간 NCI-H441 폐암 세포 이동 및 침윤을 IC50 11 nM 및 6.1 nM로 각각 억제합니다. MDCK 세포 산란을 IC50 16 nM로 억제합니다. HGF로 자극된 c-Met 인산화, 세포 생존 및 Matrigel 침윤을 IC50 11 nM, 14 nM 및 35 nM로 각각 억제합니다. 또한, 혈청으로 자극된 HMVEC 가지 형성 관 형성(혈관 튜브 형성)을 피브린 젤에서 억제합니다. 또한 Karpas299 또는 SU-DHL-1 ALCL 세포에서 NPM-ALK 인산화를 IC50 24 nM로 강력하게 억제합니다. 이 화합물은 세포 증식을 강력하게 억제하며, 이는 G(1)-S기 세포 주기 정지 및 ALK 양성 ALCL 세포에서 IC50 30 nM로 세포자멸사 유도와 관련이 있지만, ALK 음성 림프종 세포에서는 그렇지 않습니다. 또한, 원발성 종양 성장(즉, 증식 및 생존) 및 전이(예: 침윤 및 클론 형성)와 관련된 골육종 행동을 예방합니다.
키나아제 분석	세포 키나아제 인산화 ELISA 분석
키나아제 분석	세포를 10% 소 태아 혈청(FBS)이 보충된 배지에 96웰 플레이트에 접종하고 24시간 후 무혈청 배지[0.04% 소 혈청 알부민(BSA) 포함]로 옮깁니다. 리간드 의존성 RTK 인산화를 조사하는 실험에서는 해당 성장 인자를 최대 20분 동안 첨가합니다. 세포를 이 화합물과 1시간 동안 및/또는 지정된 시간 동안 적절한 리간드와 함께 배양한 후, 세포를 1mM Na₃VO₄가 보충된 HBSS로 한 번 세척하고 세포에서 단백질 용해물을 생성합니다. 이어서, 96웰 플레이트 코팅에 사용되는 특정 포획 항체와 인산화된 티로신 잔기에 특이적인 검출 항체를 사용하여 샌드위치 ELISA 방법으로 선택된 단백질 키나아제의 인산화를 평가합니다. 항체 코팅 플레이트는 (a) 단백질 용해물 존재 하에 4°C에서 밤새도록 배양하고; (b) 1% Tween 20이 포함된 PBS로 7회 세척하고; (c) 서양 고추냉이 과산화효소-접합 항-총-인산티로신(PY-20) 항체(1:500)에 30분 동안 배양하고; (d) 다시 7회 세척하고; (e) 3,3′,5,5′-테트라메틸 벤지딘 과산화효소 기질에 배양하여 0.09 N H₂SO₄를 첨가하여 중단되는 비색 반응을 시작하고; (f) 분광광도계를 사용하여 450 nm에서 흡광도를 측정합니다.
생체 내(In vivo)	GTL-16 모델에서 PF-2341066은 50 mg/kg/일 및 75 mg/kg/일 치료 코호트 모두에서 43일 투여 일정 동안 평균 종양 부피가 60% 감소하여 크고 확립된 종양(>600 mm³)의 현저한 퇴행을 유발하는 능력을 보여줍니다. 다른 연구에서는 이 화합물이 GTL-16 종양 성장을 3개월 이상 완전히 억제하는 능력을 보였으며, 12마리 쥐 중 1마리만이 50 mg/kg/일의 3개월 치료 일정 동안 종양 성장이 유의하게 증가했습니다. NCI-H441 NSCLC 모델에서 38일 PF-2341066 투여 주기 동안 50 mg/kg/일에서 평균 종양 부피가 43% 감소하는 것이 관찰되었습니다. Caki-1 RCC 모델에서 33일 PF-2341066 투여 주기 동안 50 mg/kg/일에서 각 종양의 부피가 최소 30% 감소하는 것과 관련된 평균 종양 부피가 53% 감소하는 것이 관찰되었습니다. 이 화합물은 또한 U87MG 교모세포종 또는 PC-3 전립선암 이종이식 모델에서 50 mg/kg/일에서 확립된 종양의 성장을 거의 완전히 예방하는 것을 보여주었으며, 연구 마지막 날 각각 97% 또는 84% 억제되었습니다. 대조적으로, 50 mg/kg/일로 경구 투여된 이 화학 물질은 MDA-MB-231 유방암 모델 또는 DLD-1 결장암 모델에서 종양 성장을 유의하게 억제하지 않습니다. GTL-16 종양에서 12.5 mg/kg/일, 25 mg/kg/일 및 50 mg/kg/일에서 CD31 양성 내피 세포의 유의한 용량 의존적 감소가 관찰되었으며, 이는 MVD 억제가 항종양 효능과 용량 의존적 상관 관계를 보임을 나타냅니다. 이 화합물은 GTL-16 및 U87MG 모델 모두에서 인간 VEGFA 및 IL-8 혈장 수치의 유의한 용량 의존적 감소를 보입니다. 이 화합물의 경구 투여 후 GTL-16 종양에서 인산화된 c-Met, Akt, Erk, PLCλ1 및 STAT5 수치의 현저한 억제가 관찰되었습니다. Karpas299 ALCL 종양 이종이식을 이식한 SCID-Beige 마우스에 이 화학 물질을 경구 투여하면 초기 화합물 투여 후 15일 이내에 100 mg/kg/d 용량에서 모든 종양의 완전한 퇴행과 함께 용량 의존적 항종양 효능이 나타납니다. 또한, 포스포리파제 C-감마, 신호 전달 및 전사 활성제 3, 세포외 신호 조절 키나아제, Akt를 포함한 주요 NPM-ALK 신호 전달 매개체의 이 화합물에 의한 억제는 NPM-ALK 인산화 및 기능 억제와 상관 관계가 있는 농도 또는 용량 수준에서 관찰되었습니다. 이 화합물은 원발성 종양 성장(예: 증식 및 생존) 및 전이(예: 침윤 및 클론 형성)와 관련된 골육종 행동을 예방합니다. 이 화학 물질을 경구 위관 영양으로 처리한 누드 마우스에서 골육종 이종이식편의 성장 및 관련 골용해 및 피질외 골 기질 형성은 이 화합물에 의해 예방됩니다. 50 mg/kg의 이 화합물로 c-MET 증폭 GTL-16 이종이식편을 치료하면 ¹⁸F-FDG 섭취의 느린 감소 및 포도당 수송체 1, GLUT-1의 발현 감소와 관련된 종양 퇴행이 유도됩니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/17483355/ [2] https://pubmed.ncbi.nlm.nih.gov/18089725/ [3] https://pubmed.ncbi.nlm.nih.gov/21308771/ [4] https://pubmed.ncbi.nlm.nih.gov/21764800/ [5] https://pubmed.ncbi.nlm.nih.gov/22091388/ [6] https://pubmed.ncbi.nlm.nih.gov/25733882/

적용 분야

방법	바이오마커	이미지	PMID
Western blot	pALK / pAKT / pERK / pS6 pROS1 / ROS1 pSTAT3 / STAT3 PARP / cleaved caspase-3 / Bax / Bcl-2 p-c-Met / c-Met p-mTOR		24675041
Immunofluorescence	LC3 / lysosome SRC / Met α-tubulin cytochrome c p-ALK		26384345

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT06062810	Not yet recruiting	Non-Small Cell Lung Cancer	Han Xu M.D. Ph.D. FAPCR Sponsor-Investigator IRB Chair\|Medicine Invention Design Inc	March 28 2024	Phase 2\|Phase 3
NCT04148066	Completed	Carcinoma Non-Small-Cell Lung	The Netherlands Cancer Institute\|Roche Pharma AG	July 17 2019	Not Applicable
NCT03947385	Recruiting	Metastatic Uveal Melanoma\|Cutaneous Melanoma\|Colorectal Cancer\|Other Solid Tumors	IDEAYA Biosciences	June 28 2019	Phase 1\|Phase 2
NCT03672643	Terminated	ALK or ROS1-positive NSCLC	Pfizer	January 28 2019	Phase 4
NCT03439215	Unknown status	Carcinoma Non-Small-Cell Lung	Fondazione Ricerca Traslazionale\|Clinical research technology Srl	June 13 2017	Phase 2

기술 지원

취급 설명서

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자주 묻는 질문

질문 1:
Could you tell me whether this compound represents the pure R-form, or is it the racemic mixture, so a combination of the S- and the R-form?

답변:
Our S1068 is the R enantiomer (except batches 05 and 06, which are the racemate), and S7505 is the S enantiomer.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):