Crizotinib

別名: PF-02341066 中文名稱：克唑替尼

目錄號：S1068 Purity: 99.9%

Crizotinib克唑替尼是一種有效的c-Met和ALK抑制劑，在細胞試驗中IC50分別為11 nM 和 24 nM。它同時也是有效的ROS1抑制劑，其Ki值小于0.025 nM。Crizotinib可在多種肺癌細胞系中通過抑制STAT3通路來誘導(dǎo)自噬。

Crizotinib Chemical Structure

CAS: 877399-52-5

規(guī)格	價格	庫存
10mM (1mL in DMSO)	712.53	現(xiàn)貨
5mg	573.3	現(xiàn)貨
50mg	1220.31	現(xiàn)貨
200mg	1777.23	現(xiàn)貨
1g	4832.1	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.9%

99.9

常與Crizotinib一起在實驗中被使用的化合物

Ceritinib

與Crizotinib作為ALK陽性NSCLC一線治療藥物相比，Ceritinib可顯著延長無進展生存期(PFS)。

Li J, et al. Curr Med Res Opin. 2019;35(1):105-111.

Alectinib

Alectinib在ALK陽性NSCLC的初級治療中比Crizotinib具有更佳的療效和更低的毒性。

Peters S, et al. N Engl J Med. 2017;377(9):829-838.

Brigatinib

與接受Crizotinib治療的患者相比，Brigatinib在ALK陽性NSCLC患者中表現(xiàn)出更長的無進展生存期。

Camidge DR, et al.?N Engl J Med. 2018;379(21):2027-2039.

Lorlatinib?(PF-6463922)

Lorlatinib在ALK突變或ALK擴增神經(jīng)母細胞瘤細胞系中是比Crizotinib更有效的ALK抑制劑。

Tucker ER, et al. Clin Cancer Res. 2023 Apr 3;29(7):1317-1331.

Afatinib

Crizotinib和Afatinib在MPM細胞中表現(xiàn)出抗增殖作用。

Huang L, et al. Am J Cancer Res. 2017 Feb 1;7(2):203-217.

Crizotinib相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	SGX-523 Foretinib PHA-665752 SU11274 BMS-777607 JNJ-38877605 Tivantinib PF-04217903 Tepotinib Savolitinib (AZD6094) MGCD-265 analog Golvatinib (E7050) Merestinib (LY2801653) MK-2461 NPS-1034 AMG 337 Sodium L-ascorbyl-2-phosphate NVP-BVU972 BMS-794833 S49076	點擊展開
相關(guān)化合物庫	激酶抑制劑庫酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫細胞周期化合物庫血管生成相關(guān)化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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
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
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
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 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 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 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 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 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 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 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
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
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 after 72 hrs by MTT assay, IC50 = 0.0954 μM.	24785465
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
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
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	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	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 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	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 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 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 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	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 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	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	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	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	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
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
SNU5	Growth Inhibition Assay		72 h	IC50=0.016 μM	23993328
SKOV3	Growth Inhibition Assay		72 h	IC50=12.85 μM	23993328
SK-MEL-28	Growth Inhibition Assay		72 h	IC50=10.97 μM	23993328
NCI-H661	Growth Inhibition Assay		72 h	IC50=11.47 μM	23993328
NCI-H441	Growth Inhibition Assay		72 h	IC50=17.25 μM	23993328
MKN45	Growth Inhibition Assay		72 h	IC50=0.013 μM	23993328
MDA-MB-231	Growth Inhibition Assay		72 h	IC50=10.8 μM	23993328
MCF7	Growth Inhibition Assay		72 h	IC50=9.58 μM	23993328
HCT116	Growth Inhibition Assay		72 h	IC50=14.82 μM	23993328
EBC1	Growth Inhibition Assay		72 h	IC50=0.023 μM	23993328
KARPAS299	Cytotoxic Assay		2-3 d	IC50=0.0642 μM	23742252
BAF3	Function Assay		2-3 d	Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay with IC50 of 3.479 μM	23742252
BAF3	Function Assay		2-3 d	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	Inhibition of TEL-fused insulin receptor expressed with IC50 of 1.643 μM	23742252
PAE	Function Assay		1 h	Inhibition of TRKA assessed as growth factor-induced autophosphorylation with IC50 of 0.58 μM	21812414
PAE	Function Assay		1 h	Inhibition of TRKB assessed as growth factor-induced autophosphorylation with IC50 of 0.399 μM	21812414
KARPAS299	Kinase Assay		1 h	Inhibition of ALK assessed as growth factor-induced autophosphorylation with IC50 of 0.02 μM	21812414
Jurkat	Function Assay		1 h	Inhibition of LCK assessed as growth factor-induced autophosphorylation with IC50 of 2.741 μM	21812414
HEK293	Function Assay		1 h	Inhibition of IR assessed as growth factor-induced autophosphorylation with IC50 of 2.887 μM	21812414
HEK293	Function Assay		1 h	Inhibition of AXL assessed as growth factor-induced autophosphorylation with IC50 of 0.294 μM	21812414
BAF3-BCL	Function Assay		1 h	Inhibition of ABL assessed as growth factor-induced autophosphorylation with IC50 of 1.159 μM	21812414
A549	Kinase Assay		1 h	Inhibition of human recombinant c-MET kinase expressed assessed as inhibition of HGF-induced autophosphorylation with IC50 of 0.008 μM	21812414
3T3-E	Function Assay		1 h	Inhibition of TIE2 assessed growth factor-induced autophosphorylation with IC50 of 0.448 μM	21812414
3T3	Function Assay		1 h	Inhibition of RON assessed as growth factor-induced autophosphorylation with IC50 of 0.08 μM	21812414
BAF3	Cytotoxic Assay		48 h	Cytotoxicity against mouse BAF3 cells expressing Tel-ALK with IC50 of 0.19 μM	21572589
BAF3	Cytotoxic Assay		48 h	Cytotoxicity against mouse BAF3 cells expressing EML4-ALK with IC50 of 0.28 μM	21572589
BAF3	Cytotoxic Assay		48 h	Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 with IC50 of 2.2 μM	21572589
BAF3	Cytotoxic Assay		48 h	Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 with IC50 of 0.62 μM	21572589
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
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
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
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
Antiproliferative assay	EBC1		72 hrs	Antiproliferative activity against human EBC1 cells after 72 hrs by Cell Titer-Glo assay, IC50 = 0.039 μM.	29602036
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
SMS-KCN	Cytotoxic Assay			Cytotoxicity against human SMS-KCN cells expressing ALK R1275Q mutant with IC50 of 0.91 μM	21572589
SH-SY5Y	Cytotoxic Assay			Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant with IC50 of 0.53 μM	21572589
Kelly	Cytotoxic Assay			Cytotoxicity against human Kelly cells expressing ALK F1174L mutant with IC50 of 0.42 μM	21572589
SU-DHL1	Cytotoxic Assay			Cytotoxicity against human SU-DHL1 cells expressing ALK coexpressing NPM with IC50 of 0.01 μM	21572589
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
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
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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生物活性

產(chǎn)品描述

靶點

ROS1 ^[6] (Cell-free assay)	c-Met ^[1] (A549, MDA-MB-231, GTL-16, HT29, 786-O, Colo-205, A498 cells)	ALK ^[1] (Karpas299 cells)
<0.025 nM(Ki)	11 nM	24 nM

體外研究(In Vitro)
體外研究活性	PF-2341066作用于mIMCD3小鼠和MDCK犬上皮細胞，作用于c-Met磷酸化作用時具有相似效果，IC50分別為5 nM 和20 nM。PF-2341066作用于表達c-Met ATP-結(jié)合位點突變型V1092I 或H1094R或 P-環(huán)突變 M1250T 的NIH3T3 細胞，具有相似的活性，且活力增高，IC50分別為19 nM,2 nM 和15 nM,而作用于表達野生型受體的NIH3T3 細胞時，IC50為13 nM。^[1] 相反, 觀察到PF-2341066作用于表達c-Met活化環(huán)突變型Y1230C 和Y1235D的細胞時，與作用于野生型受體相比，效果發(fā)生顯著改變，IC50分別為127 nM 和92 nM。PF-2341066 作用于分別表達內(nèi)源性c-Met 突變體R988C和 T1010I 的NCI-H69 和HOP92 細胞，也有效抑制c-Met 磷酸化, IC50分別為13 nM 和16 nM。與作用于c-Met相比，PF-2341066作用于VEGFR2 和PDGFRβ RTKs, 選擇性高1000多倍，作用于IRK和Lck選擇性高250多倍，作用于Tie2, TrkA,和TrkB選擇性高40到60倍。PF-2341066 作用于RON和 Axl RTKs時選擇性為20到30倍。相反，PF-2341066 作用于表達ALK RTK 的核磷蛋白 (NPM)- 間變性淋巴瘤激酶(ALK) 致癌融合突變體和 KARPAS299人間變性大細胞淋巴瘤(ALCL)細胞系時具有相近的IC50值，為24 nM。PF-2341066抑制c-Met依賴的癌細胞的腫瘤表現(xiàn)型，和內(nèi)皮細胞的血管生成表現(xiàn)型。PF-2341066抑制人GTL-16胃癌細胞生長，IC50為9.7 nM。PF-2341066誘導(dǎo) GTL-16細胞凋亡，IC50 為8.4 nM。PF-2341066 抑制HGF刺激的人NCI-H441肺癌細胞遷移和入侵，IC50分別為11 nM 和6.1 nM。PF-2341066抑制 MDCK細胞散射，IC50為16 nM。PF-2341066 抑制HGF-刺激的c-Met磷酸化,細胞存活，和Matrigel入侵，IC50分別為11 nM, 14 nM和35 nM。此外, PF-2341066抑制纖維蛋白膠中的血清刺激的 HMVEC分支小管形成 (形成血管)。^[1] PF-2341066 作用于Karpas299 或SU-DHL-1 ALCL細胞，也有效抑制 NPM-ALK磷酸化，IC50 為24 nM。PF-2341066 有效抑制細胞增殖，伴隨著使細胞周期停在G(1)-S期，且誘導(dǎo) ALK陽性的 ALCL 細胞凋亡，IC50為30 nM, 但是作用于ALK陰性的淋巴瘤細胞則無效果。 ^[2] 此外, PF-2341066 抑制骨肉瘤的一些活動行為，及其腫瘤生長 (例如,增殖和存活)和轉(zhuǎn)移 (例如，入侵和形成克隆)。^[3]
激酶實驗	生化激酶實驗
激酶實驗	使用連續(xù)耦合的分光光度測定c-Met催化活性，通過分析NADH消耗率而測定c-Met誘導(dǎo)的ADP產(chǎn)量，這種作用具有時間依賴性。在 340 nm處使用分光光度法在指定時間點測定吸光值的降低而計算NADH的消耗量。為了測定K_i值, 在含實驗試劑的實驗孔中加入不同濃度PF-2341066，然后在37^oC下溫育10分鐘。加入c-Met酶開始進行實驗反應(yīng)。
細胞實驗	細胞系	GTL-16胃癌細胞和T47D乳腺癌細胞
	濃度	0 nM-256 nM
	孵育時間	1小時
	方法	GTL-16胃癌細胞和T47D乳腺癌細胞接種在96孔板上，孔中含培養(yǎng)基，培養(yǎng)基中含10% 胎牛血清(FBS)，然后轉(zhuǎn)移到無血清培養(yǎng)基中[含0.04%牛血清蛋白(BSA)]，處理 24小時。在調(diào)查配體依賴的RTK 磷酸化實驗中，加入相應(yīng)的生長因子，處理20分鐘。細胞和 PF-2341066和/或適當(dāng)配體在指定時間溫育1小時，然后使用含 1 mmol/L Na₃VO₄的HBSS沖洗細胞一次,然后從細胞中獲得蛋白裂解物。隨后,通過夾心酶聯(lián)免疫吸附試驗法使用特定的捕獲抗體在96孔板上測定選定蛋白激酶的磷酸化，使用特點檢測抗體測定磷酸化的酪氨酸殘基。抗體包被的實驗板(a) 在蛋白裂解物存在時，在4^oC下過夜;(b)在溶于PBS的1% Tween-20 中沖洗7次;(c)在辣根過氧化物酶標(biāo)記的抗總磷酸（PY-20）抗體（1:500）中溫育20分鐘;(d) 再次沖洗7次;(e)在3,3^′,5,5^′-四甲基聯(lián)苯胺過氧化物酶底物中溫育，開始顯示反應(yīng)，加入0.09 N H₂SO₄終止反應(yīng); (f)在450 nm 處使用分光光度計測定吸光度。
實驗圖片	檢測方法	檢測指標(biāo)	實驗圖片	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

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	PF-2341066每天按50 mg/kg和75 mg/kg劑量處理GTL-16 模型, 引起大腫瘤 (體積大于600 mm³) 明顯衰退，且按43天處理日程處理后，平均腫瘤體積降低60%。在另一項研究中, PF-2341066處理3個月以上，完全抑制GTL-16腫瘤生長，PF-2341066每天按50 mg/kg劑量處理小鼠，3個月后，只有1/12小鼠的腫瘤生長得到提高。PF-2341066每天按50 mg/kg劑量處理NCI-H441 NSCLC 模型處理周期為38天，觀察到平均腫瘤體積降低43%。PF-2341066 每天按50 mg/kg劑量作用于 Caki-1 RCC模型，處理周期為33天，觀察到平均腫瘤體積降低53%，且每種腫瘤體積降低至少30%。PF-2341066每天按 50 mg/kg劑量作用于 U87MG 惡性膠質(zhì)瘤或PC-3前列腺癌移植瘤模型,幾乎完全抑制腫瘤生長，在實驗最后一天，抑制分別達97% 或84%。相反, PF-2341066每天按50 mg/kg劑量口服給藥處理 MDA-MB-231 乳腺癌模型,或 DLD-1 結(jié)腸癌模型，不會顯著抑制腫瘤生長。PF-2341066每天按12.5 mg/kg, 25 mg/kg, 和50 mg/kg劑量作用于 GTL-16 腫瘤，觀察到CD31陽性內(nèi)皮細胞顯著降低，這種作用存在劑量依賴性，說明 MVD 受抑制，且具有相關(guān)的抗癌高效性，這種作用也存在劑量依賴性。PF-2341066 作用于GTL-16 和 U87MG 模型，顯著降低人VEGFA 和IL-8血漿水平，這種作用存在劑量依賴性。PF-2341066口服處理GTL-16 腫瘤，觀察到磷酸化的c-Met, Akt, Erk, PLCλ1,和 STAT5水平顯著受抑制。^[1]PF-2341066 每天按100 mg/kg劑量口服處理攜帶Karpas299 ALCL 移植瘤的SCID Beige 小鼠，具有抗癌高效性，這種作用存在劑量依賴性，處理15天，所有腫瘤完全衰退。此外, PF-2341066抑制關(guān)鍵NPM-ALK信號調(diào)節(jié)器, 包括磷脂酶C-γ, 信號轉(zhuǎn)導(dǎo)器，及轉(zhuǎn)錄因子3, 細胞外信號調(diào)節(jié)激酶, 和Akt的激活劑，這些與 NPM-ALK 磷酸化和功能受抑制相關(guān)。^[2] PF-2341066 抑制骨肉瘤的一些活動行為，及其腫瘤生長(例如, 增殖和存活)和轉(zhuǎn)移 (例如，入侵和形成克隆)。PF-2341066口服飼喂裸鼠，抑制生長和相關(guān)的骨肉瘤裸鼠移植瘤的骨基質(zhì)的形成。^[3] PF-2341066 按50 mg/kg 劑量處理 c-MET-擴增的GTL-16移植瘤，引起腫瘤衰退，這與¹⁸F-FDG 攝取的緩慢降低相關(guān)，且降低葡糖糖轉(zhuǎn)運蛋白 1, GLUT-1的表達。^[4]
動物實驗	Animal Models	攜帶NCI-H441,或DLD-1,或MDA-MB-231的雌性和雄性nu/nu小鼠
	Dosages	12.5 mg/kg/day, 25 mg/kg/day, 和50 mg/kg/day
	Administration	口服處理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻
[1] Zou HY, et al. Cancer Res. 2007, 67(9), 4408-4417. [2] Christensen JG, et al. Mol Cancer Ther. 2007, 6(12 Pt 1), 3314-3322. [3] Sampson ER, et al. J Bone Miner Res. 2011, 26(6), 1283-1294. [4] Cullinane C, et al. J Nucl Med. 2011, 52(8), 1261-1267. [5] Gong HC, et al. Int J Proteomics. 2011, 2011, 215496. [6] Zou HY, et al. Proc Natl Acad Sci U S A. 2015, 112(11):3493-8. + 展開

參考文獻

[1] Zou HY, et al. Cancer Res. 2007, 67(9), 4408-4417.
[2] Christensen JG, et al. Mol Cancer Ther. 2007, 6(12 Pt 1), 3314-3322.
[3] Sampson ER, et al. J Bone Miner Res. 2011, 26(6), 1283-1294.

[4] Cullinane C, et al. J Nucl Med. 2011, 52(8), 1261-1267.
[5] Gong HC, et al. Int J Proteomics. 2011, 2011, 215496.
[6] Zou HY, et al. Proc Natl Acad Sci U S A. 2015, 112(11):3493-8.

+ 展開

化學(xué)信息&溶解度

分子量	450.34	分子式	C₂₁H₂₂Cl₂FN₅O
CAS號	877399-52-5	SDF	Download Crizotinib SDF
Smiles	CC(C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 25 mg/mL ( (55.51 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 23 mg/mL ( (51.07 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 90 mg/mL ( (199.84 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度批次：現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑					動物體內(nèi)配方計算器
體內(nèi)溶解度批次：現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑	澄清溶液	10%DMSO 1 90%Corn oil	2.5mg/ml (5.55mM)	以 1 mL 工作液為例，取100μL25mg/ml的澄清DMSO儲備液加到900μL玉米油中，混合均勻。工作液請現(xiàn)配現(xiàn)用！	動物體內(nèi)配方計算器
澄清溶液	5%DMSO 1 40%PEG300 2 10%Tween80 3 45%ddH2O	2.5mg/ml (5.55mM)	以 1 mL 工作液為例,取50 μL 50mg/ml的澄清DMSO儲備液加到400 μL PEG300中,混合均勻使其澄清;向上述體系中加入100 μL Tween80,混合均勻使其澄清;然后繼續(xù)加入450 μL ddH2O定容至1mL。工作液請現(xiàn)配現(xiàn)用!
澄清溶液	5%DMSO 1 Corn oil	4.5mg/ml (9.99mM)	以 1 mL 工作液為例，取50μL90mg/ml的澄清DMSO儲備液加到950μL玉米油中，混合均勻。工作液請現(xiàn)配現(xiàn)用！

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術(shù)支持

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操作手冊

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* 必填項

常見問題及建議解決方法

問題 1:
Could you tell me whether this product represents the pure R-form of crizotinib, or is the the racemic Crizotinib, so a mixture of the S- and the R-form?

回答：
Our S1068 Crizotinib is R enantiomer(except batch 05 and 06, they are racemate), and S7505 is 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):

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Crizotinib

產(chǎn)品質(zhì)控

常與Crizotinib一起在實驗中被使用的化合物

Crizotinib相關(guān)產(chǎn)品

相關(guān)信號通路圖

細胞實驗數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實驗計算

技術(shù)支持

常見問題及建議解決方法