TQ-B3139 (Envonalkib, CT-711)

Chemical Structure : TQ-B3139

CAS No.: 1621519-26-3

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货号: PC-49613Not For Human Use, Lab Use Only.

TQ-B3139 (Envonalkib, CT-711) is a potent inhibitor of ALK and c-Met kinases with IC50 of 14.3 and 12.5 nM in cell-free assays, respectively.

规格	价格	库存
2 mg	￥1980	In stock
5 mg	￥3280	In stock
10 mg	￥5280	In stock
25 mg	￥8980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

TQ-B3139 (Envonalkib, CT-711) is a potent inhibitor of ALK and c-Met kinases with IC50 of 14.3 and 12.5 nM in cell-free assays, respectively.
TQ-B3139 (CT-711) inhibits ALK signaling pathway and induces G1 arrest and apoptosis.
TQ-B3139 (CT-711) is an ALK inhibitor with improved ALK inhibitory activity compared with crizotinib.
TQ-B3139 (CT-711) is preferentially efficacious against cells expressing EML4-ALK (NCI-H3122, NCI-H2228), NPM1-ALK (SU-DHL-1) and ALK activating F1174L point mutation (SK-N-SH) with IC50 of 15-500 nM, but not ALK wild-type cells (NCI-H460, HCC827).
TQ-B3139 (CT-711) inhibits c-Met and overcomes resistance conferred by c-Met activition.
TQ-B3139 (CT-711) at a dose of 25 mg/kg inhibits the growth of ALK-driven tumors in vivo, exhibits significantly superiority to crizotinib against 32D harboring EML4-ALK L1196M and EML4-ALK C1156Y mutations.
Envonalkib is a potent, selective, and orally active inhibitor of ALK with IC50 of 1.96 nM, 35.1 nM, and 61.3 nM for WT and mutated L1196M and G1269S-ALK, respectively.
Envonalkib (12.5-25 mg/kg; p.o. once daily for 14 days) inhibits the growth of human non-small cell lung cancer NCI-H2228 nude mice xenografts.

物理化学性质&存储条件

分子量	506.40
分子式	C24H26Cl2FN5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4'-methoxy-6'-((S)-2-methylpiperazin-1-yl)-[3,3'-bipyridin]-6-amine

参考文献

1. Yuxiang Ma, et al. Eur J Cancer. 2022 Sep;173:238-249.