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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Met (HGFR)-KIN-8741
KIN-8741

Chemical Structure : KIN-8741

CAS No.: 2941104-53-4

KIN-8741 (KIN8741)

货号: PC-24703Not For Human Use, Lab Use Only.

KIN-8741 is a potent, selective type IIb c-Met kinase inhibitor with IC50 of 11 nM for both WT and D1228 N c-Met in cell viability assays utilized engineered Ba/F3-TPR-c-Met-WT and Ba/F3-TPR-c-Met-D1228N.

规格 价格 库存 数量
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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

KIN-8741 is a potent, selective type IIb c-Met kinase inhibitor with IC50 of 11 nM for both WT and D1228 N c-Met in cell viability assays utilized engineered Ba/F3-TPR-c-Met-WT and Ba/F3-TPR-c-Met-D1228N.
KIN-8741 exhibits subnanomolar potency in c-Met kinase assays (0.2 to 0.3 nM), demonstrates excellent selectivity in a full kinase panel of >600 kinases at 100 nM.
KIN-8741 broadly and potently inhibits the proliferation of Ba/F3-TPR-c-Met mutant cells, the D1228X and Y1230X mutations are inhibited in the single digit nanomolar EC50 range (except Y1230C EC50 = 13 nM).
KIN-8741 is the most potent c-Met inhibitor against D1228X/Y1230X mutations, compared with type II inhibitors (cabozantinib, glesatinib and merestinib).
KIN-8741 also potently inhibits back pocket mutations L1195X and F1200X (0.7–51 nM), which show varying degrees of resistance to other type II agents.
KIN-8741 (20-60 mg/kg, BID) displays potent antitumor activity against MET D1228N mutant model, and in MET gene amplification and exon14 deletion NSCLC models.

物理化学性质&存储条件

分子量 511.48
分子式 C26H23F2N3O6
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

N-{3,5-difluoro-4-[(6-{[(2S)-1-hydroxypropan-2-yl]oxy}-7-methoxyquinolin-4-yl)oxy]phenyl}-4-methoxypyridine-3-carboxamide

参考文献

1. Ouyang XS, et al. J Med Chem. 2025 Jun 3. doi: 10.1021/acs.jmedchem.5c00834.

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