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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Src-CH6953755
CH6953755

Chemical Structure : CH6953755

CAS No.: 2055918-71-1

CH6953755 (CH 6953755)

货号: PC-73124Not For Human Use, Lab Use Only.

CH6953755 (CH 6953755) is a potent, selective, orally available YES1 kinase inhibitor with IC50 of 1.8 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CH6953755 (CH 6953755) is a potent, selective, orally available YES1 kinase inhibitor with IC50 of 1.8 nM.
CH6953755 exhibits good specificity for YES1 among the tested Src family kinases (SFKs), inhibits 8/456 WT and mutant kinases at 10 nM (>60% inhibition) including YES1 and four other SFKs.
CH6953755 inhibits cell growth inhibition of YES1-amplified cancer cell lines.
CH6953755 shows selective antitumor activity against YES1-amplified xenograft tumors.
CH6953755 inhibits YAP1 nuclear localization, neither the YAP1 Y357E nor the Y357F mutation affected the suppression of YAP1 transcriptional activity by CH6953755.
YES1-YAP1 signal inhibition by CH6953755 leads to antitumor activity in YES1-amplified cancer cells.

物理化学性质&存储条件

分子量 552.557
分子式 C26H22F2N6O4S
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-(2-(5-Amino-1-(6-(2,6-difluorophenoxy)-4-methylpyridin-3-yl)-1H-pyrazole-4-carbonyl)-5-methyl-1H-indol-6-yl)methanesulfonamide

参考文献

1. Hamanaka N, et al. Cancer Res. 2019 Nov 15;79(22):5734-5745.

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