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CH6953755 是一种具有口服活性、高效性和选择性的 YES1 激酶抑制剂(IC50:1.8 nM)。CH6953755 具有抗癌活性,通过抑制 YES1 激酶来抑制癌细胞增殖。
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CH6953755 是一种具有口服活性、高效性和选择性的 YES1 激酶抑制剂(IC50:1.8 nM)。CH6953755 具有抗癌活性,通过抑制 YES1 激酶来抑制癌细胞增殖。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 527 | 现货 | |
5 mg | ¥ 1,050 | 现货 | |
10 mg | ¥ 1,480 | 现货 | |
25 mg | ¥ 2,660 | 现货 | |
50 mg | ¥ 3,730 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,280 | 现货 |
产品描述 | CH6953755 is an orally active, potent and selective YES1 kinase inhibitor (IC50:1.8 nM).CH6953755 has anticancer activity and inhibits cancer cell proliferation by inhibiting YES1 kinase. |
靶点活性 | YES1:1.8 nM |
体外活性 | CH6953755 inhibits the growth of cancer cell lines with YES1 amplification in a concentration-dependent manner (0.001-1 μM; 4 days)[1]. Preventing autophosphorylation of YES1 at the Tyr426 site, CH6953755 (0.001-1 μM; 2 hours) upregulates enzymatic activity in KYSE70 cells carrying YES1 amplification[1].In KYSE70 and RERF-LC-AI cells with YES1 amplification, CH6953755 (0.1, 0.3, 1, 3 μM) inhibits TEAD luciferase reporter gene activity[1]. |
体内活性 | CH6953755 exhibits selective antitumor activity in xenograft tumors following oral administration (60 mg/kg/day; 10 days), accompanied by inhibition of phosphorylation at Tyr426 of YES1[1]. In a dose-dependent manner, CH6953755 (oral; 7.5, 15, 30, 60 mg/kg) inhibits phosphorylation at Tyr426 of YES1[1]. |
分子量 | 552.55 |
分子式 | C26H22F2N6O4S |
CAS No. | 2055918-71-1 |
Smiles | Cc1cc2cc([nH]c2cc1NS(C)(=O)=O)C(=O)c1cnn(c1N)-c1cnc(Oc2c(F)cccc2F)cc1C |
密度 | 1.52 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (180.98 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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