CH6953755
作者：齐岳
发布时间：2023-08-25
09:10:29
点击数：
产品名称：CH6953755
产品描述：
| 产品描述 | CH6953755 is a potent, orally active and selective inhibitor of YES1 kinase (IC50: 1.8 nM). It inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo. |
| 靶点活性 | YES1:1.8 nM |
| 体外活性 | CH6953755 (0.001-1 μM; for 2 hours) prevents the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification. CH6953755 (0.001-1 μM; for 4 days) inhibits the cell growth of YES1-amplified cancer cell lines. CH6953755 (0.1, 0.3, 1, 3 μM) suppresses TEAD luciferase reporter activity in YES1-amplified KYSE70 and RERF-LC-AI. |
| 体内活性 | CH6953755 (p.o.; 7.5, 15, 30, 60 mg/kg) suppresses phospho-Tyr426 YES1 in a dose-dependent manner. CH6953755 (p.o.; 60 mg/kg/day; for 10 days) shows selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors. |
| 分子量 | 552.55 |
| 分子式 | C26H22F2N6O4S |
| CAS No. | 2055918-71-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
