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- MedChemExpress(MCE)
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- HY-138188
- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
10161-87-2
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥715.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥650.0 |
| 规格： | 10 mg | 产品价格： | ￥1105.0 |
| 规格： | 25 mg | 产品价格： | ￥2320.0 |
| 规格： | 50 mg | 产品价格： | ￥3944.0 |
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KRA-533
CAS No. : 10161-87-2
MCE 国际站：KRA-533
产品活性：KRA-533 是一种有效的 KRAS 激动剂。KRA-533 与 KRAS 蛋白中的 GTP/GDP binding pocket 结合，防止 GTP 切割，导致 GTP 结合 KRAS 的组成性活性积累，触发癌细胞中凋亡和自噬细胞死亡途径。
研究领域：GPCR/G Protein
作用靶点：Ras
In Vitro: KRA-533 (10 μM; 48 hours; HCC827 cells) enhances KRAS activity to a greater extent.
?KRA-533 (0~15 μM; 48 hours; H157 cells) enhances KRAS activity in a dose-dependent manner, which is associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death.
?KRA-533 (10 μM; 10 days; H292 cells) mediates cell growth suppression than those without KRAS mutation. KRA-533 (5~15 μM) can directly bind to WT, G12C, G12D and G13D mutant KRAS proteins. KRA-533 activates WT KRAS to increase its activity in a dose-dependent manner. KRA-533 further enhances the activities of active KRAS mutants.
In Vivo: KRA-533 (0~30 mg/kg; i.p.; 28 days) suppresses tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induces apoptosis and autophagy in tumor tissues in a dose-dependent manner.
?KRA-533 shows optimal therapeutic index between 7.5 mg/kg and 30 mg/kg doses.
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