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- HY-130149
- 2025年12月05日
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- 详细信息
- 询价记录
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
MRTX849
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
2326521-71-3
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥954.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥312.0 |
| 规格： | 5 mg | 产品价格： | ￥718.0 |
| 规格： | 10 mg | 产品价格： | ￥1150.0 |
| 规格： | 25 mg | 产品价格： | ￥2495.0 |
| 规格： | 50 mg | 产品价格： | ￥4000.0 |
| 规格： | 100 mg | 产品价格： | ￥5600.0 |
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Adagrasib
CAS No. : 2326521-71-3
MCE 国际站：Adagrasib
产品活性：Adagrasib (MRTX849) 是一种有效，口服可用，突变选择性的 KRAS G12C 共价抑制剂，具有潜在抗肿瘤活性的。Adagrasib 在半胱氨酸 12 残基处与 KRAS G12C 共价结合，将蛋白锁定在非活性的 GDP 结合构象中，并抑制 KRAS 依赖性信号转导。
研究领域：GPCR/G Protein
作用靶点：Ras
In Vitro: Adagrasib (MRTX849) (0.1-10000 nM; 3-day/2D conditions; 12-day/3D conditions) potently inhibits cell growth in the vast majority of KRAS G12C-mutant cell lines with IC50s ranging between 10 and 973 nM in the 2D format and between 0.2 and 1042 nM in the 3D format.
Adagrasib (0.24-1000 nM; 24 hours) inhibits KRAS-dependent signaling targets including ERK1/2 phosphorylation (Thr202/Tyr204 ERK1; pERK), S6 phosphorylation (RSK-dependent Ser235/236; pS6) and expression of the ERK-regulated DUSP6.
In Vivo: Adagrasib (1-100 mg/kg; i.g.; daily until day 16) demonstrates dose-dependent anti-tumor efficacy over a well-tolerated dose range, and the maximally efficacious dose of MRTX849 is between 30-100 mg/kg/day.
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