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- 保存条件:
-20°C, stored under nitrogen
- 英文名:
AMG-510
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
2296729-00-3
- 规格:
10 mM * 1 mL/5 mg/10 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1727.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥1400.0 |
| 规格: | 10 mg | 产品价格: | ¥2400.0 |
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Sotorasib
CAS No. : 2296729-00-3
MCE 国际站:Sotorasib
产品活性:Sotorasib (AMG-510) 是一种有效的,口服生物可利用的,选择性的 KRAS G12C 共价抑制剂。Sotorasib 将 KRAS G12C 锁定在非活跃的 GDP 约束状态。Sotorasib 是临床开发的第一个 KRAS G12C 抑制剂,能使 KRAS G12C 肿瘤消退。
研究领域:GPCR/G Protein
作用靶点:Ras
In Vitro: In cellular assays, Sotorasib (AMG-510) covalently modifies KRAS G12C and inhibits KRAS G12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) in all KRAS p.G12C-mutant cell lines.
?Sotorasib (AMG-510; 1-10 μM; 72 hours) also potently impairs cellular viability in both NCI-H358 and MIA PaCa-2 with IC50≈0.006 μM and 0.009 μM, respectively. Non-KRASG12C lines are insensitive to Sotorasib (IC50>7.5 μM).
In Vivo: In preclinical tumor models, Sotorasib (AMG-510) rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Sotorasib (orally; once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer.
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