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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 KRASG12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) inall KRAS p.G12C-mutant cell lines.
Sotorasib (AMG-510; 1-10 μM; 72 hours) also potently impairscellular viability in both NCI-H358 and MIA PaCa-2 withIC50≈0.006 μM and 0.009 μM, respectively.Non-KRASG12C lines are insensitive to Sotorasib (IC50>7.5 μM).
In Vivo: In preclinical tumormodels, Sotorasib (AMG-510) rapidly and irreversibly binds to KRASG12C, providing durable suppression of the mitogen-activatedprotein kinase (MAPK) signaling pathway. Sotorasib (orally; oncedaily) is capable of inducing tumor regression in mouse models ofKRAS G12C cancer.
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