AMG-510(Sotorasib)
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 导致 KRAS G12C 突变的局部晚期或转移性非小细胞肺癌 (NSCLC) 的消退。
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包装价格促销价数量
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5mg￥1200.00700.00- +
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10mg￥2000.001200.00- +
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25mg￥3000.002000.00- +
- 货号: ajci75454
- CAS: 2296729-00-3
- 别名: Sotorasib；索托拉西布; AMG-510；索托拉司;索托拉西;索拓拉西布;索托拉昔布;索托拉西布;索托拉西相关杂质;AMG510单一构型
- 分子式: C30H30F2N6O3
- 分子量: 560.59
- 纯度: ＞99%
- 溶解度: DMSO : 50 mg/mL (89.19 mM; Need ultrasonic)；H2O : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH)
- 储存: Store at -20°C
- 库存: 现货
Background
AMG-510 is a selective and orally bioavailable KRAS G12C covalent inhibitor.
In vivo pharmacodynamic assays demonstrated dose- and time-dependent inhibition of KRASG12Csignaling in human pancreatic and NSCLC tumor xenografts. Covalent modification of KRASG12C by AMG 510 was measured by mass spectrometry and correlated with p-ERK inhibition in tumors. AMG 510 significantly inhibited the growth of KRAS p.G12C xenografts and resulted in tumor regression. Combination treatment of AMG 510 with standard-of-care and targeted agents demonstrated enhanced tumor growth inhibition compared to either single agent. In a syngeneic model of KRAS p.G12C mutant cancer, AMG 510 treatment significantly inhibited tumor growth and caused regression[1].
In cellular assays, AMG 510 covalently modified KRASG12C and inhibited KRASG12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) in all KRAS p.G12C-mutant cell lines tested but did not inhibit p-ERK in cell lines with various other KRAS mutations. AMG 510 also selectively impaired viability of KRAS p.G12C mutant cell lines but did not affect cell lines with other KRAS mutations[1].
参考文献：
1. Karen Rex, et al. Abstract 3090: In vivo characterization of AMG 510 - a potent and selective KRASG12Ccovalent small molecule inhibitor in preclinical KRASG12Ccancer models. Experimental and Molecular Therapeutics.
2. Marwan Fakih, et al, Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12Cinhibitor, in advanced solid tumors. Journal of Clinical Oncology.
