AMG-510(Sotorasib)
Sotorasib (AMG-510) 是一種有效的，口服生物可利用的，選擇性的 KRAS G12C 共價抑制劑。Sotorasib 將 KRAS G12C 鎖定在非活躍的 GDP 約束狀態。Sotorasib 導致 KRAS G12C 突變的局部晚期或轉移性非小細胞肺癌 (NSCLC) 的消退。
此產品僅用于科學研究，我們不為任何個人用途提供產品和服務
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包裝價格促銷價數量
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5mg￥1200.00700.00- +
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10mg￥2000.001200.00- +
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25mg￥3000.002000.00- +
- 貨號: ajci75454
- CAS: 2296729-00-3
- 別名: 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;索托拉西相關雜質;AMG510單一構型
- 分子式: C30H30F2N6O3
- 分子量: 560.59
- 純度: ＞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)
- 儲存: Store at -20°C
- 庫存: 現貨
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].
參考文獻：
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.
