產(chǎn)品屬性：
產(chǎn)品名稱 | Sotorasib |
規(guī)格 | 10mM*1 mL in DMSO、5 mg、10 mg、50 mg、100 mg |
貨號 | EY-01Y16644 |
Cas No.: 2296729-00-3
別名: N/A
化學(xué)名: N/A
分子式: C30H30F2N6O3
分子量: 560.59
溶解度: DMSO : 100 mg/mL (178.38 mM; Need ultrasonic)|H2O : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH)
儲存條件: Store at -20°C, stored under nitrogen
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors[1][2].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[2].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)[3].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[3].[1]. 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. [2]. 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. [3]. Canon J, et al. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019 Nov;575(7781):217-223. [4]. Brian A. Lanman, et al.Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solid tumors. Cancer Chemistry.
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