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TargetMol.T8684.AMG-510 Sotorasib
  • 品牌:TargetMol
  • 型号:5 mg
  • 货号:T8684
  • cas:2296729-00-3
  • 价格: ¥1227/瓶
  • 发布日期: 2023-05-08
  • 更新日期: 2024-08-30
产品详请
产地
品牌 TargetMol
货号 T8684
用途
英文名称
包装规格 5 mg
纯度 %
CAS编号 2296729-00-3
别名 Sotorasib
分子式
是否进口
产品描述
AMG-510 is a selective and orally bioavailable KRAS G12C covalent inhibitor.
体外活性
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].
体内活性
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].
Cas No.
2296729-00-3
分子式
C30H30F2N6O3
分子量
560.59
别名
AMG-510;Sotorasib
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.
储存和溶解度
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
Powder: -20°C for 3 years
In solvent: -80°C for 2 years