Powder: -20°C for 3 years | In solvent: -80°C for 2 years
AMG-510 是一种可口服的选择性 KRAS G12C 共价抑制剂,可将 KRAS G12C 锁定在非活跃的 GDP 约束状态,能使 KRAS G12C 肿瘤消退。
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]. |
别名 | AMG-510 |
分子量 | 560.59 |
分子式 | C30H30F2N6O3 |
CAS No. | 2296729-00-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
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
( < 1 mg/mL refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Sotorasib 2296729-00-3 GPCR/G Protein MAPK Ras AMG 510 KRAS AMG-510 covalent regression mutation Inhibitor G12C anti-tumour inhibit GDP-bound phosphorylation NSCLC AMG510 inhibitor