AMG-510

AMG510单一构型生物活性靶点体外研究体内研究MSDS用途与合成方法AMG510单一构型价格(试剂级)上下游产品信息中文名称:AMG510单一构型中文同义词:AMG510单一构型;(1R)-6-氟-7-(2-氟-6-羟基苯基)-1-[4-甲基-2-(1-甲基乙基)-3-吡啶基]-4-[(2S)-2-甲基-4-(1-氧代-2-丙烯-1-基)-1-哌嗪基]-吡啶并[2,3-D]嘧啶-2(1H)-酮;索托拉西;索托拉司;SOTORASIB单一构型;AMG510游离态;索托拉西布;AMG510(索托拉西布)英文名称:Sotorasib英文同义词:PYRIDO[2,3-D]PYRIMIDIN-2(1H)-ONE,6-FLUORO-7-(2-FLUORO-6-HYDROXYPHENYL)-1-[4-METHYL-2-(1-METHYLETHYL;Pyrido[2,3-d]pyrimidin-2(1H)-one,6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-,(1R)-;AMG-510(Sotorasib);6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one;Storasib;CID137278711;Pyrido[2,3-d]pyrimidin-2(1H)-one,6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-,(1R)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one;SotorasibCAS号:2296729-00-3分子式:C30H30F2N6O3分子量:560.61EINECS号:相关类别:抑制剂;标准品;小分子抑制剂;原料;抗肿瘤类;原料药及中间体;科研出口类;特殊化学品;贝尔卡主打;武汉贝尔卡主打;APIMol文件:2296729-00-3.molAMG510单一构型性质沸点730.5±70.0°C(Predicted)密度1.36±0.1g/cm3(Predicted)酸度系数(pKa)6.52±0.35(Predicted)AMG510单一构型用途与合成方法生物活性Sotorasib(AMG510)是有效的KRASG12C共价抑制剂，具有潜在的抗肿瘤活性。该AMG510是手性化合物。靶点TargetValueK-Ras(G12C)()体外研究AMG510抑制SOS1催化的重组突变体KRAS(G12C/C118A)的核苷酸交换，但对单突变KRAS(C118A)影响甚微。AMG510选择性地降低含KRASp.G12C突变的细胞系生存活力，而对含其它KRAS突变的细胞系无影响。体内研究在临床前肿瘤模型中，AMG510可快速地以不可逆方式结合KRAS(G12C)，持久地抑制MAPK信号通路。对含KRAS(G12C)突变的小鼠肿瘤模型通过口服途径单次给药，AMG510能够诱导肿瘤消退。安全信息MSDS信息