AMG-510CAS号： 2296729-00-3分子式： C30H30F2N6O3分子量： 560.59描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
AMG-510 is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. |
| 纯度 |
98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 别名 |
AMG 510；AMG510；Sotorasib
|
| 外观 |
powder
|
| 可溶性/溶解性 |
DMSO ：100 mg/mL (178.38 mM)；
Ethanol ：100 mg/mL (178.38 mM) |
| 生物活性 | |
| 靶点 |
KRAS(G12C)
|
| In vitro(体外研究) |
AMG 510 inhibits SOS1-catalyzed nucleotide exchange of recombinant mutant KRAS (G12C/C118A) but had minimal effect on KRAS (C118A). AMG 510 also selectively impairs the viability of KRAS p.G12C mutant lines but does not affect cell lines with other KRAS mutations.
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| In vivo(体内研究) |
In preclinical tumor models, AMG 510 rapidly and irreversibly binds to KRAS (G12C), providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Dosed orally (once daily) as a single agent, AMG 510 is capable of inducing tumor regression in mouse models of KRASG12C cancer.
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分子结构图
