货号:A1155000 同义名: 索托拉西布(AMG510) / AMG-510
Sotorasib 是一种 KRAS G12C 抑制剂,对 KRAS G12C 的 IC50 值为 5.3 nM。Sotorasib 具有抗肿瘤作用,可用于 KRAS 突变相关癌症的研究。
描述 | AMG-510 is a specific covalent inhibitor of K-RAS(G12C) ,which irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. AMG-510 selectively targets the KRAS p.G12C mutant and shows potential antineoplastic activity. KRAS encodes a key signalling protein in tumours, and the G12C KRAS mutation is relatively common in some cancer types. Treatment of KRAS p.G12C lines with covalent KRASG12C inhibitor AMG 510 can increase the expression of HLA[1].AMG 510 is the first drug candidate to target this mutation[1]. In clinical trials, AMG 510 demonstrated anti-tumour activity in the first dosing cohorts and represents a potentially transformative therapy for patients[1]. |
作用机制 | AMG-510 selectively forms an irreversible covalent bond to the sulfur atom in the cysteine residue that is present in the mutated form of KRAS, but not in the normal form. KRASG12C can be targeted with covalent small molecule inhibitor AMG-510 which react with the mutant cysteine adjacent to the switch II pocket (SIIP), locking KRAS in its inactive GDP-bound state[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM | 1.78mL 0.36mL 0.18mL | 8.92mL 1.78mL 0.89mL | 17.84mL 3.57mL 1.78mL |
CAS号 | 2296729-00-3 |
分子式 | C30H30F2N6O3 |
分子量 | 560.59 |
别名 | 索托拉西布(AMG510) ;AMG-510 |
运输 | 蓝冰 |
存储条件 | In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,2-8°C |
溶解方案 | DMSO: 50 mg/mL(89.19 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 30 mg/mL(53.52 mM),配合低频超声,并调节pH至11 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |