产品说明书
Sotorasib
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同义名 : | 索托拉西布（AMG510） ;AMG-510 |
| CAS号 : | 2296729-00-3 | |
| 货号 : | A1155000 | |
| 分子式 : | C30H30F2N6O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 560.59 | |
| MDL号 : | MFCD32062763 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.78mL 0.36mL 0.18mL |
8.92mL 1.78mL 0.89mL |
17.84mL 3.57mL 1.78mL |
| 参考文献 |
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