Avitinib maleate
产品说明书
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同义名 : | 艾维替尼 ;Abivertinib maleate; AC0010 maleate |
| CAS号 : | 1557268-88-8 | |
| 货号 : | A175435 | |
| 分子式 : | C30H30FN7O6 | |
| 纯度 : | 97% | |
| 分子量 : | 603.6 | |
| MDL号 : | - | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Avitinib Maleate is the maleate form of Avitinib.Avitinib is an irreversible EGFR inhibitor selectively targeting mutated EGFR active and T790M mutations with IC50 value of 0.18nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50=7.68nM), in the kinase enzymatic assay. AC0010 potently inhibited cellular EGFR-Tyr1068 phosphorylation with IC50 value of 4.4nM and 9.8nM in NCIH1975 cells and HCC827 cells, respectively, accompanied with inhibited phosphorylation of the downstream targets Akt and ERK1/2. In a xenograft model, oral administration of AC0010 at a daily dose of 500 mg/kg resulted in complete remission of tumors with EGFR-active and T790M mutations for over 143 days with no weight loss[2]. | ||
| 作用机制 | Avitinib covalently modifies recombinant EGFR T790M mutation at the target cysteine 797 amino acid.[1] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.66mL 0.33mL 0.17mL |
8.28mL 1.66mL 0.83mL |
16.57mL 3.31mL 1.66mL |
| 参考文献 |
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