产品说明书
Firmonertinib mesylate
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同义名 : | Alflutinib mesylate;Furmonertinib mesylate;AST2818;Alflutinib (mesylate);AST2818 mesylate |
| CAS号 : | 2130958-55-1 | |
| 货号 : | A1176940 | |
| 分子式 : | C29H35F3N8O5S | |
| 纯度 : | 99%+ | |
| 分子量 : | 664.699 | |
| MDL号 : | MFCD31746903 | |
| 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: 4 mg/mL(6.02 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 |
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| 动物实验配方： |
| 生物活性 | |||
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| 靶点 |
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| 描述 | Non-small-cell lung cancer (NSCLC) accounts for approximately 85% of all types of lung cancer. The first- and second-generation EGFR tyrosine kinase inhibitors (TKIs) have been recommended as the first-line therapy for patients with EGFR mutation-positive NSCLC. But almost all patients eventually developed clinical resistance which led to the development of third-generation EGFR-TKIs. AST2818 is a newly developed third-generation EGFR-TKI selective for EGFR-sensitizing and T790M-resistant mutations. AST2818 has a pharmacologically active metabolite, AST5902, which has similar antitumor activity [1]. Nude mice (expressing EGFR L858R and T790M) were treated with AST2818 through gavage once daily [QD] for 28 d. The average tumor growth inhibition was achieved in the 10 and 30 mg/kg AST2818 by 87% and 100%, respectively. Furthermore, AST2818 was safe and well tolerated at daily doses up to 240 mg in patients with advanced NSCLC with confirmed EGFR T790M mutation. The 80 mg daily dose of AST2818 had prolonged antitumor activity in patients with NSCLC [2]. At present, AST2818 has undergone phase II/III clinical trials for non-small cell lung cancer (NSCLC) treatment in China [3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.50mL 0.30mL 0.15mL |
7.52mL 1.50mL 0.75mL |
15.04mL 3.01mL 1.50mL |
| 参考文献 |
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