|N-(2-((2-(二甲基氨基)乙基)(甲基)氨基)-5-((4-(1-甲基-1H-吲哚-3-基)嘧啶-2-基)氨基)-6-(2,2,2-三氟乙氧基)吡啶-3-基)丙烯酰胺甲磺酸盐|CsnPharm

CAS No.: 2130958-55-1

甲磺酸伏美替尼 Catalog No. CSN24797

Synonyms: Alflutinib (mesylate);AST2818;甲磺酸伏美替尼

AST2818 mesylate is an EGFR inhibitor.

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技术信息

生物活性

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].
参考文献

[1] Shi Y. Safety, Clinical Activity, and Pharmacokinetics of Alflutinib (AST2818) in Patients With Advanced NSCLC With EGFR T790M Mutation. J Thorac Oncol. 2020 Jun;15(6):1015-1026.
[2] Shi Y. Safety, Clinical Activity, and Pharmacokinetics of Alflutinib (AST2818) in Patients With Advanced NSCLC With EGFR T790M Mutation. J Thorac Oncol. 2020 Jun;15(6):1015-1026.
[3] Liu X. Simultaneous determination of alflutinib and its active metabolite in human plasma using liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2019 Nov 30;176:112735. doi: 10.1016/j.jpba.2019.06.032.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5044 mL
- 7.5222 mL
- 15.0444 mL
- 5 mM
- 0.3009 mL
- 1.5044 mL
- 3.0089 mL
- 10 mM
- 0.1504 mL
- 0.7522 mL
- 1.5044 mL

技术信息

CAS号

2130958-55-1

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H35F3N8O5S

运输

蓝冰

分子量

664.70

别名

Alflutinib (mesylate);AST2818;甲磺酸伏美替尼;Furmonertinib mesylate;AST2818 mesylate

溶解度

DMSO	16.36 mg/mL (24.6 mM)
Water	insoluble

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