BMS-754807

• 产品号: S1124
• CAS号: 1001350-96-4
• 分子式: C23H24FN9O
• 分子量: 461.4947632
• 保 存: -20°C

产品别名

• 标题: BMS-754807
• IUPAC标准名: (2S)-1-{4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide
• IUPAC传统名: (2S)-1-{4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide
• 别名: BMS754807

产品登记号

• CAS号: 1001350-96-4

产品性质

• 作用靶点: IGF-1R
• 成盐信息: Free Base
• 保存条件: -20°C

产品详细信息

详细说明 (English)

Biological Activity:
BMS-754807 is an orally bioavailable antagonist of human insulin-like growth factor type I receptor (IGF-1R) with potential antineoplastic activity. [1] BMS-754807 inhibits the phosphorylation of IGF-1R (IC50 = 13nM) and the downstream targets Akt (IC50 = 22nM) and MAPK (IC50 = 13nM) in the IGF-Sal cell line with IC50 consistent with the antiproliferative IC50 (7 nM) in this cell line. [1] The protein binding for BMS-754807 ranges from of 98.5%in mouse plasma to 95.9%in human plasma. [1]BMS-754807 (Compound 9d) achieved complete tumor growth inhibition at the 6.25 mg/kg dose. This agent was identified with strong efficacy in the IGF-Sal tumor model with minimal weight loss at the upper dose. [1]

参考文献

• Mark D. Wittman et al. J. Med. Chem.2009,52(23):7360–7363