883986-34-3
883986-34-3 结构式
基本信息
中文别名
化合物AZD2932多靶点激酶抑制剂(AZD2932)
英文别名
CS-1792AZD 2932
AGN-PC-00AQ5T
AZD 2932 USP/EP/BP
AZD 2932
AZD-2932
AGN-PC-00AQ5T
AZD2932
2-(4-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-N-(1-isopropyl-1H-pyrazol-4-yl)acetamide
Benzeneacetamide, 4-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N-[1-(1-methylethyl)-1H-pyrazol-4-yl]-
2-(4-((6,7-dimethoxyquinazolin-4-yl)oxy)phenyl)-N-(1-isopropyl-1H-pyrazol-4-yl)acetamide AZD2932
所属类别
生物化工：蛋白酪氨酸激酶常见问题列表
生物活性
AZD2932 是一种有效的多靶点蛋白酪氨酸激酶抑制剂，对VEGFR-2，PDGFRβ，Flt-3，和 c-Kit 的 IC50 分别为 8 nM，4 nM，7 nM，和 9 nM。体外研究
AZD2932 effectively inhibits the activities of VEGFR-2 (IC50, 8 nM), PDGFRβ (IC50,4 nM), Flt-3 (IC50, 7 nM), and c-Kit (IC50, 9 nM). AZD2932 inhibits both PDGFRα and PDGFRβ phosphorylation with a correlation close to 1:1. AZD2932 does not inhibit the various cytochrome P450 isoforms with the worst IC50 being against 2C9 (8.0 μM). AZD2932 has no activity against hERG (IC50, 137 μM).体内研究
In C6 rat glial tumor model, AZD2932 (p.o., b.i.d.) results in significant TGI of 64% for both 50 and 12.5 mg/kg doses. Growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. (p.o.) and LoVo tumors by 67% at 50 mg/kg b.i.d (p.o.). AZD2932 (3–50 mg/kg, p.o.) causes 60–80% inhibition of both p-VEGFR-2 and p-PDGFRβ. Single bolus oral doses of AZD2932 results in dose-related inhibition of PDGFRa phosphorylation 6 h after dosing.