883986-34-3
883986-34-3 結(jié)構(gòu)式
基本信息
中文別名
化合物AZD2932多靶點(diǎn)激酶抑制劑(AZD2932)
英文別名
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
所屬類別
生物化工：蛋白酪氨酸激酶常見問題列表
生物活性
AZD2932 是一種有效的多靶點(diǎn)蛋白酪氨酸激酶抑制劑，對VEGFR-2，PDGFRβ，F(xiàn)lt-3，和 c-Kit 的 IC50 分別為 8 nM，4 nM，7 nM，和 9 nM。體外研究
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).體內(nèi)研究
In C6 rat glial tumor model, AZD2932 (p.o., b.i.d.) results in signi?cant 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.