| 产品描述： | PDGFRβ 选择性抑制剂;PDGFRβ Selective Inhibitors;;InformationAZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor withIC50of 8 nM, 4 nM, 7 nM, and 9 nM forVEGFR-2,PDGFRβ,Flt-3, andc-Kit, respectively.TargetsPDGFRβ ; Flt3 ; VEGFR-2 ; c-Kit 4 nM; 7 nM; 8 nM; 9 nMIn vitroAZD2932 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).In vivoIn 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. |
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危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京