AZD2932是一种多靶点激酶抑制剂，细胞试验中能够抑制VEGFR2 (IC50:8 nM)，PDGFβ (IC50:4 nM)，PDGFβ (IC50:7 nM) 和 PDGFβ (IC50:9 nM)。

AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3, and c-Kit.

在C6大鼠胶质瘤模型中,口服AZD2932 (12.5 or 50 mg/kg, b.i.d.)能够抑制肿瘤生长.在带有非PDGFβ表达肿瘤细胞的异种移植物中,口服AZD2932 (50 mg/kg, b.i.d.),Calu-6肿瘤和LoVo肿瘤达生长被抑制.

AZD2932能够抑制PDGFRα和PDGFRβ磷酸化。AZD2932有效抑制多种受体,如VEGFR-2（IC50=8 nM）,PDGFRβ（IC50=4 nM）,Flt-3（IC50=7 nM）和c-Kit（IC50=9 nM）的活性。

Kinase Assays : In vitro kinase IC50 values are measured using 33P filtration binding assay after 1 hour incubation of kinase, 33P-ATP, Ibrutinib, and substrate [0.2 mg/mL poly(EY)(4:1]. Assays are performed at Reaction Biology.

883986-34-3

C24H25N5O4

447.495

H2O:<1 mgml
DMSO:82 mg/mL (183.2 mM)
Ethanol:5 mg/mL (11.17 mM),warmed
Powder: -20°C for 3 years
In solvent: -80°C for 2 years