AZD2932是有效的多靶点激酶抑制剂，细胞试验中的抑制VEGFR2，PDGFβ，PDGFβ 和 PDGFβ 的 IC₅₀ 值分别为8，4，7，9 nM。

AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC 50 s of 8, 4, 7 and 9 nM in cell assay, respectively.

Solid

VEGFR2 8 nM (IC50) PDGFRβ 4 nM (IC50

AZD2932 has a potent and balanced profile against PDGFβ, VEGFR-2, Flt-3 and c-Kit. It 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). has not independently confirmed the accuracy of these methods. They are for reference only.

Twice daily oral dosing (b.i.d.) of AZD2932 10 h apart results in significant tumor growth inhibition of 64% for both 50 and 12.5 mg/kg doses on the day the control animals are terminated. Xenografts bearing non PDGFβ expressing tumor cells are also sensitive to AZD2932 treatment: growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. and and LoVo tumors by 67% at 50 mg/kg b.i.d. This is due AZD2932 potent activity against VEGFR2 as well as a potential effect on pericytes and tumor-associated fibroblasts due to PDGFR a and b inhibition. AZD2932 at 3–50 mg/kg b.i.d. 10 h apart gives 60–80% inhibition of both p-VEGFR2 and p-PDGFβ in a 1:1 ratio. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Plé PA, et al. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6.

In Vitro: DMSO : 10 mg/mL (22.35 mM; Need ultrasonic)配制储备液