货号	规格	价格	上海	北京	珠海	重庆	武汉
S81059-5mg促销	99.30%	￥290.00 ￥232.00 S81059-5mg ￥232.00 现货	8 8	-	-	-	-
S81059-25mg促销	99.30%	￥830.00 ￥664.00 S81059-25mg ￥664.00 现货	7 7	-	-	-	-
S81059-100mg	≥98%	￥2140.00 S81059-100mg ￥2140.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively.

靶点：

VEGFR2:8 nM (IC50);PDGFRβ:4 nM (IC50);FLT3:7 nM (IC50);c-Kit:9 nM (IC50);VEGFR; FLT; PDGFR; c-Kit

体外研究：

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)

体内研究：

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

参考文献：

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.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.235 ml	11.174 ml	22.347 ml
5 mM	0.447 ml	2.235 ml	4.469 ml
10 mM	0.223 ml	1.117 ml	2.235 ml
50 mM	0.045 ml	0.223 ml	0.447 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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