貨號	規(guī)格	價格	上海	北京	武漢	南京
S81059-5mg	99.3%	￥310.00 S81059-5mg ￥310.00 現(xiàn)貨	9 9	-	-	-
S81059-25mg	99.3%	￥890.00 S81059-25mg ￥890.00 現(xiàn)貨	8 8	-	-	-
S81059-100mg	≥98%	￥2290.00 S81059-100mg ￥2290.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

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.

產(chǎn)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.

靶點：

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

體外研究：

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)

體內(nèi)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

參考文獻(xiàn)：

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

保存條件：

-20℃

配置溶液濃度參考：

	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：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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