货号	规格	价格	上海	北京	珠海	重庆	武汉
S80676-5mg促销	97.30%	￥740.00 ￥592.00 S80676-5mg ￥592.00 现货	8 8	-	-	-	-
S80676-10mg促销	97.30%	￥1440.00 ￥1150.00 S80676-10mg ￥1150.00 现货	5 5	-	-	-	-
S80676-50mg	≥95%	￥4030.00 S80676-50mg ￥4030.00 2-3天	0 货期：2-3天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S80676-5mg促销

97.30%

￥740.00 ￥592.00

S80676-10mg促销

97.30%

￥1440.00 ￥1150.00

S80676-50mg

≥95%

￥4030.00

货期：2-3天

产品描述：

N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively

靶点：

Drug Metabolite;VEGFR;PDGFR;c-Kit

体内研究：

Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo. Sunitinib (80 mg/kg/day) for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with appr 40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model

参考文献：

1. Sun L, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor r 2. Mendel DB, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Can 3. O'Farrell AM, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101(9):3597-605. Epub 2003 Jan 16.

溶解性：

DMSO : 6.25 mg/mL (16.87 mM; ultrasonic and warming and heat to 60°C)

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.7 ml	13.498 ml	26.996 ml
5 mM	0.54 ml	2.7 ml	5.399 ml
10 mM	0.27 ml	1.35 ml	2.7 ml
50 mM	0.054 ml	0.27 ml	0.54 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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