货号	规格	价格	上海	北京	珠海	重庆	武汉
S82027-5mg促销	98.90%	￥80.00 ￥64.00 S82027-5mg ￥64.00 现货	9 9	-	-	-	-
S82027-10mg促销	98.90%	￥145.00 ￥116.00 S82027-10mg ￥116.00 现货	9 9	-	-	-	-
S82027-50mg	98.90%	￥550.00 S82027-50mg ￥550.00 现货	2 2	-	-	-	-
S82027-100mg	≥98%	￥790.00 S82027-100mg ￥790.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

SKLB-610是一种多靶点的酪氨酸激酶 (tyrosine kinases)抑制剂。它对VEGFR2的抑制作用最为有效，是FGFR2和PDGFR的弱抑制剂

靶点：

VEGFR2; FGFR2; PDGFR; PDGFR; FGFR2;VEGFR; FGFR; PDGFR

体外研究：

In vitro, SKLB610 shows selective inhibition of VEGF-stimulated human umbilical vein endothelial cells (HUVECs) proliferation, and this proliferation inhibitory effect is associated with decreased phosphorylation of VEGFR2 and p42/44 mitogen-activated protein kinase (p42/44 MAPK). SKLB610 inhibits a panel of human cancer cells proliferation in a concentration-dependent manner and human nonsmall cell lung cancer cell line A549 and human colorectal cancer cell line HCT116 are most sensitive to SKLB610 treatment. At concentration of 10μM, SKLB610 inhibits 65% FGFR2 activity and 55% PDGFRE activity, respectively. Relative to PDGFR2 and FGFR2 SKLB610 has more selective inhibition of VEGFR2 which shows 97% inhibition of VEGFR2 activity at 10μM in vitro. No inhibition of enzyme activity is detected when 10μM of SKLB610 is examined against PI3K, EGFR, Aurora-A, CDK2/cyclinE and CDK6/cyclinD3

体内研究：

In vivo, chronic intraperitoneally administration of SKLB610 at dose of 50mg/kg/d results in significant inhibition in the growth of established human A549 and HCT116 tumor xenografts in nude mice without exhibit toxicity

动物实验：

Animal Models: Female BALB/c nude mice implanted with HCT116 and A549 cells Dosages: 50 mg/kg/day Administration: IP

参考文献：

1. Cao ZX, et al. SKLB610: a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo. Cell Physiol Biochem. 2011, 27(5):565-74.

溶解性：

Soluble in DMSO、Ethanol

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.408 ml	12.038 ml	24.075 ml
5 mM	0.482 ml	2.408 ml	4.815 ml
10 mM	0.241 ml	1.204 ml	2.408 ml
50 mM	0.048 ml	0.241 ml	0.482 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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