產(chǎn)品目錄

規(guī)格	10 mM * 1 mL in DMSO 2mg 5mg 10mg 50mg
CAS	1058137-23-7
別名	E 3810; E3810
化學(xué)名	6-[7-[(1-aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl]oxy-N-methylnaphthalene-1-carboxamide
分子式	C26H25N3O4
分子量	443.49
溶解度	Soluble in DMSO
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

E-3810 is a small-molecule dual inhibitor of VEGF and FGF receptors with IC 50 values of 7, 25, 10, 17.5, 82.5 and 237.5 nM for VEGFR-1, 2, 3, FGFR-1, 2 and 3, respectively [1].

The vascular endothelial growthfactor (VEGF) and fibroblast growth factor (FGF) are important factors in angiogenesis. They promote the process of angiogenesis through binding to their associated tyrosine kinase receptors and trigger a cascade signaling pathway that finally leads to the increased proliferation of the blood vessel cells and permeability of the vessels. Tumor cells are rapidly proliferating cells which need more vessels to deliver nutrients, therefore VEGFR and FGFR are attractive targets in antitumor treatment. As a selective inhibitor of VEGFR and FGFR, E-3810 shows potent effects in both in vitro and in vivo assays [1].

E-3810 exerted potent inhibition effects on all the three receptors of VEGFR family and two members (FGFR-1 and 2) of FGFR family in MTS assay. It also had effects on colony stimulating factor (CSF)-1R with IC50 value of 5 nM. When treated with human umbelical vein cells (HUVEC), E-3810 significantly inhibited cell proliferation induced by the addition of VEGF and bFGF with IC50 values of 40 and 50 nM, respectively. In NIH3T3 cells, E-3810 showed no inhibitory efficacy on PDGFR until the concentration of it was up to μM range, demonstrating the selectivity of E-3810 [1].

In the mice model, oral administration of 20 mg/kg E-3810 for 7 days significantly inhibited vessel formation induced by bFGF. E-3810 also exerted effective inhibition on tumor growth in variety of human tumor xenografts such as A498, HT29 and A2780. Besides that, it was reported that the combination treatment of E-3810 and paclitaxel showed higher antitumor activity than that of paclitaxel with brivanib or sunitinib in the MDA-MB-231 breast cancer xenografts [1, 2].

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1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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