dw10075anovelselectiveandsmallmoleculeinhibitorofvegfrexhibitsantitumoractivitiesbothinvitroandinvivo

	dw10075anovelselectiveandsmallmoleculeinhibitorofvegfrexhibitsantitumoractivitiesbothinvitroandinvivo
	Ll Mengyuan 2; Lv Yongcong 3; Tong Linjiang 3; Peng Ting 3; Qu Rong 3; Zhang Tao 1; Sun Yiming 3; Chen Yi 3; Wei Lixin 2; Geng Meiyu 3
刊名	actapharmacologicasinica
	2016
卷号	37 期号:3 页码:398
关键词	DW10075 VEGF/VEGF receptor inhibitor Antitumor Angiogenesis U87-MG human glioblastoma
ISSN号	1671-4083
英文摘要	Aim: Targeting the VEGF Methods: In vitro tyrosine kinase activity was measured using ELISA, and intracellular signaling pathway proteins were detected by Western blot analysis. Endothelial cell proliferation was examined with CCK-8 assays, and tumor cell proliferation was determined with SRB assays. Cell migration, tube formation and rat aortic ring assays were used to detect antiangiogenic activity. Antitumor efficacy was further evaluated in U87-MG human glioblastoma xenograft tumors in nude mice receiving DW10075 (500 mg·kg ?1 ·d ?1 , po ) for two weeks. Results: Among a panel of 21 kinases tested, DW10075 selectively inhibited VEGFR-1, VEGFR-2 and VEGFR-3 (the IC 50 values were 6.4, 0.69 and 5.5 nmol 50 values ranging from 2.2 μmol Conclusion: DW10075 is a potent and highly selective inhibitor of VEGFR that deserves further development.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/287081]
专题	中国科学院上海药物研究所
作者单位	1.中国科学院大学 2.中国科学院西北高原生物研究所 3.中国科学院上海药物研究所
推荐引用方式 GB/T 7714	Ll Mengyuan,Lv Yongcong,Tong Linjiang,et al. dw10075anovelselectiveandsmallmoleculeinhibitorofvegfrexhibitsantitumoractivitiesbothinvitroandinvivo[J]. actapharmacologicasinica,2016,37(3):398.
APA	Ll Mengyuan.,Lv Yongcong.,Tong Linjiang.,Peng Ting.,Qu Rong.,...&Ding Jian.(2016).dw10075anovelselectiveandsmallmoleculeinhibitorofvegfrexhibitsantitumoractivitiesbothinvitroandinvivo.actapharmacologicasinica,37(3),398.
MLA	Ll Mengyuan,et al."dw10075anovelselectiveandsmallmoleculeinhibitorofvegfrexhibitsantitumoractivitiesbothinvitroandinvivo".actapharmacologicasinica 37.3(2016):398.