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- LY-2874455 1254473-64-7

- LY-2874455 1254473-64-7
LY-2874455 1254473-64-7
产品描述 描述 LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.纯度 98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 可溶性/溶解性 100 mM in DMSO and ethanol生物活性 靶点 FGFR2 ,FGFR1 ,FGFR4 ,FGFR3 ,VEGFR2In vitro(体外研究) In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455 inhibits FGF/FGFR-mediated signaling activities. LY2874455 shows FGFR-dependent antiproliferative effects in KMS-11, OPM-2, SNU-16 and KATO-III cells.In vivo(体内研究) LY2874455 exhibits a potent inhibition of FGF-induced Erk phosphorylation in the heart tissues of mice with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively. In mice bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 xenograft, LY2874455 (3 mg/kg p.o.) results in dose-dependent inhibition of the tumor growth.参考文献 参考文献 1. Zhao G, et al. Mol Cancer Ther. 2011, 10(11), 2200-2210.
研究领域 研究领域 CancerGrowth factorsFGFCancerSignal transductionProtein phosphorylationTyrosine kinasesReceptor tyrosine kinasesCardiovascularAngiogenesisGrowth FactorsFGFFGF ReceptorsDevelopmental BiologyLineage specificationEctodermNeuroscienceDevelopmentNeuroscienceNeurology processNeurogenesisSignal TransductionGrowth Factors/HormonesFGFSignal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine KinasesStem CellsLineage MarkersEctodermDrug DiscoverySmall Molecule DrugLead Compound DiscoveryLY-2874455 1254473-64-7温馨提示:本产品仅作科研实验使用,不支持临床等研究
