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- HMN-214 173529-46-9

- HMN-214 173529-46-9
HMN-214 173529-46-9
产品描述 描述 HMN-214(IVX214) is a potent PLK1 inhibitor an average IC50 of 0.12 μM.
纯度 99%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 别名 HMN-214,HMN214,HMN 214,IVX214可溶性/溶解性 10 mM in DMSO生物活性 靶点 Polo-like Kinase (PLK)In vitro(体外研究) HMN-214 is a prodrug of HMN-176. HMN-176 shows potent activities against 22 human tumor cell lines, with a mean IC50s of 118 nM. HMN-176 (3-300 nM) inhibits luciferase expression driven by the MDR1 promoter in a dose dependent manner in HeLa cells. HMN-176 (30-3000 nM) also dose-dependently suppresses complex formation on the Y-box. HMN-214 (3.3 μM) enhances luciferase expression relative to vehicle control with the 1,4C-1,4Bis polymer (11-fold) and PEI (37-fold) in PC3-PSMA cells. HMN-214 (≥ 3.3 μM) significantly reduces cell proliferation, causes considerable changes in cell morphology in MB49 cells.In vivo(体内研究) HMN-214 (33 mg/kg, p.o.) converts to HMN-176 in rats. HMN-214 has no effect on the conduction velocity and the amplitude of action potentials in the aciatic and tibial nerves. HMN-214 (20 mg/kg, p.o.) exhibits antitumor activity in mice. HMN-214 (10, 20 mg/kg, p.o.) decreases MDR1 mRNA expression in nude mice bearing KB- and KB-A.1.-derived tumors.参考文献 参考文献 1. Garland LL, et al. Clin Cancer Res. 2006 Sep 1;12(17):5182-9.
2. Takagi M, et al. Invest New Drugs. 2003 Nov;21(4):387-99.
研究领域 研究领域 CancerCell cycleCell divisionCell CycleCell DivisionSpindleCell CycleKinases/PhosphatasesOtherEpigeneticsCell cycleKinases/PhosphatasesOtherNeuroscienceProcessesDrug DiscoverySmall Molecule DrugLead Compound DiscoveryHMN-214 173529-46-9温馨提示:本产品仅作科研实验使用,不支持临床等研究
