HMN-214

HMN-214CAS号: 173529-46-9分子式: C22H20N2O5S分子量: 424.47描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献

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.
  • 分子结构图

    HMN-214