OTSSP167 HCl

    • 货号:MC0518
      • CasNo:
      • 1431698-10-0
      • 分子式:
      • C25H29Cl3N4O2
      • 纯度:
      • >98%
      • 靶点:
      • MELK
      • IC50:
      • IC50: 0.41 nM (MELK)
      • 体外研究:
      • OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC50values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively[1]. OTSSP167 can abrogate the mitotic checkpoint, disrupt MCC and MCC-APC/C interaction in MCF7 cells. OTSSP167 causes GFP-MELK localization to cell cortex in prometaphase cells[2]. OTSSP167 is a MELK selective inhibitor, exhibits a strong in vitro activity, conferring an IC50 of 0.41 nM[3].
      • 体内研究:
      • OTSSP167 (20 mg/kg, i.v.) results in tumor growth inhibition (TGI) of 73% in xenograft mouse model; OTSSP167 (1, 5, and 10 mg/kg, p.o.) reveals TGI of 51, 91, and 108%, respectively. OTSSP167 (20 mg/kg, p.o.) shows no tumor growth suppressive effect on PC-14 xenografts[1].
      • 简介:
      • OTSSP167 is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).
      • 特异性:
      • Target: MELK. Fields: OTSSP167 is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).
      • 来源:
      • Rabbit
      • 稀释:
      • IC50: 0.41 nM (MELK)
      • 浓度:
      • >98%
      • 储存:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • 其他名称:
      • MELK inhibitor; OTSSP-167; OTSSP 167
      • 分子量:
      • 523.88
      • 产品图片