OTSSP167 hydrochloride 是一种高效的，ATP 竞争性的MELK抑制剂，其 IC50=0.41 nM。

OTSSP167 hydrochloride is a highly potent inhibitor of MELK(IC50 : 0.41 nM).

OTSSP167 is a highly potent MELK inhibitor with IC of 0.41 nM.?OTSSP167 inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like), which we identified as novel MELK substrates and are important for stem-cell characteristics and invasiveness.?The compound suppressed mammosphere formation of breast cancer cells and exhibited significant tumor growth suppression in xenograft studies using breast, lung, prostate, and pancreas cancer cell lines in mice by both intravenous and oral administration.?This MELK inhibitor should be a promising compound possibly to suppress the growth of tumor-initiating cells and be applied for treatment of a wide range of human cancer.

1431698-10-0

C25H29Cl3N4O2

523.88

OTSSP 167 盐酸盐

DMSO:33 mg/mL (63 mM),Need ultrasonic
H2O:7.14 mg/mL (13.63 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years