OTS-167 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、选择性的 MELK 抑制剂，IC50 为 0.41 nM。

A highly potent and selective MELK inhibitor with IC50 of 0.41 nM; shows anti-proliferative activity for A549, T47D, DU4475, and 22Rv1 cancer cells with IC50 of 6.7, 4.3, 2.3, and 6.0 nM, respectively; inhibits the phosphorylation of PSMA1 and DBNL, two novel MELK substrates and are important for stem-cell characteristics and invasiveness; shows robust tumor growth inhibition (TGI) in xenograft models; orally active.Blood Cancer Phase 2 Clinical.

OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC50 values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively.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.OTSSP167 is a MELK selective inhibitor, exhibits a strong in vitro activity, conferring an IC50 of 0.41 nM.

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.

OTSSP-167 hydrochloride

PI3K/Akt/mTOR signaling

MELK

MELK

Cancer

Blood cancer

1431698-10-0

523.8824

C25H29Cl3N4O2

>98% (HPLC)

DMSO: ≥ 5.6 mg/mL; H2O: 2 mg/mL

CC(=O)C1=CN=C2C=CC(=NC2=C1NC3CCC(CC3)CN(C)C)C4=CC(=C(C(=C4)Cl)O)Cl.Cl

1-(6-(3,5-dichloro-4-hydroxyphenyl)-4-(((1r,4r)-4-((dimethylamino)methyl)cyclohexyl)amino)-1,5-naphthyridin-3-yl)ethanone hydrochloride

(-20℃)

With Ice Pack

≥ 2 years