OTSSP 167 盐酸盐
| 中文名称 | OTSSP 167 盐酸盐 |
|---|---|
| 中文同义词 | OTSSP 167 盐酸盐 |
| 英文名称 | OTSSP167HCL |
| 英文同义词 | OTSSP167HCL;1-[6-(3,5-Dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-ethanone hydrochloride;OTSSP167 HCl (OTS167);Ethanone,1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-,hydrochloride(1:1);OTS-167 hydrochloride;MELK INHIBITOR; OTSSP-167; OTSSP 167;OTSSP167 HCl (OTS167 HCl);OTSSP167hydrochloride/OTSSP-167hydrochloride |
| CAS号 | 1431698-10-0 |
| 分子式 | C25H29Cl3N4O2 |
| 分子量 | 523.88236 |
| EINECS号 | |
| 相关类别 | 医药 |
| Mol文件 | 1431698-10-0.mol |
| 结构式 |  |
OTSSP 167 盐酸盐 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 结晶固体 |
IC50: 0.41 nM (MELK)
OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC 50 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 IC 50 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.