中文名 | OTSSP167 (hydrochloride) |
英文名 | OTSSP167 (hydrochloride) |
别名 | OTSSP 167 盐酸盐 |
英文别名 | OTSSP 167 OTSSP-167 OTSSP167HCL MELK INHIBITOR OTS-167 hydrochloride OTSSP167 HCl (OTS167) OTSSP167 (hydrochloride) OTSSP167 HCl (OTS167 HCl) 1-[6-(3,5-Dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-ethanone hydrochloride |
CAS | 1431698-10-0 |
化学式 | C25H29Cl3N4O2 |
分子量 | 523.88236 |
溶解度 | DMSO: ≥ 5.6 mg/mL; H2O: 2 mg/mL |
存储条件 | -20℃ |
体外研究 | 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. |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.909 ml | 9.544 ml | 19.088 ml |
5 mM | 0.382 ml | 1.909 ml | 3.818 ml |
10 mM | 0.191 ml | 0.954 ml | 1.909 ml |
5 mM | 0.038 ml | 0.191 ml | 0.382 ml |
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