Name | OTSSP167 |
Synonyms | CS-1832 OTSSP167 OTSSP 167 OTSSP-167 MELK inhibitor OTSSP 167 hydrochloride OTSSP-167 hydrochloride OTSSP167 (hydrochloride) |
CAS | 1431697-89-0 |
EINECS | 200-258-5 |
Molecular Formula | C25H28Cl2N4O2 |
Molar Mass | 487.42 |
Solubility | DMSO: <1 mg/mLEthanol: <1 mg/mLWater: <1 mg/mL( < 1 mg/ml refers to the product slightly soluble or insoluble) |
Storage Condition | -20℃ |
Use | OTSSP167 is an inhibitor of maternal embryonic leucine zipper kinase (MELK) with IC50 value of 0.41nM . |
Target | MELK |
In vitro study | OTSSP167 inhibits A549, T47D, DU4475, and 22Rv1 cancer cells, which express MELK at high levels with IC50 of 6.7, 4.3, 2.3, and 6.0 nM, respectively. OTSSP167 inhibits the phosphorylation of PSMA1 (proteasome subunit alpha -1) and DBNL(Drebrin-like), which are novel MELK substrates critical for stem cell characterization and invasion. OTSSP167 inhibits the formation of microspheres by breast cancer cells by inhibiting the phosphorylation of psma1. |
In vivo study | OTSSP167 by intravenous and oral administration to mice, using breast, lung, prostate, and pancreatic cancer cell lines for transplantation tumor study, OTSSP167 has a significant inhibitory effect on tumor growth. OTSSP167 20 mg/kg dose of intravenous treatment of MDA-MB-231 model, once every two days, resulting in tumor growth inhibition rate (TGI) of 73%, 10 mg/kg dose of oral treatment, once a day, the growth inhibition rate (TGI) was 72%. OTSSP167 acts on multiple cancer types, is dose-dependent, and MELK-dependent, with little or no effect on body weight loss. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.052 ml | 10.258 ml | 20.516 ml |
5 mM | 0.41 ml | 2.052 ml | 4.103 ml |
10 mM | 0.205 ml | 1.026 ml | 2.052 ml |
5 mM | 0.041 ml | 0.205 ml | 0.41 ml |