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OTSSP167 hydrochloride is an orally administrative MELK selective inhibitor with IC50 of 0.41 nM. OTSSP167 inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like). OTSSP167 exhibits a strong in vitro activity, conferring an IC50 of 0.41nM and in vivo effect on various human cancer xenograft models. OTSSP167 hydrochloride 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.
| Molecular Weight | 523.88 |
| Formula | C25H28Cl2N4O2.HCl |
| CAS Number | 1431698-10-0 |
| Form | Solid |
| Solubility (25°C) | Water ≥ 1 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related MELK Products |
|---|
| MELK-8a hydrochloride
MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC50 of 2 nM. |
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