OTSSP167 hydrochloride (C09-1160-241)

OTSSP167 (OTS167) hydrochloride is a highly potent and ATP-competitive MELK inhibitor with IC 50 value of 0.41 nM.In VitroOTSSP167 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoOTSSP167 (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 0.41 nM (MELK). Specifications and Purity: 99%. Molecular Formula: C25H29Cl3N4O2. Molecular Weight: 523.88. PubChem CID: 135565272. Isomeric SMILES: CC(=O)C1=CN=C2C=CC(=NC2=C1NC3CCC(CC3)CN(C)C)C4=CC(=C(C(=C4)Cl)O)Cl.Cl.