OTSSP167 HCl

Cas No.:	1431698-10-0
Chemical Name:	MELK inhibitor; OTSSP-167; OTSSP 167
Synonyms:	MELK inhibitor; OTSSP-167; OTSSP 167
SMILES:	C(=O)(C1=C(N[C@H]2CC[C@H](CN(C)C)CC2)C2C(N=C1)=CC=C(C1=CC(Cl)=C(O)C(Cl)=C1)N=2)C.Cl
Formula:	C25H29Cl3N4O2
M.Wt:	523.88
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	OTSSP167 (hydrochloride) is a highly potent MELK inhibitor with IC50 value of 0.41 nM.
In Vivo:	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[1].
In Vitro:	OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC50 values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively[1]. 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[2]. OTSSP167 is a MELK selective inhibitor, exhibits a strong in vitro activity, conferring an IC50 of 0.41 nM[3].