OTSSP167 (OTS167) is a highly potent and ATP-competitiveMELKinhibitor withIC₅₀value of 0.41 nM.

IC50: 0.41 nM (MELK)

OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC₅₀values 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 IC₅₀of 0.41 nM^[3].

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].

487.42

C₂₅H₂₈Cl₂N₄O₂

1431697-89-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 1.

  OTSSP167 is prepared in vehicle (PBS)^[4].