OTSSP167,1431697-89-0

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OTSSP167

CAS No. : 1431697-89-0

MCE 国际站：OTSSP167

产品活性：OTSSP167 (OTS167) 是一种高效的，ATP 竞争性的 MELK 抑制剂，IC₅₀ 值为 0.41 nM。

研究领域：PI3K/Akt/mTOR

作用靶点：MELK

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. 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 IC₅₀ 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.

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