OTSSP167 (hydrochloride)
CAS No. : 1431698-10-0
(Synonyms: OTS167 (hydrochloride))
| Size | Price | Stock |
|---|---|---|
| 5mg | $100 | In-stock |
| 10mg | $150 | In-stock |
| 25mg | $250 | In-stock |
| 50mg | $450 | In-stock |
| 100mg | $750 | In-stock |
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| Cat. No. : | HY-15512A |
| M.Wt: | 523.88 |
| Formula: | C25H29Cl3N4O2 |
| Purity: | >98 % |
| Solubility: | H2O : 7.14 mg/mL (ultrasonic);DMSO : 33.33 mg/mL (ultrasonic) |
OTSSP167 (OTS167) hydrochloride is a highly potent and ATP-competitive MELK inhibitor with IC50 value of 0.41 nM.
IC50 & Target:IC50: 0.41 nM (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[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].
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].
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