OTSSP167
CAS No. : 1431697-89-0
(Synonyms: OTS167)
| Size | Price | Stock |
|---|---|---|
| 5mg | $100 | In-stock |
| 10mg | $150 | In-stock |
| 25mg | $250 | In-stock |
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| Cat. No. : | HY-15512 |
| M.Wt: | 487.42 |
| Formula: | C25H28Cl2N4O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 2.5 mg/mL (ultrasonic;warming;adjust pH to 4 with 1M HCl;heat to 60°C) |
OTSSP167 (OTS167) 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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