MELK inhibitor
OTSSP167 (hydrochloride)
CAS: 1431698-10-0
Molecular Formula: C25H29Cl3N4O2
MELK inhibitor - Names and Identifiers
MELK inhibitor - Physico-chemical Properties
| Molecular Formula | C25H29Cl3N4O2 |
| Molar Mass | 523.88236 |
| Solubility | DMSO: ≥ 5.6 mg/mL; H2O: 2 mg/mL |
| Storage Condition | -20℃ |
| In vitro study | OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC 50 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 IC 50 of 0.41 nM. |
| In vivo study | 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. |
MELK inhibitor - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.909 ml | 9.544 ml | 19.088 ml |
| 5 mM | 0.382 ml | 1.909 ml | 3.818 ml |
| 10 mM | 0.191 ml | 0.954 ml | 1.909 ml |
| 5 mM | 0.038 ml | 0.191 ml | 0.382 ml |
Last Update：2024-01-02 23:10:35
MELK inhibitor - Reference Information
| biological activity | OTSSP167 hydrochloride is a highly efficient, ATP competitive MELK inhibitor with an IC50 value of 0.41 nM. |
| target | IC50: 0.41 nM (MELK) |
| in vitro research | OTSSP167 inhibits the growth of A549 (lung), t47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC 50 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 GFP-MELK localization to cell cortex in prometaphase cells. OTSSP167 is a MELK selective inhibitor, exhibits a strong in vitro activity, conferring an IC 50 of 0.41 nM. |
| in vivo study | 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. |
Last Update：2024-04-09 21:04:16
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