OTS964
Modify Date: 2025-08-25 16:27:00
OTS964 structure
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Common Name | OTS964 | ||
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| CAS Number | 1338542-14-5 | Molecular Weight | 392.51 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H24N2O2S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of OTS964OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM[1]. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM[2]. |
| Name | OTS964 |
|---|
| Description | OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM[1]. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM[2]. |
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| Related Catalog | |
| Target |
TOPK:28 nM (IC50) CDK11B:40 nM (Kd) |
| In Vitro | OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation[1]. OTS964 (10 nM; 48 hours) increases cancer cell death[1]. OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner[3]. Cell Proliferation Assay[1] Cell Line: LU-99 cells Concentration: 10 nM Incubation Time: 48 hours Result: Suppressed cancer cell proliferation. Apoptosis Analysis[1] Cell Line: LU-99 cells Concentration: 10 nM Incubation Time: 48 hours Result: Increased cancer cell death. Western Blot Analysis[3] Cell Line: Hs683 cells, H4 cells Concentration: 0.1, 1, 2 μM Incubation Time: 24 and 48 hours Result: Increased the expression of LC3-II and decreased the expression of P62, both in a dose-dependent manner. |
| In Vivo | OTS964 (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression[1]. OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression[1]. Animal Model: Nude mice bearing LU-99 lung cancer cells[1] Dosage: 40 mg/kg Administration: Intravenously; on days 1, 4, 8, 11, 15, and 18 Result: The tumors continued shrinking even after the treatment and finally revealed complete regression. Animal Model: Nude mice bearing LU-99 lung cancer cells[1] Dosage: 50 or 100 mg/kg Administration: Oral administration; once every day for 2 weeks Result: Achieved complete tumor regression. |
| References |
| Molecular Formula | C23H24N2O2S |
|---|---|
| Molecular Weight | 392.51 |