OTS964 是一种口服有效的，高亲和力和选择性的TOPK抑制剂，IC50为 28 nM。OTS964 也是一种有效的细胞周期蛋白依赖激酶CDK11抑制剂，结合 CDK11B 的Kd值为 40 nM。
| 生物活性 | OTS964 is an orally active, high affinity and selectiveTOPKinhibitor with anIC50of 28 nM[1]. OTS964 is also a potent inhibitor of thecyclin-dependent kinaseCDK11, which binds to CDK11B with aKdof 40 nM[2]. |
| IC50& Target[1][2] | CDK11B 40 nM (Kd) | TOPK 28 nM (IC50) |
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体外研究
(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. |
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体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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