OTS964,1338542-14-5

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OTS964

CAS No. : 1338542-14-5

MCE 国际站：OTS964

产品活性：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 K_d 值为 40 nM。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：TOPK  |  CDK  |  Apoptosis

In Vitro: OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation.
OTS964 (10 nM; 48 hours) increases cancer cell death.
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.

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.
OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression.

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