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OTS964
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:1338542-14-5
包装与价格:
包装价格(元)
5 mg电议
50 mg电议
100 mg电议

产品介绍
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。

产品描述

OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC 50 of 28 nM [1]. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a K d of 40 nM [2].

体外活性

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.

体内活性

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.

Cas No.

1338542-14-5

分子式

C23H24N2O2S

分子量

392.51

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years