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CAS No.: 1338545-07-5

OTS964 HCl Catalog No. CSN17709

Synonyms: OTS964 (hydrochloride);OTS964 HCl

OTS-964 is a TOPK (T-LAK cell originated protein kinase) inhibitor with IC50 value of 28 nM, which can specifically block cytokinesis, leading to apoptosis, in a broad range of cancer cells.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 TOPK

IC50:28nM
描述TOPK (T-lymphokine-activated killer cell-originated protein kinase) is highly and frequently transactivated in various cancer tissues, including lung and triple-negative breast cancers, and plays an indispensable role in the mitosis of cancer cells. OTS-964 is a potent TOPK inhibitor with high affinity and selectivity for TOPK kinase with IC₅₀ value of 28 nM. OTS964 (2 μM) could inhibit 79.7% of TOPK activity, whereas the mean and the SD of the inhibitory effects against other kinases were 18.5 and 24.6%, respectively. OTS964 inhibited the growth of TOPK-positive cells with low IC₅₀ values [A549 (31 nM), LU-99 (7.6 nM), DU4475 (53 nM), MDA-MB-231 (73 nM), T47D (72 nM), Daudi (25 nM), UM-UC-3 (32 nM), HCT-116 (33 nM), MKN1 (38 nM), MKN45 (39 nM), HepG2 (19 nM), MIAPaca-2 (30 nM), and 22Rv1 (50 nM)]. In mice bearing LU-99 lung cancer cells, a TGI (tumor growth inhibition) of 44% was observed on day 22 without any body weight loss after intravenous treatment of OTS964 at 40 mg/kg. A TGI of 110% was observed on day 22 after treatment of liposomal OTS964 at 40 mg/kg. The U-99 xenograft mice were intravenously treated with liposomal OTS964 (40 mg/kg) or vehicle at days 1, 4, 8, and 11, and tumors were collected on day 12. Treatment with OTS964 significantly increased the number of LU-99 cells with the “intercellular bridge” (P < 0.0001), which is one of the markers indicating impaired cell division. The oral administration of free OTS964 at 50 or 100 mg/kg once every day for 2 weeks resulted in TGIs of 79 and 113% on day 15, respectively, without any body weight loss in LU-99 xenograft model^[2].
参考文献

[1] Ikeda Y, Park JH, et al. T-LAK Cell-Originated Protein Kinase (TOPK) as a Prognostic Factor and a Potential Therapeutic Target in Ovarian Cancer. Clin Cancer Res. 2016 Dec 15;22(24):6110-6117.
[2] Matsuo Y, Park JH, Miyamoto T, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med. 2014;6(259):259ra145.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3311 mL
- 11.6557 mL
- 23.3114 mL
- 5 mM
- 0.4662 mL
- 2.3311 mL
- 4.6623 mL
- 10 mM
- 0.2331 mL
- 1.1656 mL
- 2.3311 mL

技术信息

CAS号

1338545-07-5

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H25ClN2O2S

运输

蓝冰

分子量

428.97

别名

OTS964 (hydrochloride);OTS964 HCl

溶解度

DMSO	85.0 mg/mL (198.1 mM)
Water	Insoluble
Ethanol	1.0 mg/mL (2.3 mM)

动物实验配方

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