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OTS964 hydrochloride

产品编号 T4135 CAS 1338545-07-5

别名: OTS964

OTS964 hydrochloride (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。它也是一种细胞周期蛋白依赖激酶 CDK11抑制剂，结合 CDK11B 的 Kd 值为 40 nM。

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OTS964 hydrochloride, CAS 1338545-07-5

规格	价格/CNY	货期
1 mg	￥ 547	现货
2 mg	￥ 783	现货
5 mg	￥ 1,270	现货
10 mg	￥ 1,990	现货
25 mg	￥ 3,890	现货
50 mg	￥ 5,570	现货
100 mg	￥ 7,790	现货
500 mg	￥ 15,500	现货
1 mL * 10 mM (in DMSO)	￥ 1,250	现货

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其他形式的 OTS964 hydrochloride:

OTS964
询价

选择批次

纯度: 98.02%

纯度: 96.5%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	OTS964 hydrochloride (OTS964) is a potent and selective TOPK inhibitor with potential anticancer activity.
靶点活性	TOPK:28 nM
体外活性	OTS964 inhibits the growth of TOPK-positive cells with low IC50 values [A549 (31 nM), LU-99 (7.6 nM), DU4475 (53 nM), MDAMB- 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)], whereas its growth inhibitory effect against TOPK-negative HT29 cancer cells is significantly weaker, with IC50 of 290 nM. Although OTS964 reveals some suppressive effect on Src family kinases, the response to OTS964 in these cancer cells is not correlated with the expression of Src family kinases c-Src, Fyn, and Lyn, supporting the TOPK-dependent growth inhibitory effects of OTS964. Time lapse imaging in T47D cells shows that treatment with OTS964 induces cytokinesis defects followed by apoptosis
体内活性	Although administration of the free compound induces hematopoietic adverse reactions (leukocytopenia associated with thrombocytosis), the drug delivered in a liposomal formulation effectively causes complete regression of transplanted tumors without showing any adverse reactions in mice. Inhibition of TOPK activity with the liposomal OTS964 suppresses tumor growth through induction of cytokinesis defects and subsequent apoptosis. Although oral administration of OTS964 causes some hematopoietic toxicity, this is a transient effect. The spontaneous recovery from leukocytopenia is occured and the anticancer effectiveness of the oral drug is similar to that of the liposomal formulation, oral administration of the drug may prove to be more practical
细胞实验	Cell lines:?A549 cells, LU-99 cells, DU4475 cells, MDA-MB-231 cells, T47D cells, Daudi cells, UM-UC-3 cells, HCT-116 cells, MKN1 cells, MKN45 cells, HepG2 cells, MIAPaca-2 cells, 22Rv1 cells and HT29 cells Concentrations: --Incubation Time: 72 h Method: Cells (100 μl) are plated in 96-well plates at a certain density. The cells are allowed to adhere overnight before exposure to compounds for 72 hours at 37°C. Plates are read with a spectrophotometer at a wavelength of 450 nm. All assays are carried out in triplicate. After measuring IC50 values, we calculates the z scores to produce P values. After log transformation (base 10) of IC50 values (nM), the mean and SD are calculated for the log values of the IC50 for the 13 TOPK-positive cell lines.Method: Cells (100 μl) are plated in 96-well plates at a certain density. The cells are allowed to adhere overnight before exposure to compounds for 72 hours at 37°C. Plates are read with a spectrophotometer at a wavelength of 450 nm. All assays are carried out in triplicate. After measuring IC50 values, we calculates the z scores to produce P values. After log transformation (base 10) of IC50 values (nM), the mean and SD are calculated for the log values of the IC50 for the 13 TOPK-positive cell lines.
动物实验	Animal Models: BALB/cSLC-nu/nu miceFormulation: 5% glucoseDosages: 40 mg/kgAdministration: i.v.

别名	OTS964
分子量	428.97
分子式	C23H24N2O2S·HCl
CAS No.	1338545-07-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 1 mg/mL (2.33 mM)

DMSO: 79 mg/mL (184.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.3312 mL	11.6558 mL	23.3117 mL	58.2791 mL
DMSO	5 mM	0.4662 mL	2.3312 mL	4.6623 mL	11.6558 mL
	10 mM	0.2331 mL	1.1656 mL	2.3312 mL	5.8279 mL
	20 mM	0.1166 mL	0.5828 mL	1.1656 mL	2.914 mL
	50 mM	0.0466 mL	0.2331 mL	0.4662 mL	1.1656 mL
	100 mM	0.0233 mL	0.1166 mL	0.2331 mL	0.5828 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Matsuo Y, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145

文献引用

1. Wang J, Luo L, Ding Q, et al. Development of a Multi-Target Strategy for the Treatment of Vitiligo via Machine Learning and Network Analysis Methods. Frontiers in pharmacology. 2021, 12.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

OTS964 hydrochloride 1338545-07-5 Apoptosis Cell Cycle/Checkpoint MAPK CDK TOPK inhibit Inhibitor Cyclin dependent kinase OTS964 OTS-964 Hydrochloride OTS 964 OTS-964 hydrochloride OTS964 Hydrochloride OTS-964 OTS 964 Hydrochloride inhibitor

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OTS964 hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords