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OTS514 Hydrochloride
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。
OTS514 Hydrochloride图片
CAS NO:2319647-76-0
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议
10 mg电议
25 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
OTS-514 hydrochloride
产品介绍
OTS5144 hydrochloride 是一种高效的TOPK抑制剂,IC50为 2.6 nM。它可强效抑制 TOPK 阳性的肿瘤细胞生长,诱导细胞周期停滞和凋亡。

产品描述

OTS514 is a highly effective TOPK(T-LAK cell-originated protein kinase) inhibitor (IC50: 2.6 nM).

体外活性

OTS514 can inhibit the growth of kidney cancer cell lines (VMRC-RCW, Caki-1, Caki-2, 769-P, and 786-O), in which TOPK was highly expressed (IC50:19.9-44.1 nM)[1]. OTS514 markedly inhibits the growth of TOPK-positive cancer cells. It also shows the significant growth-inhibitory effect on ovarian cancer cell lines (IC50: 3.0-46 nM)[3].

体内活性

In mouse xenograft studies with human lung cancer cells, OTS514 shows certain efficacy but also caused severe hematopoietic toxicity (reduction of red blood cells and white blood cells associated with marked increase in platelets)[2]. Compared with vehicle control (P< 0.001), OTS514 (p.o.) significantly elongated overall survival in the ES-2 abdominal dissemination xenograft model.

细胞实验

Cell lines: CD34+ HSCs. Concentrations: 20 or 40 nM. Incubation Time: 48 h. Method: Cells were cultured in RPMI supplemented with 20% fetal bovine serum and 1×StemSpan CC100.Cells were treated with OTS514 (20 or 40 nM) or OTS964 (100 or 200 nM) for 48 hours.Collected cells were washed with PBS and resuspended in 100 ml of PBS followed by staining with CD41a antibody for 20 min at room temperature.Finally,the cells were washed with PBS again and then analyzed for CD41a staining by flow cytometry.Expression of STAT5 was examined by Western blot with an anti-STAT5 antibody.

动物实验

Animal: BALB/cSLC-nu/nu mice. Solvent: 5% glucose (i.v.); 0.5% methylcellulose (p.o.). Dosages: 1,2.5,and 5 mg/kg

Cas No.

2319647-76-0

分子式

C21H20N2O2S.HCl

分子量

400.92

别名

OTS-514 hydrochloride

储存和溶解度

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years