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OTS514 hydrochloride(1338540-63-8(free base))

Catalog No. T4134 CAS 2319647-76-0

Synonyms: OTS-514 hydrochloride

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

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OTS514 hydrochloride(1338540-63-8(free base)), CAS 2319647-76-0

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	OTS514 is a highly effective TOPK(T-LAK cell-originated protein kinase) inhibitor (IC50: 2.6 nM).
Targets&IC50	TOPK:2.6 nM
In vitro	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].
In vivo	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.
Cell Research	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.
Animal Research	Animal: BALB/cSLC-nu/nu mice. Solvent: 5% glucose (i.v.); 0.5% methylcellulose (p.o.). Dosages: 1,2.5,and 5 mg/kg

Synonyms	OTS-514 hydrochloride
Molecular Weight	400.92
Formula	C21H20N2O2S.HCl
CAS No.	2319647-76-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Kato T, et al. Oncotarget. 2016, 7(14):17652-64. 2. Matsuo Y, et al. Sci Transl Med. 2014, 6(259):259ra145. 3. Ikeda Y, et al. Clin Cancer Res. 2016, 22(24):6110-6117.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Preclinical Compound Library HIF-1 Signaling Pathway Compound Library Anti-Obesity Compound Library Hematonosis Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library

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(S)-(−)-Perillyl alcohol CPI-360 Diclofenac Potassium PF-543 GSK1904529A Ezatiostat LYN-1604 Curzerene

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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