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OTS514 hydrochloride

Catalog No.GC25691

OTS514 is a highly potent TOPK(T-LAK cell-originated protein kinase) inhibitor with an IC50 value of 2.6 nM. OTS514 induces cell cycle arrest and apoptosis.

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OTS514 hydrochloride Chemical Structure

Cas No.: 2319647-76-0

Size Price Stock Qty
2mg
$84.00
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5mg
$155.00
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25mg
$499.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

OTS514 is a highly potent TOPK(T-LAK cell-originated protein kinase) inhibitor with an IC50 value of 2.6 nM. OTS514 induces cell cycle arrest and apoptosis.

OTS514 has growth inhibitory effect on five kidney cancer cell lines, VMRC-RCW, Caki-1, Caki-2, 769-P and 786-O, in which TOPK was highly expressed. The IC50 values range from 19.9 to 44.1 nM[1]. OTS514 strongly suppressed the growth of TOPK-positive cancer cells. It also shows significant growth-inhibitory effect on ovarian cancer cell lines with IC50 values of 3.0 to 46 nM[3].

Mouse xenograft studies with human lung cancer cells demonstrated the in vivo efficacy of OTS514 but found that the compound also caused severe hematopoietic toxicity [reduction of red blood cells (RBCs) and white blood cells (WBCs) associated with marked increase in platelets][2]. Oral administration of OTS514 significantly elongated overall survival in the ES-2 abdominal dissemination xenograft model, compared with vehicle control (P < 0.001)[3].

[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.

Chemical Properties

Cas No. 2319647-76-0 SDF Download SDF
Formula C21H20N2O2S.HCl M.Wt 400.92
Solubility DMSO: 80 mg/mL (199.54 mM);Water: 80 mg/mL (199.54 mM);Ethanol: 5 mg/mL (12.47 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.4943 mL 12.4713 mL 24.9426 mL
5 mM 0.4989 mL 2.4943 mL 4.9885 mL
10 mM 0.2494 mL 1.2471 mL 2.4943 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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