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OTS514 hydrochloride

OTS514 hydrochloride
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Purity:99.41%
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OTS514 hydrochloride

Catalog No. T4134Cas No. 2319647-76-0
OTS514 hydrochloride is a highly effective TOPK(T-LAK cell-originated protein kinase) inhibitor (IC50: 2.6 nM).
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Pack SizePrice/USDAvailabilityQuantity
1 mg$56In Stock
2 mg$98In Stock
5 mg$177In Stock
10 mg$323In Stock
25 mg$585In Stock
50 mg$789In Stock
100 mg$997In Stock
500 mg$1,990In Stock
1 mL x 10 mM (in DMSO)$177In Stock
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Product Introduction

Bioactivity
Description
OTS514 hydrochloride is a highly effective TOPK(T-LAK cell-originated protein kinase) inhibitor (IC50: 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
AliasOTS-514 hydrochloride, OTS514 hydrochloride(1338540-63-8(free base))
Chemical Properties
Molecular Weight400.92
FormulaC21H20N2O2S.HCl
Cas No.2319647-76-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 27.5 mg/mL (68.59 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4943 mL12.4713 mL24.9426 mL124.7132 mL
5 mM0.4989 mL2.4943 mL4.9885 mL24.9426 mL
10 mM0.2494 mL1.2471 mL2.4943 mL12.4713 mL
20 mM0.1247 mL0.6236 mL1.2471 mL6.2357 mL
50 mM0.0499 mL0.2494 mL0.4989 mL2.4943 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μLDMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μLDMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μLTween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify.
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