Home MAPK TOPK inhibitor - Apoptosis related activator OTS514 hydrochloride

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OTS514 hydrochloride TOPK inhibitor

Cat.No.S7652

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 hydrochloride TOPK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 400.92

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S765201 DMSO]80 mg/mL]false]Water]80 mg/mL]false]Ethanol]5 mg/mL]false Purity: 99.42%
99.42

Chemical Information, Storage & Stability

Molecular Weight 400.92 Formula

C21H20N2O2S.HCl

 Storage (From the date of receipt)
CAS No. 2319647-76-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles Cl.CC(CN)C1=CC=C(C=C1)C2=C3C(=C(C)C=C2O)NC(=O)C4=C3C=CS4

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (199.54 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 80 mg/mL

Ethanol : 5 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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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Mechanism of Action

Targets/IC50/Ki
TOPK [2]
(Cell-free assay)
2.6 nM
In vitro
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].
In vivo
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].
References

Applications

Methods Biomarkers Images PMID
Western blot TOPK p-FOXM1 / FOXM1 S7652-WB1 28075524
Growth inhibition assay Cell viability S7652-viability1 28075524

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