OTS514 hydrochloride
Based on 3 publication(s) in Google Scholar
OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells. OTS514 hydrochloride induces cell cycle arrest and apoptosis.
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- CAS. Nr.: 2319647-76-0
- Formel: C21H21ClN2O2S
- Molecular Weight:400.92
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) OTS514 hydrochloride
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Biologische Aktivität
IC50: 2.6 nM (TOPK)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
19.52 nM
Compound: OTS514
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Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
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[PMID: 30453248] |
| HCT-116 | IC50 |
18.89 nM
Compound: OTS514
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Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
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[PMID: 30453248] |
| HCT-15 | IC50 |
187.1 nM
Compound: OTS514
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Antiproliferative activity against human HCT15 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT15 cells after 72 hrs by MTT assay
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[PMID: 30453248] |
OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138+ stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human myeloma cell lines (MM1.S, MM1.R, RPMI 8226, 8226Dox40, KMS34, KMS34CFZ, KMS11, JJN3, LP-1, NCI H929, U266B1)
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Concentration:1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 nM
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Incubation Time:72 hours
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Result:IC50 values ranged from 11.6 to 29.4 nM in parental cell lines, indicating a potent inhibitory effect. Only the RPMI 8226-Dox40 cell line, which overexpresses the multi-drug resistance transporter gene ABCB1, was resistant.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells[1]
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Dosage:1, 2.5, and 5 mg/kg
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Administration:Intravenously treated; once every day for 2 weeks
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Result:Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.
Chemical Information
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CAS. Nr. 2319647-76-0
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Molecular Weight 400.92
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Formel C21H21ClN2O2S
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SMILES
O=C1NC2=C(C(C3=CC=C([C@@H](C)CN)C=C3)=C(O)C=C2C)C4=C1SC=C4.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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J Exp Clin Cancer Res
2023 Apr 4;42(1):80. PMID: 37016377 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845 -
Reinheit & Dokumentation
Verweise
[1]. Matsuo Y, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145. [Content Brief]
[2]. Stefka AT, et al. Potent anti-myeloma activity of the TOPK inhibitor OTS514 in pre-clinical models. Cancer Med. 2020 Jan;9(1):324-334. [Content Brief]
Calculators
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