T-2513 hydrochloride
T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
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- CAS. Nr.: 187793-52-8
- Formel: C25H28ClN3O5
- Molecular Weight:485.96
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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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Topoisomerase I |
SN-38 is the metabolite of T-2513 hydrochloride[1].
T-2513 hydrochloride has a broad cytotoxicity against a range of human tumor cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:WiDr, HT-29, SK-BR-3, MKN-1, SK-LU-1, LX-1, KB, and HeLaS3 cells
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Concentration:15.1-111.5 ng/mL
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Incubation Time:24 hours
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Result:Exhibited cytotoxicity against a panel of human tumor cell lines with GI50s of 32.1, 97.6, 38.6, 15.6, 111.5, 15.1, 34.0, and 50.9 ng/mL for WiDr, HT-29, SK-BR-3, MKN-1, SK-LU-1, LX-1, KB, and HeLaS3 cells, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats bearing Walker-256 carcinoma[2]
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Dosage:1, 10, and 100 mg/kg
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Administration:
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Result:The ED50 was 23 mg/kg.
Chemical Information
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CAS. Nr. 187793-52-8
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Molecular Weight 485.96
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Formel C25H28ClN3O5
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SMILES
CCC1=C2C(C(N3C2)=CC([C@](O)(C(OC4)=O)CC)=C4C3=O)=NC5=CC=C(OCCCN)C=C51.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.
Reinheit & Dokumentation
Verweise
[1]. Stephan A Veltkamp, et al. Clinical and pharmacologic study of the novel prodrug delimotecan (MEN 4901/T-0128) in patients with solid tumors. Clin Cancer Res. 2008 Nov 15;14(22):7535-44. [Content Brief]
[2]. S Okuno, et al. Complete regression of xenografted human carcinomas by camptothecin analogue-carboxymethyl dextran conjugate (T-0128). Cancer Res. 2000 Jun 1;60(11):2988-95. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)