A DNA-intercalating antitumor agent that forms covalent adducts in DNA after being enzymatically activated with CYP3A4

Ellipticine – 25 mg

Brand:
Cayman
CAS:
519-23-3
Storage:
-20
UN-No:
De Minimis - 3462 / 6.1

Ellipticine is an alkaloid isolated from Apocyanaceae plants that exhibits antitumor activities by intercalating into DNA and/or inhibiting DNA topoisomerase II.{30281,30282,30280} It forms covalent adducts in DNA after being enzymatically activated with cytochrome P450 isoforms (e.g., CYP3A4, CYP1A1, or CYP1A2) or by peroxidases in target tissues.{30282,30280} Ellipticine has been shown to inhibit the proliferation of human breast adenocarcinoma MCF-7 cells, leukemia HL-60 and CCRF-CEM cells, neuroblastoma IMR-32, UKF-NB-3, and UKF-NB-4 cells, and U87MG glioblastoma cells with IC50 values ranging from 0.27-4.7 µM.{30282}  

 

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Description

A DNA-intercalating antitumor agent that forms covalent adducts in DNA after being enzymatically activated with CYP3A4, CYP1A1, or CYP1A2 or by peroxidases in target tissues; inhibits the proliferation of human breast adenocarcinoma, leukemia, neuroblastoma, and glioblastoma cells (IC50s = 0.27-4.7 µM)

Formal name: 5,11-dimethyl-6H-pyrido[4,3-b]carbazole

Synonyms:  NSC 71795

Molecular weight: 246.3

CAS: 519-23-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Natural Products|Alkaloids||Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Cancer|DNA Damage and Repair|DNA Intercalating Agents||Research Area|Cancer|DNA Damage and Repair|Topoisomerase||Research Area|Toxicology|Drug Metabolism|Cytochrome P450

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