Edotecarin is a potent inhibitor oftopoisomeraseIthat can induces single-strand DNA cleavage, withIC₅₀of 50 nM.

In the presence of human colon cancer cells labeled with³Hthymidine, edotecarin (0.6 μmol/L) increases the formation of DNA-protein complexes in a time-dependent manner^[1].

Edotecarin produces an 83% increase in survival in mice bearing intracranial D-456MG glioma and shows a strong antimetastatic effect^[1]. Edotecarin results in tumor growth delays ranging from 10.45 days at the lowest dose (3 mg/kg) to 24.83 days at the highest (100 mg/kg). Combination treatment of edotecarin plus irinotecan improves antitumor activity in vivo compared with either agent alone^[2].

608.55

Solid

C₂₉H₂₈N₄O₁₁

174402-32-5

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