Edotecarin  (Synonyms: J 107088; PF 804950)

Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC₅₀ of 50 nM.

In the presence of human colon cancer cells labeled with ³Hthymidine, edotecarin (0.6 μmol/L) increases the formation of DNA-protein complexes in a time-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

608.55

C₂₉H₂₈N₄O₁₁

174402-32-5

Solid

Yellow to orange

O=C1N(NC(CO)CO)C(C2=C1C3=C(C4=C2C5=C(N4[C@H]6[C@@H]([C@H]([C@@H]([C@@H](CO)O6)O)O)O)C=C(O)C=C5)NC7=C3C=CC(O)=C7)=O

Room temperature in continental US; may vary elsewhere.

• [1]. Saif MW, et al. Edotecarin: a novel topoisomerase I inhibitor. Clin Colorectal Cancer. 2005 May;5(1):27-36.  [Content Brief]

  [2]. Ciomei M, et al. Antitumor efficacy of edotecarin as a single agent and in combination with chemotherapy agents in a xenograft model. Clin Cancer Res. 2006 May 1;12(9):2856-61.  [Content Brief]