Edotecarin

"目录号: HY-13618

Cell Cycle/DNA Damage-

Edotecarin 是一种有效的topoisomerase I抑制剂，可诱导单链 DNA 断裂，IC50值为 50 nM。

Topoisomerase

相关产品

Doxorubicin hydrochloride-Etoposide-INNO-206-Irinotecan hydrochloride-Campathecin-Daunorubicin Hydrochloride-Topotecan Hydrochloride-Epirubicin hydrochloride-Exatecan Mesylate-SN-38-Idarubicin hydrochloride-Daun02-Tirapazamine-Amsacrine-TAS-103 dihydrochloride-

生物活性

Description

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

IC50& Target

IC50: 50 nM (topoisomerase I)[1]

In Vitro

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].

In Vivo

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].

Clinical Trial

NCT00087503

Pfizer

Stomach Neoplasms

April 2004

Phase 2

NCT00068952

Pfizer

Glioblastoma

August 2003

Phase 3

NCT00070031

Memorial Sloan Kettering Cancer Center-National Cancer Institute (NCI)

Breast Cancer

June 2003

Phase 2

NCT00072332

Memorial Sloan Kettering Cancer Center-National Cancer Institute (NCI)

Esophageal Cancer-Gastric Cancer-Unspecified Adult Solid Tumor, Protocol Specific

August 2003

Phase 1

NCT00067314

Pfizer

Breast Neoplasms-Neoplasm Metastasis

June 2003

Phase 2

View MoreCollapse

References

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

[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.