(4S)-4α-エチル-4,9-ジヒドロキシ-1H-ピラノ[3',4':6,7]インドリジノ[1,2-b]キノリン-3,14(4H,12H)-ジオン

外観

白色～黄色～黄赤色粉末～結晶

説明

DNA topoisomerases relax supercoiled DNA during replication, transcription, recombination, repair, and chromosome condensation. The relaxation of DNA supercoiling by topoisomerase I at single-strand breaks represents a target for anticancer agents to intercalate between DNA base pairs, leading to the activation of apoptotic and cell cycle arrest pathways. (S)-10-hydroxy-Camptothecin is an inhibitor of topoisomerase I originally isolated from the Chinese tree C. acuminata. It is a member of the camptothecin family that demonstrates less toxicity than its parent compound. (S)-10-hydroxy-Camptothecin has strong anti-tumor activity against a wide range of experimental tumors including L1210 leukemia cells (IC₅₀ = 1.15 μM). In vitro treatment of human HepG2 cells with 5-20 μM (S)-10-hydroxy-camptothecin results in cell cycle arrest at the G₂/M phase.

化学的特性

Yellow Solid

使用

A Camptothecin derivative; a topoisomerase inhibitor for cancer therapy