Gimatecan(ST1481)是一种有效的拓扑异构酶I(topoisomeraseI)抑制剂。Gimatecan是一种具有口服活性的喜树碱类似物。具有抗肿瘤活性。
货号:ajcx30714
CAS:292618-32-7
分子式:C25H25N3O5
分子量：447.48
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity[1].

Gimatecan (3 to 300 ng/mL) significantly inhibits the growth of human bladder cancer models (HT1376 and MCR), thus reflecting antiproliferative potency[1].Gimatecan causes a persistent S-phase arrest At 0.003 µg/mL and the number of S-phase cells increased after treatment with a higher concentration (0.03 µg/mL)[1]. Cell Proliferation Assay[1] Cell Line: HT1376 cells harbor a p53 mutation; MCR cells harbor two p53 mutations: one in exon 4 (CGC→CCC) and one in exon 9 (CAG→TAG)

Gimatecan (2 mg/kg; treatment per os, every fourth day for four times) is effective for inhibiting tumor growth[1]. Animal Model: Athymic Swiss nude mice bearing HT1376 model[1]

[1]. Paola Ulivi, et al. Cellular Basis of Antiproliferative and Antitumor Activity of the Novel Camptothecin Derivative, Gimatecan, in Bladder Carcinoma Models. Neoplasia. 2005 Feb;7(2):152-61.