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  • Gimatecan
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Gimatecan

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。

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¥3775-3775
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3020-3020
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  • 货号: ajcx30714
  • CAS: 292618-32-7
  • 别名: ST1481
  • 分子式: C25H25N3O5
  • 分子量: 447.48
  • 纯度: >98%
  • 溶解度:
  • 储存: 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.

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