Gimatecan是一种有效的拓扑异构酶 I (Topoisomerase I) 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。

Gimatecan is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.

Gimatecan (3 to 300 ng/mL) significantly inhibits the growth of human bladder cancer models (HT1376 and MCR), thus reflecting antiproliferative potency. 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].

Gimatecan (2 mg/kg; treatment per os, every fourth day for four times) is effective for inhibiting tumor growth[1].

292618-32-7

C25H25N3O5

447.48

LBQ707;STI481

H2O:Insoluble
DMSO:31.5mg/mL (70.4mM),ultrasonic and warming and adjust pH to 10 with NaOH and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years