Gimatecan

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Gimatecan (ST1481) 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 (ST1481) 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).Cell Proliferation AssayCell 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)Concentration:3 to 300 ng/mL Incubation Time:1, 6, and 24 hours Result:IC50s of 90±3 and 9.0±0.4 ng/mL for MCR and HT1376 cells after treatment for 1 hours. IC50s of 5.0±0.2 and 2.8±0.1 ng/mL for MCR and HT1376 cells after treatment for 24 hours. The growth-inhibitory effect was dose-dependent and time-dependent. HT1376 cells were more sensitive than MCR cells at least following a short-term exposure.

Gimatecan (2 mg/kg; treatment per os, every fourth day for four times) is effective for inhibiting tumor growth.Animal Model:Athymic Swiss nude mice bearing HT1376 model Dosage:2 mg/kg Administration:Treatment per os, every fourth day for four times Result:Caused a marked tumor growth inhibition during treatment.

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Cell Cycle/DNA Damage

Topoisomerase

Topoisomerase

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292618-32-7

447.48

C25H25N3O5

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 33.33 mg/mL (74.48 mM; ultrasonic and warming and adjust pH to 10 with NaOH and heat to 60°C )

CC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4ccccc4c(\C=N\OC(C)(C)C)c3Cn1c2=O

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(-20℃)

With Ice Pack

≥ 2 years