GIMATECAN

生物活性靶点体外研究体内研究 GIMATECAN 试剂级价格

GIMATECAN

CAS号:292618-32-7
英文名:ST1481
中文名:GIMATECAN
CBNumber:CB01011641
分子式:C25H25N3O5
分子量:447.488
MOL File:292618-32-7.mol

GIMATECAN化学性质

沸点 :780.6±70.0 °C(Predicted)
密度 :1.37±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
酸度系数(pKa) :11.20±0.20(Predicted)
形态 :Solid
颜色 :Light yellow to yellow

GIMATECAN性质、用途与生产工艺

生物活性 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。
靶点

Topoisomerase I

体外研究

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 Assay

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)
Concentration:	3 to 300 ng/mL
Incubation Time:	1, 6, and 24 hours
Result:	IC ₅₀ s of 90±3 and 9.0±0.4 ng/mL for MCR and HT1376 cells after treatment for 1 hours. IC ₅₀ s 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.

体内研究

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.