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Gimatecan

目录号: PL12367 纯度: ≥99%

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。

CAS No. :292618-32-7

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中文名称	Gimatecan
中文别名	吉马替康
英文名称	Gimatecan
英文别名	Gimatecan;(4S)-11-((E)-((1,1-Dimethylethoxy)imino)methyl)-4-ethyl-4-hydroxy-1,12-dihydro-14H-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4H)-dione;7-[(E)-tert-butyloxyiminomethyl]-camptothecin;(E)-7-phenyl-2-hepten-4,6-diyn-1-ol;(E)-7-tert-butoxyiminomethyl-camptothecin;1-Phenyl-hepten-(5)-trans-diin-(1.3)-ol-(7);2-Heptene-4,6-diyn-1-ol,7-phenyl-,(E);7-(t-butoxy)iminomethylcamptothecin;7-hydroxy-1-phenyl-hept-5E-ene-1,3-diyne;7-Phenyl-hept-2t-en-4,6-diin-1-ol;7-phenyl-hept-2t-ene-4,6-diyn-1-ol;7-tert-butoxyiminomethylcamptothecin;ST1481;trans-1-Hydroxy-7-phenyl-hepten-(2)-diin-(4,6);trans-7-Phenyl-hepten-(2)-diin-(4.6)-ol-(1)
Cas No.	292618-32-7
分子式	C₂₅H₂₅N₃O₅
分子量	447.48
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	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。

产品详情

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。

生物活性

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

性状

Solid

IC50 & Target[1][2]

Topoisomerase I

体外研究(In Vitro)

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). has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay

体内研究(In Vivo)

Gimatecan (2 mg/kg; treatment per os, every fourth day for four times) is effective for inhibiting tumor growth. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic Swiss nude mic

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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.

溶解度数据	In Vitro: DMSO : 33.33 mg/mL (74.48 mM; ultrasonic and warming and adjust pH to 10 with NaOH and heat to 60°C)配制储备液

搜索质检报告(COA)

产品使用指南

Data Sheet

[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Gimatecan

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