Gimatecan(Synonyms: ST1481)

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Gimatecan (Synonyms: ST1481) 纯度: 99.20%

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(Synonyms: ST1481)

Gimatecan Chemical Structure

CAS No. : 292618-32-7

规格 价格 是否有货 数量
5 mg ￥3500 In-stock
10 mg   询价  
50 mg   询价  

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生物活性

Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity[1].

IC50 & Target[1]

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[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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)
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.

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Athymic Swiss nude mice bearing HT1376 model[1]
Dosage: 2 mg/kg
Administration: Treatment per os, every fourth day for four times
Result: Caused a marked tumor growth inhibition during treatment.

Clinical Trial

分子量

447.48

Formula

C25H25N3O5
CAS 号

292618-32-7
中文名称

吉马替康
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2347 mL 11.1737 mL 22.3474 mL
5 mM 0.4469 mL 2.2347 mL 4.4695 mL
10 mM 0.2235 mL 1.1174 mL 2.2347 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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