Gimatecan ST1481|cas:292618-32-7|西域试剂

Gimatecan ST1481,99.20%

产品编号：Bellancom-B0063| CAS NO：292618-32-7| 分子式：C₂₅H₂₅N₃O₅| 分子量：447.48

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。

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货号	价格	库存与货期
Bellancom-B0063	￥3500.00	杭州北京（现货）
Bellancom-B0063	￥5800.00	杭州北京（现货）
Bellancom-B0063	￥11000.00	杭州北京（现货）

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Gimatecan ST1481

产品介绍

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.

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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:	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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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西域网站选购。

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

参考文献

. 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. [Content Brief]

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产品编号(Item Number)

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上游产品 2
39684-28-1 84017-99-2
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Gimatecan ST1481,99.20%

Gimatecan ST1481

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