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 potenttopoisomeraseIinhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity[1]. |
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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].
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. |
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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].
| 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. |
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| 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 |
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| 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℃) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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