Gemcitabine Hydrochloride (LY 188011 Hydrochloride) 是一种嘧啶核苷类似物抗代谢药 (nucleoside antimetabolite/analog) 和抗肿瘤剂。Gemcitabine 抑制 DNA 合成 (DNA synthesis) 和修复,导致细胞自噬 (autophagy) 和凋亡 (apoptosis)。
生物活性 | Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is apyrimidine nucleosideanalog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibitsDNA synthesisand repair, resulting inautophagyandapoptosis[1][2]. |
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体外研究 (In Vitro) | Gemcitabine Hydrochloride (purchased from MedChem Express, 0.003-1 μM; 3 days) kills both mouse and human senescent cells effectively and potently[4]. Gemcitabine Hydrochloride inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively[1].
Cell Viability Assay[4] Cell Line: | Non-senescent and replication-induced senescent new born dermal fibroblasts (NBFs) | Concentration: | 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM | Incubation Time: | 3 days | Result: | Killed replication-induced senescent NBFs for 3 days with 11.0% cell viability. |
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体内研究 (In Vivo) | Gemcitabine Hydrochloride can be administered via endotracheal spray in rats without marked toxicity with a maximum tolerated dose of 4 mg/kg once a week for 9 weeks. The toxicity of Gemcitabine is lower via lung than oral administration at dosages of 2, 4, and 6 mg/kg[2]. Treatment of the LSL-KrasG12D/+; LSL-Trp53R172H; Pdx-1-Cre mice with either Gemcitabine (50 mg/kg, i.p.) or the combination DMAPT/Gemcitabine Hydrochloride significantly increases the median survival time by more than 30 days compared to the placebo group (254.5 or 255 days vs. 217.5 days, respectively)[3].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: H2O : 33.33 mg/mL(111.23 mM;Need ultrasonic) DMSO : 25 mg/mL(83.43 mM;ultrasonic and warming and heat to 60℃) DMF : 2.5 mg/mL(8.34 mM;Need ultrasonic) 配制储备液 1 mM | 3.3371 mL | 16.6856 mL | 33.3712 mL | 5 mM | 0.6674 mL | 3.3371 mL | 6.6742 mL | 10 mM | 0.3337 mL | 1.6686 mL | 3.3371 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 (sealed storage, away from moisture and light)。-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: PBS Solubility: 60 mg/mL (200.23 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.94 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.94 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.94 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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