store at low temperture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Gemcitabine 是一种嘧啶核苷类似物抗代谢药和抗肿瘤剂。它抑制 DNA 合成和修复,导致细胞自噬和凋亡。
产品描述 | Gemcitabine is a DNA synthesis inhibitor that can inhibit the growth of MIAPaCa2, BxPC3 and Capan2 cells (IC50s: 40/18/12 nM). It can also induce autophagy. |
靶点活性 | BxPC3:18nM, Capan2:12 nM, MIAPaCa2:40nM |
体外活性 | MTS assay demonstrates that Gemcitabine at 15 nM, indole-3-carbinol (I3C) at 50 μM and the combination does not affect hTERT-HPNE cell viability. However, treatment with Gemcitabine at 15 nM, I3C at 50 μM and the combination result in 31%, 19% and 72% cell death of BxPC-3 cells, respectively[1]. Gemcitabine inhibits the growth of HL-60 promyelocytic leukemia cells (LC50: 40 nM) [2]. Gemcitabine induces autophagy of SPC-A1 and A549 cells [3]. |
体内活性 | Gemcitabine 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 [4]. Treatment of the LSL-KrasG12D/+; LSL-Trp53R172H; Pdx-1-Cre mice with either Gemcitabine (50 mg/kg, i.p.) or the combination DMAPT/Gemcitabine significantly increased the median survival time by more than 30 days compared to the placebo group (254.5 [P=0.015] or 255 days [P=0.018] vs. 217.5 days, respectively) [5]. |
细胞实验 | The cytotoxic effect of gemcitabine was evaluated with the MTT assay. SPC-A1 or A549 cells were treated with gemcitabine (0.05–500 lM) for 24 h. Then, 10 ll of MTT (5 mg/ml in PBS) was added to each well and incubated for 4 h at 37 C. Then, the formazan crystals were solubilized with 200 ll DMSO. The absorbance at 570 nm was measured using an automatic multiwell spectrophotometer. The experiment was repeated four times for each group [3]. |
动物实验 | At 1 month of age, LSL-Kras G12D/+; LSL-Trp53 R172H; Pdx-1-Cre mice are randomized into treatment groups (placebo, DMAPT, Gemcitabine, DMAPT/Gemcitabine). Placebo (vehicle=hydroxylpropyl methylcellulose, 0.2% Tween 80 [HPMT]) and DMAPT (40 mg/kg body weight in HPMT) are administered by oral gastric lavage once daily. Gemcitabine (50 mg/kg body weight in PBS) is administered by intraperitoneal injection twice weekly. Mouse weight is monitored weekly. Treatment is continued until mice show signs of lethargy, abdominal distension or weight loss at which time they are sacrificed. Successful excision-recombination events are confirmed in the pancreata of mice by detecting the presence of a single LoxP site [5]. |
别名 | NSC 613327, 吉西他滨, LY188011 |
化合物与蛋白结合的复合物 |
Drosophila melanogaster deoxyribonucleoside kinase successfully activates gemcitabine in transduced cancer cell lines |
分子量 | 263.2 |
分子式 | C9H11F2N3O4 |
CAS No. | 95058-81-4 |
store at low temperture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Ethanol: <1 mg/mL
DMSO: 15 mg/mL (56.99 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
bottom
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Gemcitabine 95058-81-4 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog DNA/RNA Synthesis inhibit LY 188011 NSC 613327 吉西他滨 LY-188011 LY188011 Inhibitor inhibitor