Gemcitabine hydrochloride
作者：齐岳
发布时间：2023-09-05
08:50:40
点击数：
产品名称：Gemcitabine hydrochloride
产品描述：
| 产品描述 | Gemcitabine is a DNA synthesis inhibitor (IC50s: 12, 18, 40, 92.7, 89.3 in Capan2, BxPC-3, Mia Paca-2, PANC-1, and PL-45 cells, respectively). |
| 靶点活性 | DNA synthesis (Capan2):12nM, DNA synthesis (PANC-1):92.7nM, DNA synthesis (PL-45 cells):89.3nM, DNA synthesis (Mia Paca-2):40nM, DNA synthesis (BxPC-3):18nM |
| 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 | LY 188011 hydrochloride, 吉西他滨盐酸盐, LY188011, Gemzar, Gemcitabine HCl, 盐酸吉西他滨 |
| 分子量 | 299.66 |
| 分子式 | C9H11F2N3O4·HCl |
| CAS No. | 122111-03-9 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: 30 mg/mL (100 mM)
DMSO: 6 mg/mL (20 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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