Gemcitabine

产品编号: T0251 别名:

NSC 613327,吉西他滨,LY188011

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。

陶术生物的所有产品和服务仅用于科学研究，我们不为任何个人用途提供产品和服务。

CAS：95058-81-4

规格	库存	价格/RMB	数量
{{item.packagingtext}}	{{item.goodshuoqi}}	{{item.moneyunit}} {{item.finalprice}} {{item.pricetext==null\|\|item.pricetext==''?pricetext:item.pricetext}}

生物活性化学信息储存和溶解度信息参考文献引用文献

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.

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].

Cas No.

95058-81-4

分子式

C9H11F2N3O4

分子量

263.201

别名

NSC 613327;吉西他滨;LY188011;Gemcitabine

参考文献

[1]Wang H, et al. Enhanced efficacy of Gemcitabine by indole-3-carbinol in pancreatic cell lines: the role of human equilibrativenucleoside transporter 1. Anticancer Res. 2011 Oct;31(10):3171-80.[2]Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination[J]. Antiviral Research. 2020: 104931 [3]Wang Y, et al. Licoricidin enhances gemcitabine-induced cytotoxicity in osteosarcoma cells by suppressing the Akt and NF-κB signal pathways. Chem Biol Interact. 2018 May 18;290:44-51.[4]Chang Z, Zhang Y, Liu J, et al. GATA1 Promotes Gemcitabine Resistance in Pancreatic Cancer through Antiapoptotic Pathway[J]. Journal of Oncology. 2019 Apr 10;2019:9474273.[5]Liu L, Liu S, Deng P, et al. Targeting the IRAK1-S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma[J]. Cancer Research.[6]Yip-Schneider MT, et al. Dimethylaminoparthenolide and Gemcitabine: a survival study using a genetically engineered mouse model of pancreatic cancer. BMC Cancer. 2013 Apr 17;13:194.[7]Wu HM, et al. Gemcitabine-Induced Autophagy Protects Human Lung Cancer Cells from Apoptotic Death. Lung. 2016 Dec;194(6):959-966. Epub 2016 Sep 7.[8]Lou M, et al. Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. J Biol Chem. 2017 Jun 2;292(22):9136-9149.[9]Gagnadoux F, et al. Safety of pulmonary administration of gemcitabine in rats. J Aerosol Med. 2005 Summer;18(2):198-206 [10]Ross DD, et al. Molecular effects of 2',2'-difluorodeoxycytidine (Gemcitabine) on DNA replication in intact HL-60 cells. Biochem Pharmacol. 1994 Oct 18;48(8):1619-30.

引用文献

[1]Shi Y H, Xu Q C, Zhu Y Q, et al. Imatinib facilitates gemcitabine sensitivity by targeting epigenetically activated PDGFC signaling in pancreatic cancer. Molecular Therapy. 2022 [2]Liu L, Liu S, Deng P, et al. Targeting the IRAK1-S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma. Cancer Research. 2021 Mar 1;81(5):1413-1425. doi: 10.1158/0008-5472.CAN-20-2125. Epub 2021 Jan 5.[3]Liu L, Liu S, Deng P, et al. Targeting the IRAK1–S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma. Cancer Research. 2021, 81(5): 1413-1425.[4]Sun Y, Ren D, Zhou Y, et al. Histone acetyltransferase 1 promotes gemcitabine resistance by regulating the PVT1/EZH2 complex in pancreatic cancer. Cell Death & Disease. 2021, 12(10): 1-13.[5]Chang Z, Zhang Y, Liu J, et al. GATA1 Promotes Gemcitabine Resistance in Pancreatic Cancer through Antiapoptotic Pathway. Journal of Oncology. 2019 Apr 10;2019:9474273 [6]Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination. Antiviral Research. 2020: 104931 [7]Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9

储存和溶解度

Ethanol:<1 mg/mL
DMSO:15 mg/mL (56.99 mM)
store at low temperture,keep away from direct sunlight
Powder: -20°C for 3 years
In solvent: -80°C f

剂量换算 Gemcitabine 95058-81-4

对于各种应用，安全且有效的用药剂量是很有必要的了解更多

体内实验配液计算器

第一步：请输入动物实验的基本信息

剂量 mg/kg

每只动物体重 g

给药体积 ul

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO +

% +

% Tween 80 +

% ddH₂O

% DMSO +

重置计算

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

计算器

摩尔计算器可以帮助您计算

制备已知体积和浓度溶液所需的化合物质量
将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

质量

浓度

体积

分子量

重置计算

稀释计算器可以帮助您计算

制备已知体积和浓度溶液所需的化合物质量
将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

浓度（起始）

体积（起始）

浓度（终点）

体积（终点）

重置计算

配液计算器可以帮助您计算

重组计算器可帮助您快速计算试剂的体积，以重组您的小瓶。

溶液体积

质量

配液浓度

重置计算

配液计算器可以帮助您计算

输入化合物的化学式以计算其摩尔质量和元素组成
提示：化学式需区分大小写

分子结构式

总分子量

g/mol

重置计算

技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

inhibit LY 188011 NSC 613327 吉西他滨 LY-188011 Autophagy LY188011 Nucleoside Antimetabolite/Analog Inhibitor DNA/RNA Synthesis Gemcitabine Apoptosis 95058-81-4

Gemcitabine 相关推荐

相关化合物库推荐该产品包含在如下化合物库中：

注册成功

Gemcitabine

NSC 613327,吉西他滨,LY188011

摩尔计算器可以帮助您计算

稀释计算器可以帮助您计算

配液计算器可以帮助您计算

配液计算器可以帮助您计算