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Gemcitabine

产品编号 T0251 CAS 95058-81-4

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。

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Gemcitabine, CAS 95058-81-4

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其他形式的 Gemcitabine:

Gemcitabine hydrochloride
现货

选择批次

纯度: 100%

纯度: 99.67%

纯度: 99.62%

纯度: 99%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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

存储

store at low temperture,keep away from direct sunlight　|　Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

Ethanol: <1 mg/mL

DMSO: 15 mg/mL (56.99 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

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. 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. 3. 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. 4. Gagnadoux F, et al. Safety of pulmonary administration of gemcitabine in rats. J Aerosol Med. 2005 Summer;18(2):198-206 5. 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. 6. 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. 7. 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. 8. 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 9. 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. 10. Liu L, Liu S, Deng P, et al. Targeting the IRAK1-S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma[J]. Cancer Research.

文献引用

1. Li Y, Tang S, Shi X, et al.Metabolic classification suggests the GLUT1/ALDOB/G6PD axis as a therapeutic target in chemotherapy-resistant pancreatic cancer.Cell Reports Medicine.2023 2. 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 3. 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 4. 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. 5. 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. 6. 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 7. 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

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

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

给药体积

μL

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+

计算重置

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

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

bottom

技术支持

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。

Keywords

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

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Gemcitabine

存储

溶解度

参考文献

文献引用

相关产品

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剂量换算

体内实验配液计算器

计算器

输入分子式，点击计算，可计算出产品的分子量。

技术支持

Keywords