Gemcitabine HCl

Catalog No.S1149 Batch:S114909

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Technical Data

Formula

C9H11F2N3O4.HCI
Molecular Weight 299.66 CAS No. 122111-03-9
Solubility (25°C)* In vitro Water 59 mg/mL (196.88 mM)
DMSO Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Gemcitabine is a pyrimidine nucleoside analog antitumor drug that can inhibit DNA synthesis and repair, leading to cell autophagy and apoptosis. It is mainly used to treat various solid tumors such as pancreatic cancer and non-small cell lung cancer, and is often combined with chemotherapy to enhance efficacy.
Targets
DNA synthesis (Capan2 cells) [1] DNA synthesis (BxPC3 cells) [1] DNA synthesis (MIAPaCa2 cells) [1] DNA synthesis (PANC1 cells) [1]
12 nM 18 nM 40 nM 50 nM
In vitro Gemcitabine induced NF-κB activity in BxPC-3, PANC-1, and MIA PaCa-2 cells and decreased the level of the NF-κB inhibitor IκBα in BxPC-3 and PANC-1 cells. Treatment of BxPC-3 cells with low dose Gemcitabine for 48 hours results in a dose-dependent increase in NF-κB binding. In contrast, NF-κB DNA binding is decreased in BxPC-3 cells treated with the higher Gemcitabine doses for 48 h; however, 24-h treatment with these higher doses increases NF-κB binding in BxPC-3 cells [2]
In vivo Intratumoral NF-κB activity is significantly elevated (1.3- to 1.8-fold) in the Gemcitabine-treated mice compared to the PBS-treated mice, suggesting that Gemcitabine also induces NF-κB activation. [2]
Features Gemcitabine has been used to treat pancreatic cancer and has demonstrated effective anti-tumor activity.

Protocol (from reference)

Cell Assay:[2]
  • Cell lines

    BxPC-3, MIA PaCa-2, and PANC-1 cells

  • Concentrations

    0.2 μM

  • Incubation Time

    24 hours or 48 hours

  • Method

    BxPC-3, MIA PaCa-2, and PANC-1 cells are seeded in a 96-well plate. After 24 hours, cells are treated with vehicle, DMAPT and/or Gemcitabine for an additional 24 hours or 48 hours. Apoptosis is quantified using the Cell Death Detection ELISA to detect the amount of cytoplasmic histone-associated DNA fragments and expressed relative to vehicle-treated cells.
Animal Study:[2]
  • Animal Models

    Athymic nude mice with MIA PaCa-2 cells

  • Dosages

    50 mg/kg or 100 mg/kg

  • Administration

    Administered via i.p.

References

  • https://pubmed.ncbi.nlm.nih.gov/12138244/
  • https://pubmed.ncbi.nlm.nih.gov/22618517/
  • https://pubmed.ncbi.nlm.nih.gov/22590527/

Customer Product Validation

<p>RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um.</p>

Data from [ Nucleic Acids Res , 2014 , 42(10), 6436-47 ]

<p> </p><p>Injection of low-dose GEM suppresses tumor growth in vivo. BALB/c mice were injected s.c. with 5x 10^5 CT26 cells into the right flank. On day 10, mice were injected i.p. with GEM (50 or 100 mg/kg). Arrows indicate the injection of GEM. Tumor size(mm2) was measured twice weekly. Each group consisted of five or six mice, and lines represent tumor growth in each mouse. The mean ± SD of the results on day 30 after tumor inoculation are also shown. Similar results were obtained in two experiments. *P\0.05 indicates statistical significance by ANOVA with Dunnett’s post hoc test. NS, not significant.</p>

Data from [ Cancer Immunol Immunother , 2013 , 62, 383–391 ]

<p>Cells were seeded in 96 well paltes, and then treated with the indicated concentration of Gemcitabine for 48 h. Cell survival was measured by a standarad MTT assay.</p><div><div> </div></div><p> </p>

, , Dr. Helen Sadik of Johns Hopkins University

Analysis of CD31-positive staining in EMT-6 tumour treated with anti-CTLA-4 therapies. (A)EMT-6/P tumours were implanted s.c. into female Balb/c mice. Tumour bearing mice were treated with (i.e. a repeat of the experiment shown in Figure 2) saline control, CTLA-4, metronomic CTX (ld CTX), gemcitabine (Gem), or CTLA-4 plus ld CTX, or CTLA-4 with sequential Gemcitabine. The experiment was terminated as the tumours were starting to respond to the different therapies, as assessed by caliper measurements. Tumours were resected, fixed, and then paraffin embedded, and 5μ sections were then stained (brown) for CD31 (black bar=100 μ). (B) Image analysis of × 20 pictures of CD31 immunohistochemistry of tumour tissues from control- and drug-treated groups of mice. The quantification of the images was performed by the image analysis software ImageJ (Image Processing and Analysis in Java; Wayne Rasband, Research Services Branch, National Institute of Mental Health, Bethesda, MD, USA) and the results are shown as the ratio between the CD31-positive area and the total area of the image. A one-way ANOVA analysis followed by Bartlett’s post test was applied to the results to demonstrate significant differences among the treatment groups. The statistical analysis of the data was performed with GraphPad Prism v.5.0. Blue lines, mean±s.d.; *P<0.05 vs control group.

Data from [ , , Br J Cancer, 2017, 116(3):324-334 ]

Selleck's Gemcitabine HCl Has Been Cited by 191 Publications

Macropinocytosis maintains CAF subtype identity under metabolic stress in pancreatic cancer [ Cancer Cell, 2025, S1535-6108(25)00271-5] PubMed: 40712568
Dynamic regulation of integrin β1 phosphorylation supports invasion of breast cancer cells [ Nat Cell Biol, 2025, 27(6):1021-1034] PubMed: 40419795
Senescence-associated lysosomal dysfunction impairs cystine deprivation-induced lipid peroxidation and ferroptosis [ Nat Commun, 2025, 16(1):6617] PubMed: 40731111
Pancreatic cancer-derived extracellular vesicles remodel the tumor microenvironment and enhance chemoresistance by delivering KRASG12D protein to cancer-associated fibroblasts [ Mol Ther, 2025, S1525-0016(25)00027-9] PubMed: 39810420
NIR pH-Responsive PEGylated PLGA Nanoparticles as Effective Phototoxic Agents in Resistant PDAC Cells [ Polymers (Basel), 2025, 17(8)1101] PubMed: 40284366
UPP1 enhances bladder cancer progression and gemcitabine resistance through AKT [ Int J Biol Sci, 2024, 20(4):1389-1409] PubMed: 38385072
A novel DDIT3 activator dehydroevodiamine effectively inhibits tumor growth and tumor cell stemness in pancreatic cancer [ Phytomedicine, 2024, 155377] PubMed: none
CCL3 predicts exceptional response to TGFβ inhibition in basal-like pancreatic cancer enriched in LIF-producing macrophages [ NPJ Precis Oncol, 2024, 8(1):246] PubMed: 39478186
Establishment, characterization, and biobanking of 36 pancreatic cancer organoids: prediction of metastasis in resectable pancreatic cancer [ Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5] PubMed: 38619751
Obg-like ATPase 1 exacerbated gemcitabine drug resistance of pancreatic cancer [ iScience, 2024, 27(6):110027] PubMed: 38883822

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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