Gemcitabine HCl

Catalog No.S1149 Synonyms: LY188011

Gemcitabine HCl Chemical Structure

Molecular Weight(MW): 299.66

Gemcitabine HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.

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4 Customer Reviews

  • 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.

    Nucleic Acids Res 2014 42(10), 6436-47. Gemcitabine HCl purchased from Selleck.

    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.

    Br J Cancer, 2017, 116(3):324-334. Gemcitabine HCl purchased from Selleck.

  •  

    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.

    Cancer Immunol Immunother 2013 62, 383–391. Gemcitabine HCl purchased from Selleck.

    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.

     

     

    Dr. Helen Sadik of Johns Hopkins University. Gemcitabine HCl purchased from Selleck.

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Biological Activity

Description Gemcitabine HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.
Features Gemcitabine has been used to treat pancreatic cancer and has demonstrated effective anti-tumor activity.
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CCRF-CEM MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEOzeIhKSzVyPUKuPUDDuSBzLkigcm0> MXeyNlQzPTh6NR?=
CCRF-CEM/dCK−/− NIHKWnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUeyRmt7UUN3ME2yOFAvPCEEsTCyPU4xKM7:TR?= NYftXXV3OjJ2MkW4PFU>
L1210 wt Mnz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFwMzFCtUAxNjNibl2= M3jjTVIzPDJ3OEi1
L1210 10K MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWe0e|V[UUN3ME2yNk4zKMLzIEOuO{DPxE1? MoTvNlI1OjV6OEW=
TC-1  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7OO5RRUUN3ME2xOE44KMLzIEKuPEBvVQ>? M1rm[VIzPDJ3OEi1
TC-1-GR NGTGN|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7zTWM2OD1|Nj63JOKyKDVwMTFOwG0> NFrmbXYzOjR{NUi4OS=>
MIA PaCa-2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPXWGNKSzVyPUS5MlchyrFiMUeuO{BvVQ>? MX[yNlQzPTh6NR?=
PANC-1 M{SwOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjnZ3JKSzVyPU6gOFAxKM7:TR?= M1rNXVIzPDJ3OEi1
CCRF-CEM MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PwUmlEPTB;Mj65JOKyKDFwODDuUS=> MUiyNlQzPTh6NR?=
CCRF-CEM-AraC-8C M4XRdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rmUGlEPTB;OUm4MlghyrFiOT60JI5O NHf2ZYQzOjR{NUi4OS=>
CCRF-CEM  NHH6XJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFy2e2o4OiCq NEHTSnRKSzVyPUKuNEDDuSByLk[gcm0> NH;ueYwzOTh3MUi0Ny=>

... Click to View More Cell Line Experimental Data

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]

Protocol

Cell Research:[2]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Athymic nude mice with MIA PaCa-2 cells
  • Formulation: Phosphate-buffered saline
  • Dosages: 50 mg/kg or 100 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro Water 19 mg/mL (63.4 mM)
DMSO Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
Saline
20 mg/mL

* 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.

Chemical Information

Molecular Weight 299.66
Formula

C9H11F2N3O4.HCI

CAS No. 122111-03-9
Storage powder
Synonyms LY188011

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02181634 Active, not recruiting Cholangiocarcinoma PrECOG, LLC.|Celgene Corporation December 9, 2014 Phase 2
NCT01535924 Recruiting Adult Lymphocyte Depletion Hodgkin Lymphoma|Adult Lymphocyte Predominant Hodgkin Lymphoma|Adult Mixed Cellularity Hodgkin Lymphoma|Adult Nodular Lymphocyte Predominant Hodgkin Lymphoma|Adult Nodular Sclerosis Hodgkin Lymphoma|Recurrent Adult Hodgkin Lymphoma Kristie Blum|Ohio State University Comprehensive Cancer Center February 9, 2012 Phase 1|Phase 2
NCT01285037 Recruiting Cancer Eli Lilly and Company September 9, 2009 Phase 1
NCT01828736 Completed Recurrent Bladder Cancer|Stage IV Bladder Cancer|Transitional Cell Carcinoma of the Bladder Association Pour La Recherche des Thérapeutiques Innovantes en Cancérologie|Roche Pharma AG February 9, 2004 Phase 2
NCT01352962 Active, not recruiting Urethral Neoplasms|Neoplasms, Urethral|Ureter Cancer|Cancer of the Urethra|Urethral Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 5, 2011 Phase 1
NCT03027284 Recruiting Advanced Cancer|Metastatic Cancer|Biliary Tract Carcinoma|Cholangiocarcinoma|Gall Bladder Carcinoma|Solid Tumor|Non-Hodgkins Lymphoma Eli Lilly and Company February 3, 2017 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    What’s the difference between S1714 and S1149 and which one is better?

  • Answer:

    They have the same biological activities. The free base(S1714) dissolves better in DMSO, and the hydrochloride (S1149) dissolves better in water.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID