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 NYKzNo51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DpT2lEPTB;Mj65JOKyKDFwODDuUS=> M1[welIzPDJ3OEi1
CCRF-CEM/dCK−/− NU\RdmFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJ2MD60JOKyKDJ7LkCg{txO NGPoblgzOjR{NUi4OS=>
L1210 wt MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzjTWM2OD1zLkOgxtEhOC5|IH7N NYP1Tmc2OjJ2MkW4PFU>
L1210 10K MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXuR21KSzVyPUKyMlIhyrFiMz63JO69VQ>? M1nuNFIzPDJ3OEi1
TC-1  Ml3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[5WYdXUUN3ME2xOE44KMLzIEKuPEBvVQ>? NXKxbWZbOjJ2MkW4PFU>
TC-1-GR MkLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLBTWM2OD1|Nj63JOKyKDVwMTFOwG0> MlGwNlI1OjV6OEW=
MIA PaCa-2 MlLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGr0NFZKSzVyPUS5MlchyrFiMUeuO{BvVQ>? MkPINlI1OjV6OEW=
PANC-1 NFXtcYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DkTmlEPTB;PjC0NFAh|ryP MV:yNlQzPTh6NR?=
CCRF-CEM MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfIZpdKSzVyPUKuPUDDuSBzLkigcm0> MlHXNlI1OjV6OEW=
CCRF-CEM-AraC-8C NX3XPGtWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TJSGlEPTB;OUm4MlghyrFiOT60JI5O NG\jUnUzOjR{NUi4OS=>
CCRF-CEM  NITqVpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlewO|IhcA>? M{PTVGlEPTB;Mj6wJOKyKDBwNjDuUS=> M{GzUVIyQDVzOESz

... 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 to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.
19mg/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
in solvent
Synonyms LY188011

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03422523 Recruiting Diffuse Large B Cell Lymphoma|Relapsed Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma University Hospital Southampton NHS Foundation Trust|Hoffmann-La Roche May 9 2018 Phase 2
NCT03579836 Recruiting Locally Advanced Pancreatic Cancer|Metastatic Pancreatic Cancer BeyondBio Inc. May 9 2018 Phase 1|Phase 2
NCT03449901 Recruiting Soft Tissue Sarcoma Washington University School of Medicine|Polaris Pharmaceuticals Inc. May 9 2018 Phase 2
NCT03432598 Recruiting Locally Advanced or Metastatic Lung Cancer BeiGene August 9 2017 Phase 2
NCT02181634 Completed Cholangiocarcinoma PrECOG LLC.|Celgene Corporation December 9 2014 Phase 2
NCT01924260 Active not recruiting Acinar Cell Adenocarcinoma of the Pancreas|Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer|Unspecified Adult Solid Tumor Protocol Specific University of California Davis|National Cancer Institute (NCI)|Takeda August 9 2013 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.

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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