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product name Gemcitabine


Description: Gemcitabine (also known as LY-188011, NSC 613327) 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. Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis.

Reference: Oncology. 2002;62(4):354-62; J Gastrointest Surg. 2012 Jul;16(7):1333-40.



Molecular Weight (MW)

263.2
Formula

C9H11F2N3O4
CAS No.

95058-81-4
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 15 mg/mL (57.0 mM)
Water: 16 mg/mL (60.8 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)

 

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19396142

In Vitro

In vitro activity: 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.

Kinase Assay: 

Cell Assay: 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.
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.
Animal model Athymic nude mice with MIA PaCa-2 cells
Formulation & Dosage Dissolved in PBS; 50 or 100 mg/kg; i.p. injection
References Oncology. 2002;62(4):354-62; J Gastrointest Surg. 2012 Jul;16(7):1333-40.

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