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product name Gemcitabine HCl


Description: Gemcitabine hydrochloride (also known as LY188011) is a DNA synthesis inhibitor. 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; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. 

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



Molecular Weight (MW)

299.66
Formula

C9H11F2N3O4.HCI
CAS No.

122111-03-9
Storage

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

DMSO: <1 mg/mL
Water: 19 mg/mL (63.4 mM)
Ethanol: <1 mg/mL (slightly soluble or insoluble)
Solubility (In vivo)

Saline: 20 mg/mL

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19396143

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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