| CAS NO: | 122111-03-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| Molecular Weight (MW) | 299.66 |
|---|---|
| Formula | C9H11F2N3O4.HCI |
| CAS No. | 122111-03-9; 95058-81-4 (free base); |
| 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 |
| Synonym | Abbreviations: dFdC; dFdCyd; LY188011; LY-188011; LY 188011; gemcitabine; Gemzar. Chemical Name: 4-amino-1-((2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one hydrochloride SMILES Code: O=C1N=C(N)C=CN1[C@@H]2O[C@H](CO)[C@@H](O)C2(F)F.[H]Cl |
| 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. 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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