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Gemcitabine HCl (Gemzar,LY188011)

  Cat. No.:  DC2107   Featured
Chemical Structure
122111-03-9
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Field of application
Gemcitabine Hydrochloride (Gemzar) 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,showed potent activity against COVID-19(SARS-COV-2) with EC50 MERS-COV(1.216), SARS-COV(4.9
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 122111-03-9
Chemical Name: 4-amino-1-((2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one hydrochloride
Synonyms: LY188011; LY-188011; LY 188011; Abbreviations: dFdC; dFdCyd; gemcitabine; Gemzar.
SMILES: C1=CN(C(=O)N=C1N)[C@H]2C([C@@H]([C@H](O2)CO)O)(F)F.Cl
Formula: C9H12ClF2N3O4
M.Wt: 299.66
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Gemcitabine hydrochloride is a DNA synthesis inhibitor with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM in BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells, respectively.
In Vivo: The aim of study is to formulate PLGA nanoparticles (NPs) of Gemcitabine Hydrochloride (Gemcitabine HCl) for enhanced oral bioavailability via absorption through M cells of Peyer’s patches. Gemcitabine HCl is available as i.v. infusion due to its short half life (8-17 min), rapid metabolism and limited tumor uptake. Gemcitabine loaded PLGA NPs shows 21.47-fold increase in relative bioavailability in comparison to plain drug solution after oral delivery[2]. After i.v. injection of Gemcitabine at doses of 50, 100, and 120, and 300 mg/kg, the highest dose caused considerable body weight loss (p<0.05 at all the time points evaluated, starting from day 3 of first injection) compared with that of the untreated group and complete mortality, whereas 120 mg/kg is determined as the lethal dose 10% (LD10) and 100 mg/kg is considered as the maximal tolerated dose, which does not cause any mortality and a minimal body weight loss[3].
In Vitro: MTS assay demonstrates that Gemcitabine at 15 nM, indole-3-carbinol (I3C) at 50 μM and the combination does not affect hTERT-HPNE cell viability. However, treatment with Gemcitabine at 15 nM, I3C at 50 μM and the combination results in 31%, 19% and 72% cell death of BxPC-3 cells, respectively[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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