Gemcitabine (Hydrochloride) | CAS:122111-03-9

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Name:Gemcitabine Hydrochloride; LY 188011 hydrochloride
Cat. No. :CS-0755
CAS No. :122111-03-9
Formula:C9H12ClF2N3O4
M. Wt. : 299.66
Solubility:H2O: ≥ 66.66 mg/mL

Gemcitabine hydrochloride is a DNA synthesis inhibitor with IC50 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.IC50 & Target: DNA synthesis[1]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].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 (p10) and 100 mg/kg is considered as the maximal tolerated dose, which does not cause any mortality and a minimal body weight loss[3].

Reddy LH, et al. Preclinical toxicology (subacute and acute) and efficacy of a new squalenoyl Gemcitabine anticancernanomedicine. J Pharmacol Exp Ther. 2008 May;325(2):484-90. Wang H, et al. Enhanced efficacy of Gemcitabine by indole-3-carbinol in pancreatic cell lines: the role of human equilibrativenucleoside transporter 1. Anticancer Res. 2011 Oct;31(10):3171-80. Joshi G, et al. Enhanced bioavailability and intestinal uptake of Gemcitabine HCl loaded PLGA nanoparticles after oral delivery. Eur J Pharm Sci. 2014 Aug 18;60:80-9.