Gemcitabine

95058-81-4

C9H11F2N3O4

DMSO : >= 103.3 mg/mL (392.48 mM)

Cell Cycle/DNA Damage; Cell Cycle/DNA Damage; Autophagy

Gemcitabine (NSC 613327; LY188011) is a DNA synthesis inhibitor which inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC₅₀s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively. IC50 & Target: DNA synthesis^[1] In Vitro: MTS assay demonstrates that Gemcitabine at 15 nM, indole-3-carbinol (I3C) at 50 uM and the combination does not affect hTERT-HPNE cell viability. However, treatment with Gemcitabine at 15 nM, I3C at 50 uM and the combination results in 31%, 19% and 72% cell death of BxPC-3 cells, respectively^[1]. In Vivo: Treatment of the LSL-Kras^G12D/+; LSL-Trp53^R172H; Pdx-1-Cre mice with either Gemcitabine (50 mg/kg, i.p.) or the combination DMAPT/Gemcitabine significantly increased the median survival time by more than 30 days compared to the placebo group (254.5 [P=0.015] or 255 days [P=0.018] vs. 217.5 days, respectively)^[2]. Gemcitabine can be administered via endotracheal spray in rats without marked toxicity with a maximum tolerated dose of 4 mg/kg once a week for 9 weeks. The toxicity of Gemcitabine is lower via lung than oral administration at dosages of 2, 4, and 6 mg/kg^[3].