Gemcitabine (hydrochloride)

Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis^[1][2]. IC50 & Target:DNA synthesis^[1] In Vitro: Gemcitabine Hydrochloride (purchased from MedChem Express, 0.003-1 μM; 3 days) kills both mouse and human senescent cells effectively and potently^[4].
Gemcitabine Hydrochloride 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^[1].
In Vivo: Gemcitabine Hydrochloride 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^[2].
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 Hydrochloride significantly increases the median survival time by more than 30 days compared to the placebo group (254.5 or 255 days vs. 217.5 days, respectively)^[3].