Gemcitabine  别名：NSC 613327; LY188011; 吉西他滨

Gemcitabine (吉西他滨; LY-188011; NSC 613327) 是DNA合成抑制剂，对PANC1，MIAPaCa2，BxPC3和Capan2细胞的IC50分别为50 nM，40 nM，18 nM和12 nM。Gemcitabine 抑制 DNA 合成 (DNA synthesis) 和修复，导致细胞自噬 (autophagy) 和凋亡 (apoptosis)。

Gemcitabine对Pan02小鼠胰腺癌细胞的IC50为 0.3 uM (https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8268835/)。

Experimental protocol

After 1 week of implantation, mice were randomized into the following treatment groups (n = 6) based on the bioluminescence measured after the first IVIS imaging: (a) untreated control (olive oil, 100 uL daily); (b) curcumin alone (1 g/kg), once daily p.o.; (c) gemcitabine alone (25 mg/kg), twice weekly by i.p. injection; and (d) combination of curcumin (1 g/kg), once daily p.o., and gemcitabine (25 mg/kg), twice weekly by i.p. injection. Tumor volumes were monitored weekly by the bioluminescence IVIS Imaging System 200 using a cryogenically cooled imaging system coupled to a data acquisition computer running Living Image software (Xenogen Corp., Alameda, CA).

Animal models to evaluate effects of gemcitabine on Gr-1⁺/CD11b⁺ immune suppressor cells in vivo
One million tumor cells were inoculated s.c. on one flank of C57Bl/6 or BALB/c mice. When tumors reached a minimal volume of 700 to 1,000 mm³, mice were injected i.p. with a single dose of 120 mg/kg of gemcitabine diluted in saline. Control mice received saline alone.

LSL-Kras^G12D/+; LSL-Trp53^R172H; Pdx-1-Cre mouse model

At 1 month of age, LSL-Kras^G12D/+; LSL-Trp53^R172H; Pdx-1-Cre mice were randomized into treatment groups (placebo, DMAPT, gemcitabine, DMAPT/gemcitabine). Placebo (vehicle = hydroxylpropyl methylcellulose, 0.2% Tween 80 [HPMT]) and DMAPT (40 mg/kg body weight in HPMT) were administered by oral gastric lavage once daily. Gemcitabine (50 mg/kg body weight in PBS) was administered by intraperitoneal injection twice weekly. Mouse weight was monitored weekly. Treatment was continued until mice showed signs of lethargy, abdominal distension or weight loss at which time they were sacrificed. Successful excision-recombination events were confirmed in the pancreata of mice by detecting the presence of a single LoxP site.

AbMole has not independently confirmed the accuracy of these methods. They are for reference only.