吉西他滨 T0251

Product Introduction
Bioactivity


英文名: Gemcitabine

描述: Gemcitabine (LY188011) 是一种人工合成的胞嘧啶核苷衍生物，一种 DNA 合成抑制剂。Gemcitabine 具有抗肿瘤活性和抗代谢活性。Gemcitabine 可以引起细胞自噬和凋亡。

细胞实验: The cytotoxic effect of gemcitabine was evaluated with the MTT assay. SPC-A1 or A549 cells were treated with gemcitabine (0.05–500 lM) for 24 h. Then, 10 ll of MTT (5 mg/ml in PBS) was added to each well and incubated for 4 h at 37 C. Then, the formazan crystals were solubilized with 200 ll DMSO. The absorbance at 570 nm was measured using an automatic multiwell spectrophotometer. The experiment was repeated four times for each group [3].

动物实验: At 1 month of age, LSL-Kras G12D/+; LSL-Trp53 R172H; Pdx-1-Cre mice are 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) are administered by oral gastric lavage once daily. Gemcitabine (50 mg/kg body weight in PBS) is administered by intraperitoneal injection twice weekly. Mouse weight is monitored weekly. Treatment is continued until mice show signs of lethargy, abdominal distension or weight loss at which time they are sacrificed. Successful excision-recombination events are confirmed in the pancreata of mice by detecting the presence of a single LoxP site [5].

体外活性: 方法：PDAC 衍生成对原发性癌症细胞 (PCCs) PCC-1、PCC-2、PCC-5、PCC-6 和 PDAC 细胞 BxPC-3、 Mia PaCa-2、Panc-1 用 Gemcitabine (0.001-1000 µM) 处理 48 h，使用 MTT 方法检测细胞生长抑制情况。结果：Gemcitabine 剂量依赖性地抑制 PCC-1、PCC-2、PCC-5、PCC-6、BxPC-3、 Mia PaCa-2、Panc-1 细胞生长，IC50 分别为 1.2/0.3/1.2/4.3/4.2/7.9/10.5 µM。[1]方法：人胰腺癌细胞 PK-1 用 Gemcitabine (30 nM) 处理 24-48 h，使用 Flow Cytometry 方法检测细胞周期情况。结果：Gemcitabine 诱导 PK-1 细胞在 G0/G1 期的百分比增加，S 期及 G2/M 细胞比例下降。Gemcitabine 诱导 PK-1 细胞 S 期细胞周期停滞。[2]方法：人肺癌细胞 SPC-A1 和 A549 用 GFP 标记的 LC3 转染，24 h 后 加 Gemcitabine (5 μM) 孵育 24 h，使用共聚焦激光扫描显微镜检测 LC3 表达情况。 结果：LC3-II 的积累是自噬的标志。 Gemcitabine 显著增加了肿瘤细胞的 GFP-LC3 点，表明自噬水平提高。[3]

体内活性: 方法：为检测体内抗肿瘤活性，将 Gemcitabine (20 mg/kg) 腹腔注射给携带人高级别脑膜瘤肿瘤 HKBMM 的 BALB/cAJcl-nu/nu 小鼠，每周两次，持续四周。结果：Gemcitabine 治疗不仅抑制了肿瘤的发生，而且抑制了肿瘤生长。Gemcitabine 在体内阻断肿瘤细胞的细胞周期进程并促进细胞凋亡。Gemcitabine 通过细胞抑制和细胞毒性机制对高级别脑膜瘤发挥强大的抗肿瘤活性。[4]方法：为检测体内抗肿瘤活性，将 Gemcitabine (50 mg/kg/每周两次/腹腔注射) 和 DMAPT (40 mg/kg/天/灌胃) 给携带胰腺癌肿瘤的 LSL-KrasG12D/+; LSL-Trp53R172H; Pdx-1-Cre 突变小鼠。结果：Gemcitabine 或 DMAPT/Gemcitabine 组合显著提高了中位生存率 (254.5 或 255  天与 217.5 天)，并降低了胰腺腺癌的发生率和多样性。Gemcitabine 治疗增加了小鼠血浆中 IL-1α、IL-1β和IL-17的水平，而 DMAPT/Gemcitabine 降低了 IL-12p40、MCP-1、MIP-1β、eotaxin 和 TNF-α的水平，都是 κB 的靶基因。[5]

存储条件: store at low temperature,keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 15 mg/mL (56.99 mM)
5% DMSO+95% Saline : 0.75 mg/mL (2.85 mM)


关键字: inhibit | NSC-613327 | Autophagy | LY 188011 | Nucleoside Antimetabolite/Analog | Gemcitabine | Inhibitor | DNA/RNA Synthesis | Apoptosis | NSC613327 | LY-188011

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相关库: Drug Repurposing Compound Library | Drug-Fragment Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | DNA Damage & Repair Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途