Gemcitabine

规格	价格/CNY		数量
50 mg	￥ 423	现货
100 mg	￥ 592	现货
200 mg	￥ 898	现货
500 mg	￥ 1,681	现货
1 g	￥ 2,570	现货
1 mL * 10 mM (in DMSO)	￥ 134	现货

规格

价格/CNY

货期

数量

50 mg

￥ 423

现货

100 mg

￥ 592

现货

200 mg

￥ 898

现货

500 mg

￥ 1,681

现货

1 g

￥ 2,570

现货

1 mL * 10 mM (in DMSO)

￥ 134

现货

存储

store at low temperature,keep away from direct sunlight　|　Powder: -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)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.7994 mL	18.997 mL	37.9939 mL	94.9848 mL
	5 mM	0.7599 mL	3.7994 mL	7.5988 mL	18.997 mL
	10 mM	0.3799 mL	1.8997 mL	3.7994 mL	9.4985 mL
	20 mM	0.19 mL	0.9498 mL	1.8997 mL	4.7492 mL
	50 mM	0.076 mL	0.3799 mL	0.7599 mL	1.8997 mL

产品描述	Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.
靶点活性	BxPC-3 cells:18nM, Capan-2 cells:12 nM, MIAPaCa2:40nM
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]
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].

别名	吉西他滨, NSC 613327, LY188011
化合物与蛋白结合的复合物	Drosophila melanogaster deoxyribonucleoside kinase successfully activates gemcitabine in transduced cancer cell lines
分子量	263.2
分子式	C9H11F2N3O4
CAS No.	95058-81-4

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