Name: Gemcitabine hydrochloride
Brand: TargetMol
SKU: T6069
Price: 223 CNY
Availability: InStock
Rating: 5 (10 reviews)

Gemcitabine hydrochloride

很棒

产品编号 T6069Cas号 122111-03-9

别名 吉西他滨盐酸盐, LY 188011 hydrochloride, Gemzar, Gemcitabine HCl

Gemcitabine hydrochloride (LY 188011 hydrochloride) 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。

规格

价格

库存

数量

25 mg

¥ 287

In stock

50 mg

¥ 397

In stock

100 mg

¥ 597

In stock

200 mg

¥ 897

In stock

500 mg

¥ 1,630

In stock

1 g

¥ 2,530

In stock

1 mL x 10 mM (in DMSO)

¥ 223

In stock

产品介绍

生物活性

产品描述	Gemcitabine hydrochloride (LY 188011 hydrochloride) 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	DNA synthesis (PL-45 cells):89.3 nM, DNA synthesis (Capan2 cells):12 nM, DNA synthesis (BxPC-3 cells):18 nM, DNA synthesis (Mia Paca-2 cells):40 nM, DNA synthesis (PANC-1 cells):92.7 nM
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 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (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	吉西他滨盐酸盐, LY 188011 hydrochloride, Gemzar, Gemcitabine HCl

化学信息

分子量	299.66
分子式	C₉H₁₁F₂N₃O₄·HCl
CAS No.	122111-03-9
Smiles	Cl.Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)C2(F)F)c(=O)n1
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

H2O: 30 mg/mL (100.11 mM), Sonication is recommended.

DMSO: 81.7 mg/mL (272.64 mM), Sonication is recommended.

溶液配制表

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.3371 mL	16.6856 mL	33.3712 mL	166.8558 mL
5 mM	0.6674 mL	3.3371 mL	6.6742 mL	33.3712 mL
10 mM	0.3337 mL	1.6686 mL	3.3371 mL	16.6856 mL
20 mM	0.1669 mL	0.8343 mL	1.6686 mL	8.3428 mL
50 mM	0.0667 mL	0.3337 mL	0.6674 mL	3.3371 mL
100 mM	0.0334 mL	0.1669 mL	0.3337 mL	1.6686 mL

体内实验配液计算器