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Gemcitabine HCI
盐酸吉西他滨 /Gemcitabine HCI
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货号：A309564
同义名：
吉西他滨盐酸盐
/ LY 188011 hydrochloride;Gemcitabine(hydrochloride)
Gemcitabine HCI (LY 188011 Hydrochloride) 是一种嘧啶核苷类 似物抗代谢物和抗肿瘤 剂，通过抑制 DNA 合成和修复，导致自噬 和细胞凋亡 。
Gemcitabine HCI 化学结构
Gemcitabine HCI 3D分子结构
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Gemcitabine HCI 纯度/质量文件 产品仅供科研
货号：A309564
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产品说明书
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Gemcitabine HCI 质控信息
Gemcitabine HCI 生物活性
描述
Gemcitabine hydrochloride is the hydrochloride form of Gemcitabine. Gemcitabine (dFdCTP, LY-188011, NSC 613327, (+)-2'-Deoxy-2',2'-difluorocytidine) is a deoxycytidine analogue that has a spectrum of activity against solid tumors[1] [2] [3] [4] [4] [6]
作用机制
Gemcitabine, as nucleoside analogue, can inhibit DNA synthesis through inhibition of ribonucleotide reductase and incorporation into DNA.[2] [3]
Gemcitabine HCI 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
CCRF-CEM
Growth Inhibition Assay
IC50=2.9 ± 1.8 nM
22425885
CCRF-CEM
Growth Inhibition Assay
IC50=2.9 ± 1.8 nM
22425885
CCRF-CEM
Growth Inhibition Assay
72 h
IC50=2.0 ± 0.6 nM
21851843
CCRF-CEM/dCK−/−
Growth Inhibition Assay
IC50=240.4 ± 29.0 μM
22425885
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Gemcitabine HCI 动物研究
Dose
Mice: 0.15 mg/kg - 300 mg/kg[7] [8] [9]
Administration
i.v., p.o.
Pharmacokinetics
Animal
Dogs[8]
Dose
30 mg/kg
Administration
i.v.
MRT
2.22 ± 0.388 h
t1/2β
3.23 ± 1.03 h
AUC
61.7 ± 6.35 mg·h/L
CL
0.492 ± 0.0538 L/h·kg
Vss
1.08 ± 0.154 L/kg
Gemcitabine HCI 参考文献
[1] Hertel LW, Boder GB, et al. Evaluation of the antitumor activity of gemcitabine (2',2'-difluoro-2'-deoxycytidine). Cancer Res. 1990 Jul 15;50(14):4417-22.
[2] Pereira S, Fernandes PA, et al. Mechanism for ribonucleotide reductase inactivation by the anticancer drug gemcitabine. J Comput Chem. 2004 Jul 30;25(10):1286-94.
[3] Heinemann V, Xu YZ, et al. Cellular elimination of 2',2'-difluorodeoxycytidine 5'-triphosphate: a mechanism of self-potentiation. Cancer Res. 1992 Feb 1;52(3):533-9.
[4] Huang P, Chubb S, et al. Action of 2',2'-difluorodeoxycytidine on DNA synthesis. Cancer Res. 1991 Nov 15;51(22):6110-7.
[5] Huang P, Chubb S, et al. Action of 2',2'-difluorodeoxycytidine on DNA synthesis. Cancer Res. 1991 Nov 15;51(22):6110-7.
[6] Shi Z, Azuma A, et al. S-Phase arrest by nucleoside analogues and abrogation of survival without cell cycle progression by 7-hydroxystaurosporine. Cancer Res. 2001 Feb 1;61(3):1065-72.
[7] Turk J, Bemis K, et al. General pharmacology of gemcitabine hydrochloride in animals. Arzneimittelforschung. 1994 Sep;44(9):1089-92.
[8] Freise KJ, Martín-Jiménez T, et al. Pharmacokinetics of gemcitabine and its primary metabolite in dogs after intravenous bolus dosing and its in vitro pharmacodynamics. J Vet Pharmacol Ther. 2006 Apr;29(2):137-45.
[9] Gemcitabine
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Gemcitabine HCI 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
3.34mL
0.67mL
0.33mL
16.69mL
3.34mL
1.67mL
33.37mL
6.67mL
3.34mL
Gemcitabine HCI 技术信息
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