吉西他滨 Gemcitabine

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上海伟进生物科技有限公司
18930085161 021-54960076
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Last Updated 2025-08-12 19:55

吉西他滨 Gemcitabine

产品描述 Gemcitabine (同义名:吉西他滨, LY 188011; NSC 613327; Zefei; LY188011; LY-188011) 是 deoxycytidine 的核苷类似物,抑制 PANC1, MIAPaCa2, BxPC3 and Capan2I增殖的 C50分别为 50 nM, 40 nM, 18 nM 和 12 nM。作为药物前体进入细胞后被核苷激酶活化为 gemcitabine二磷酸 (dFdCDP)和 gemcitabine三磷酸 (dFdCTP)。 Gemcitabine插入到正在复制的 DNA链中,使 DNA链终止延伸,从而抑制 DNA合成以及随后的细胞凋亡 [1]。在 BxPC-3, PANC-1和 MIA PaCa-2细胞中, gemcitabine激活 NF-κB,并降低 BxPC-3和 PANC-1细胞中的 IκBα水平 [2]。 Gemcitabine是第一批广泛用于胰腺癌治疗的抗肿瘤药物,能显著延迟完全切除胰腺癌病人的复发 [3]。 Gemcitabine还被用于其他癌症如非小细胞肺癌,膀胱癌和乳腺癌病人的治疗。另外, gemcitabine与 dimethylamino parthenolide (DMAPT) [2], EXEL‑9844 [4]和 Turmeric Force™(TF) [5]等药物联合作用表现出协同抗肿瘤作用。 靶点 化学特性
Cas No.: 95058-81-4 分子量 : 263.20
分子式 : C9H11F2N3O4 纯度 : >99 %
同义名 : LY 188011; NSC 613327; Zefei; LY188011; LY-188011
化学名 : 3-Pyridinecarboxamide, 4-amino-1-[3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
外观 : 白色至浅黄色固体
溶解 : 溶于 DMSO (up to 100 mg/ml)
保存: 2 年 -20 ℃ 固体
储存液配制
储存液 (1 ml DMSO 体系 ) 1 mM 5 mM 10 mM
质量 (mg) 0.2632 1.3160 2.6320
结构式
使用浓度 ( 仅作参考 )
Gemcitabine 的具体使用浓度请参考相关文献,并根据自身实验条件(如实验目的,细胞种类,培养特性等)进行摸索和优化。
参考文献
[1] Plunkett W,et al. Preclinical characteristics of gemcitabine. Anticancer Drugs. 6:7-13(1995).
[2]Holcomb BK, et al. Dimethylamino parthenolide enhances the inhibitory effects of gemcitabine in human pancreatic cancer cells. J Gastrointest Surg. 16(7):1333-40(2012).
[3]Chen SH, et al. Gemcitabine-induced pancreatic cancer cell death is associated with MST1/cyclophilin D mitochondrial complexation. Biochimie. 103:71-9(2014).
[4]Matthews DJ, et al. Pharmacological abrogation of S-phase checkpoint enhances the anti-tumor activity of gemcitabine in vivo. Cell Cycle. 6(1):104-10(2007).
[5] Ramachandran C, et al. Potentiation of gemcitabine by Turmeric Force in pancreatic cancer cell lines.Oncol Rep. 23(6):1529-35(2010).
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