Gemcitabine, Hydrochloride Salt(盐酸吉西他滨),是吉西他滨的盐酸盐形式,又称为LY-188011、NSC 613327、Gemzar®等。Gemcitabine是deoxycytidine的核苷类似物,进入细胞后即被核苷激酶活化为 gemcitabine二磷酸(dFdCDP)和gemcitabine三磷酸(dFdCTP),dFdCDP抑制核糖核苷酸还原酶,从而抑制DNA合成;dFdCTP插入到正在复制的DNA链中,终止DNA链延伸,从而抑制DNA合成,并诱导细胞凋亡,表现出细胞毒性作用。
Gemcitabine已经被批准用于治疗多种癌症,包括卵巢癌,乳腺癌,非小细胞肺癌,肺癌和胰腺癌。其他药物,如carboplatin,paclitaxel和DMAPT,与gemcitabine共同使用时具有协同抗肿瘤作用,因此,被用来联合治疗多种癌症。
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参考文献
[1] Plunkett W, et al. Gemcitabine: metabolism, mechanisms of action, and self-potentiation. Seminars in Oncology 22:3-10(1995).
[2] Oettle H, et al. Adjuvant chemotherapy with gemcitabine vs observation in patients under-going curative-intent resection of pancreatic cancer: a randomized controlled trial. Journal of the American Medical Association 297 (3): 267–277(2007).
[3] Matthews DJ, et al. Pharmacological Abrogation of S-Phase Checkpoint Enhances the Anti-Tumor Activity of Gemcitabine In Vivo. Cell Cycle 6: 104-110(2007).
[4] RamachandranC, et al. Potentiation of gemcitabine by Turmeric Force™ in pancreatic cancer cell lines. ONCOLOGY REPORTS 23: 1529-1535(2010).
[5] Holcomb BK, et al. DimethylaminoParthenolide Enhances the Inhibitory Effects of Gemcitabine in Human Pancreatic Cancer Cells. J Gastrointest Surg. 16: 1333-1340(2012).
[6] Lee JJ, et al. Predictive Modeling of In Vivo Response to Gemcitabine in Pancreatic Cancer. PLoSComputBiol 9(9): e1003231 (2013).
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