盐酸吉西他滨
Gemcitabine Hydrochloride (Synonyms: Gemcitabine HCl; LY 188011 hydrochloride;NSC 613327 HCl)
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基本信息
中文名称盐酸吉西他滨
英文名称 Gemcitabine Hydrochloride (Synonyms: Gemcitabine HCl; LY 188011 hydrochloride;NSC 613327 HCl)
CAS号122111-03-9
分子式C₉H₁₂ClF₂N₃O₄
分子量299.66
外观White to off-white powder
储存条件 4°C, sealed storage, away from moisture and light
安全信息
产品详情

Gemcitabine is an active metabolite of the gemcitabine prodrugs NUC-1031   and gemcitabine elaidate   and a prodrug form of gemcitabine di- and triphosphates. Gemcitabine is phosphorylated by intracellular kinases to the intermediate metabolite gemcitabine monophosphate   and the active di- and triphosphate forms.It is cytotoxic to HepG2 hepatocellular carcinoma and A549 non-small cell lung cancer (NSCLC) cells (IC50s = 5.2 and 16 nM, respectively) and inhibits tumor growth in various breast, colon, lung, and pancreatic cancer mouse xenograft models. Gemcitabine (12 mg/kg) sensitizes tumors to antibodies targeting programmed cell death protein 1 (PD-1), decreases the number of tumor-infiltrating regulatory T cells (Tregs), and increases survival in an MC-38 syngeneic mouse model of colon carcinoma.  Formulations containing gemcitabine have been used in the treatment of cancer.
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