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发布者：信康 浏览次数：
产品名称:N/ACAS:180977-34-8别名：英文名：FTI 277 HYDROCHLORIDE
- 储存条件 −20°C
- 溶解度 H2O: soluble
- 形态amorphous semi-solid
- 生物活性FTI 277 HCl是FTI 277的甲酯，是一种有效的选择性farnesyltransferase (FTase)抑制剂，IC50为500 pM，选择性比密切相关的GGTase I 高100倍。
- 体外研究FTI-277 inhibits Ras processing with an IC50 of 100 nM, but not the geranylgeranylated Rap1A processing in whole cells. FTI-277 induces accumulation of cytoplasmic non-farnesylated H-Ras, accumulates inactive Ras/Raf complexes in the cytoplasm, and blocks constitutive MAPK activation in H-RasF cells. FTI-277 causes increased apoptosis after irradiation and increases radiosensitivity in H-ras-transformed rat embryo cells. FTI-277 also inhibits cell growth and induces apoptosis in drug-resistant myeloma tumor cells. In SH-SY5Y cells, FTI-277 diminishes the toxic effects of methamphetamine on induction in cell degeneration, activation in c-Jun-N-terminal kinase cascades, and Ras activation.
- 体内研究In mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d i.p.) effectively clears HDV viremia.
