FTI 277 HCl|cas 180977-34-8|DC Chemicals
FTI 277 HCl is the methyl ester of FTI 277, which is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I.
Product Name: FTI 277 HCl |Catalog Number: DC8421 | cas: 180977-34-8 | Other names: FTI277,FTI-277,FTI 277 | Chemical name:4-[2(R)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(S)-methionine methyl ester hydrochloride | Molecule Formula: C22H30ClN3O3S2 | MW: 484.07
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. [1] FTI-277 causes increased apoptosis after irradiation and increases radiosensitivity in H-ras-transformed rat embryo cells. [2] FTI-277 also inhibits cell growth and induces apoptosis in drug-resistant myeloma tumor cells. [3] 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. [4]In mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d i.p.) effectively clears HDV viremia.
For research and scientific purpose only, not for human use.
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