Name | FTI-277 (hydrochloride) |
Synonyms | FTI 277 CS-1757 FTI 277 HCl FTI 277 HCL FTI 277 HYDROCHLORIDE FTI-277 (hydrochloride) FTI-277 TRIFLUOROACETATE SALT 4-[2(R)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(S)-methionine methyl ester hydrochloride (S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate FTI 277 HCl |
CAS | 180977-34-8 |
EINECS | 604-604-1 |
Molecular Formula | C22H30ClN3O3S2 |
Molar Mass | 484.075 |
Solubility | DMSO: ≥ 4.7 mg/mL |
Appearance | amorphous semi-solid |
Storage Condition | Inert atmosphere,2-8°C |
In vitro study | 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 diages the toxic effects of methomorphetamine on induction in cell degeneration, activation in c-Jun-N-terminal kinase cascades, and Ras activation. FTI-277 inhibited Ras processing with an IC50 of 100 nM, but did not inhibit tetra-isoprenated Rap1A processing in whole cells. FTI-277 induces accumulation of cytoplasmic farnesylation H-Ras, accumulation of inactive Ras/Raf in the cytoplasm, and blocking constitutive MAPK activation in H-RasF cells. FTI-277 causes an increase in apoptosis after radiation and increases the radiosensitivity of H-ras transformed rat embryonic cells. In drug-resistant myeloma cells, FTI-277 also inhibit cell growth and induce apoptosis. In SH-SY5 cells, FTI-277 reduced cell degeneration, activation, c-Jun-N-terminal kinase cascade and methamphetamine-induced toxic effects during Ras activation. |
In vivo study | In mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d I. p.) effective clears HDV viremia. in mice infected with hepatitis B Virus (HBV) and HDV, FTI-277 (50 mg/kg/d I. p.) HDV Virus was effectively cleared. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.066 ml | 10.329 ml | 20.658 ml |
5 mM | 0.413 ml | 2.066 ml | 4.132 ml |
10 mM | 0.207 ml | 1.033 ml | 2.066 ml |
5 mM | 0.041 ml | 0.207 ml | 0.413 ml |