Information FTI 277 HCl 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. FTI 277 HCl inhibits cell growth and induces apoptosis . FTI 277 HCl is effective in clearing HDV viremia. Targets FTase (Cell-free assay) 500 pM In vitro 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. In vivo In mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d i.p.) effectively clears HDV viremia. Cell Research(from reference) Cell lines：8226, U266, and H929 multiple myeloma cell lines Concentrations：~10 μM Incubation Time：96 hours
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FTI 277 HCl
Dangerous GoodsCAS number：180977-34-8 molecular formula：C22H30ClN3O3S2
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Specs
| Chinese alias | - | ||
| English alias | 4-[2(R)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(S)-methionine methyl ester hydrochloride | ||
| CAS number | 180977-34-8 | molecular formula | C22H30ClN3O3S2 |
| molecular weight | 484.07 g/mol | Exact mass | 10mM in DMSO |
| PSA | 120.000 Ų | logp | 2.897 |
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Safety information
Signal word：
Warning
Hazard Statement：
H302: 吞食有害 H410: 对水生生物有剧毒并具有长期持续影响 H372: 通过长时间或反复暴露对器官造成损害
Statement of Preventive Measures：
P273: 避免释放到环境中。 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。
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