中文名 | FTI-277 (hydrochloride) |
英文名 | FTI-277 (hydrochloride) |
别名 | 法尼基转移酶FTASE抑制剂(FTI-277 HYDROCHLORIDE) N-[4-[2(R)-氨基-3-巯基丙基]氨基-2-苯基苯甲酰基]-(S)-蛋氨酸甲酯盐酸盐 |
英文别名 | 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 |
化学式 | C22H30ClN3O3S2 |
分子量 | 484.075 |
溶解度 | H2O: 可溶 |
存储条件 | Inert atmosphere,2-8°C |
外观 | 无定形半固体 |
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. FTI-277抑制Ras加工,IC50 为100 nM,但不抑制全细胞中四异戊二烯化Rap1A加工。FTI-277诱导细胞质非法尼化H-Ras积累,在细胞质中积累无活性的Ras/Raf,并阻断H-RasF细胞中组成型MAPK激活。 FTI-277引起辐射后细胞凋亡增加,并增加H-ras转化的大鼠胚胎细胞的辐射敏感性。在耐药骨髓瘤细胞中,FTI-277也会抑制细胞生长,并诱导细胞凋亡。在SH-SY5细胞中,FTI-277减少细胞退化,活化,c-Jun-N端激酶级联和Ras激活过程中甲基苯丙胺诱导的毒性作用。 |
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. 在感染乙型肝炎病毒(HBV) 和 HDV的小鼠体内,FTI-277 (50 mg/kg/d i.p.)有效清除HDV病毒血症。 |
危险品标志 | Xi - 刺激性物品 |
风险术语 | 36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36 - 穿戴适当的防护服。 |
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 |
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