FTI 277 hydrochlorideCAS号： 180977-34-8分子式： C22H30ClN3O3S2分子量： 484.07描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
FTI 277 hydrochloride 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. |
| 纯度 |
＞98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
FTI 277 HCl；FTI 277
|
| 外观 |
amorphous semi-solid
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| 可溶性/溶解性 |
DMSO : 89 mg/mL (183.9 mM)
Ethanol : 12 mg/mL (24.8 mM) Water : 14 mg/mL (28.9 mM) |
| 生物活性 | |
| 靶点 |
FTase
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| In vitro(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.
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| In vivo(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.
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| 参考文献 | |
| 参考文献 |
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分子结构图
