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| 品牌 | absin | CAS | 180977-34-8 |
|---|---|---|---|
| 分子式 | C22H30ClN3O3S2 | 纯度 | >98% |
| 分子量 | 484.07 | 货号 | abs47028136 |
| 规格 | 2mg | 供货周期 | 现货 |
| 主要用途 | is the methyl ester of FTI 277 | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
FTI 277 hydrochloride 180977-34-8
| 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. |
| 基本信息 | |
| 别名 | FTI 277 HCl;FTI 277 |
| 外观 | amorphous semi-solid |
| 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 |
| 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. |
| 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. |
| 参考文献 | |
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| 研究领域 | |
| 研究领域 | Signal TransductionMetabolism Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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