FTI 277 HYDROCHLORIDE
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- CAS号:
- 180977-34-8
- 英文名:
- FTI 277 HYDROCHLORIDE
- 英文别名:
- CS-1757;FTI 277 HCl;FTI 277 HCL;FTI 277;FTI 277 HYDROCHLORIDE;FTI-277 TRIFLUOROACETATE SALT;FTI 277 HYDROCHLORIDE USP/EP/BP;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;(S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate hydrochloride;(S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate hydrochloride
- 中文名:
- FTI 277 HYDROCHLORIDE
- 中文别名:
- FTI-277盐酸盐;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
- CBNumber:
- CB2503510
- 分子式:
- C22H30ClN3O3S2
- 分子量:
- 484.075
- MOL File:
- 180977-34-8.mol
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FTI 277 HYDROCHLORIDE化学性质
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储存条件:
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Inert atmosphere,2-8°C
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溶解度:
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H2O: soluble
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形态:
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amorphous semi-solid
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FTI 277 HYDROCHLORIDE性质、用途与生产工艺
FTI 277 HCl是FTI 277的甲酯，是一种有效的选择性farnesyltransferase (FTase)抑制剂，IC50为500 pM，选择性比密切相关的GGTase I 高100倍。
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 mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d i.p.) effectively clears HDV viremia.
FTI 277 HCl是FTI 277的甲酯，是一种有效的选择性farnesyltransferase (FTase)抑制剂，IC50为500 pM，选择性比密切相关的GGTase I 高100倍。FTI 277 HCl可抑制细胞生长并诱导凋亡。FTI 277 HCl可有效清除HDV病毒血症。
| Target | Value |
FTase
(Cell-free assay)
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500 pM
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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。
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。
FTI 277 HYDROCHLORIDE
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-15872A | FTI-277 hydrochloride | | 1 mg | 502元 |
| 2024/01/25 | HY-15872A | FTI 277 HYDROCHLORIDE
FTI-277 hydrochloride | 180977-34-8 | 2mg | 800元 |
FTI 277 HYDROCHLORIDE
生产厂家
180977-34-8, FTI 277 HYDROCHLORIDE 相关搜索:
- Inhibitors
- 药靶配体
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- 小分子抑制剂
- 抑制剂
- C22H30ClN3O3S2
- FTI-277盐酸盐
- 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
- 180977-34-8
- (S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate hydrochloride
- FTI 277 HCL;FTI 277
- CS-1757
- (S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate hydrochloride
- FTI 277 HYDROCHLORIDE USP/EP/BP
- (S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate FTI 277 HCl
- FTI 277 HCl
- FTI-277 TRIFLUOROACETATE SALT
- FTI 277 HYDROCHLORIDE
- 4-[2(R)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(S)-methionine methyl ester hydrochloride