化合物FTI 277 hydrochloride T2700
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Product IntroductionBioactivity英文名: FTI-277 hydrochloride描述: FTI-277 hydrochloride (FTI 277 HCl) 是一种法尼基转移酶FTase 抑制剂，高效 Ra
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Product Introduction
Bioactivity
英文名: FTI-277 hydrochloride
描述: FTI-277 hydrochloride (FTI 277 HCl) 是一种法尼基转移酶FTase 抑制剂，高效 Ras CAAX 肽模拟物，可抑制H-Ras 和K-Ras 信号转导，还可抑制hepatitis delta virus 感染。
细胞实验: Cells are seeded at 8000–14 000 cells/well in 96-well plates. To establish a dose–response to FTI-277, cells are incubated for 96 h in two-fold serial dilutions ranging from 3.75 times 10-7 M to 1 times 10-5 M. Following continuous drug exposure, 50 μL MTT dye is added. The insoluble formazan complex is solubilized with DMSO and absorbance measured at 540 nm. IC50s and 95% confidence intervals are calculated by regression analysis of the linear portion of the dose–response curve. (Only for Reference)
激酶实验: FTase and GGTase I Activity Assay: FTase and GGTase I activities from 60,000×g supernatants of human Burkitt lymphoma (Daudi) cells are assayed. Inhibition studies are performed by determining the ability of Ras CAAX peptidomimetics to inhibit the transfer of [3H]farnesyl and [3H]geranylgeranyl from [3H]farnesylpyrophosphate and [3H]geranylgeranylpyrophosphate to H-Ras-CVLS and H-Ras-CVLL, respectively.
体外活性: 在感染乙型肝炎病毒和丁型肝炎病毒的小鼠体内,FTI-277（50 mg/kg/day,i.p.）可有效清除丁型肝炎病毒血症.
体内活性: 在耐药骨髓瘤细胞中,FTI-277对细胞生长有抑制作用,还诱导细胞凋亡。在SH-SY5细胞中,FTI-277对细胞退化、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有减弱作用。FTI-277抑制Ras加工（IC50：100 nM）,但对全细胞中四异戊二烯化Rap1A加工无影响。FTI-277导致辐射后细胞凋亡增加,并使H-ras转化的大鼠胚胎细胞的辐射敏感性增加。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: Ethanol : 12 mg/mL (24.8 mM)
H2O : 14 mg/mL (28.9 mM)
DMSO : 89 mg/mL (183.9 mM)
关键字: Inhibitor | Farnesyl Transferase | FTI 277 | Ras | Ftase | FTI-277 Hydrochloride | FTI 277 Hydrochloride | inhibit | FTI277 Hydrochloride | FTI-277 | FTI277 hydrochloride | Apoptosis | FTI 277 hydrochloride | FTI277
相关产品: Propylparaben | UNC1215 | Cl-amidine hydrochloride | 1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil | Flavokawain A | OSI-930 | Fangchinoline | Sinapinic Acid | Ligustrazine | Isocurcumenol
相关库: Anti-Prostate Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Active Compound Library | Highly Selective Inhibitor Library | Preclinical Compound Library
Bioactivity
英文名: FTI-277 hydrochloride
描述: FTI-277 hydrochloride (FTI 277 HCl) 是一种法尼基转移酶FTase 抑制剂，高效 Ras CAAX 肽模拟物，可抑制H-Ras 和K-Ras 信号转导，还可抑制hepatitis delta virus 感染。
细胞实验: Cells are seeded at 8000–14 000 cells/well in 96-well plates. To establish a dose–response to FTI-277, cells are incubated for 96 h in two-fold serial dilutions ranging from 3.75 times 10-7 M to 1 times 10-5 M. Following continuous drug exposure, 50 μL MTT dye is added. The insoluble formazan complex is solubilized with DMSO and absorbance measured at 540 nm. IC50s and 95% confidence intervals are calculated by regression analysis of the linear portion of the dose–response curve. (Only for Reference)
激酶实验: FTase and GGTase I Activity Assay: FTase and GGTase I activities from 60,000×g supernatants of human Burkitt lymphoma (Daudi) cells are assayed. Inhibition studies are performed by determining the ability of Ras CAAX peptidomimetics to inhibit the transfer of [3H]farnesyl and [3H]geranylgeranyl from [3H]farnesylpyrophosphate and [3H]geranylgeranylpyrophosphate to H-Ras-CVLS and H-Ras-CVLL, respectively.
体外活性: 在感染乙型肝炎病毒和丁型肝炎病毒的小鼠体内,FTI-277（50 mg/kg/day,i.p.）可有效清除丁型肝炎病毒血症.
体内活性: 在耐药骨髓瘤细胞中,FTI-277对细胞生长有抑制作用,还诱导细胞凋亡。在SH-SY5细胞中,FTI-277对细胞退化、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有减弱作用。FTI-277抑制Ras加工（IC50：100 nM）,但对全细胞中四异戊二烯化Rap1A加工无影响。FTI-277导致辐射后细胞凋亡增加,并使H-ras转化的大鼠胚胎细胞的辐射敏感性增加。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: Ethanol : 12 mg/mL (24.8 mM)
H2O : 14 mg/mL (28.9 mM)
DMSO : 89 mg/mL (183.9 mM)
关键字: Inhibitor | Farnesyl Transferase | FTI 277 | Ras | Ftase | FTI-277 Hydrochloride | FTI 277 Hydrochloride | inhibit | FTI277 Hydrochloride | FTI-277 | FTI277 hydrochloride | Apoptosis | FTI 277 hydrochloride | FTI277
相关产品: Propylparaben | UNC1215 | Cl-amidine hydrochloride | 1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil | Flavokawain A | OSI-930 | Fangchinoline | Sinapinic Acid | Ligustrazine | Isocurcumenol
相关库: Anti-Prostate Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Active Compound Library | Highly Selective Inhibitor Library | Preclinical Compound Library
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