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| Product | Description | |
|---|---|---|
| FTI 277 | FTI 277. Group: Biochemicals. Grades: Purified. CAS No. 1217447-06-7. Pack Sizes: 1mg. US Biological Life Sciences. |  Worldwide |
| FTI 277 HCl | FTI-277 inhibits Ras processing with an IC50 of 100 nM, but not the geranylgeranylated Rap1A processing in whole cells. Synonyms: FTI277 HCl; FTI 277 HCl; FTI-277 HCl. Grades: >98%. CAS No. 180977-34-8. Molecular formula: C22H30ClN3O3S2. Mole weight: 484.07. |  |
| FTI 277 trifluoroacetate salt | FTI 277 is a prodrug form of FTI 276 that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM) with antiproliferative activity. It potently inhibits H-Ras and K-Ras processing in whole cells (IC50 = 0.1 and 10 μM, respectively) and disrupts constitutive H-Ras-specific activation of MAPK. Synonyms: FTI 277 trifluoroacetate salt; FTI277 trifluoroacetate salt; FTI-277 trifluoroacetate salt; N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl]methionine methyl ester trifluoroacetate salt. Grades: ≥95% by HPLC. CAS No. 1217447-06-7. Molecular formula: C22H29N3O3S2.C2HF3O2. Mole weight: 561.64. | |
| FTI-277 | FTI-277, a peptide mimetic of the COOH-terminal Cys-Val-Ile-Met of K-Ras4B that inhibited potently FTase in vitro (IC50 = 500 pM) and was highly selective for FTase over geranylgeranyltransferase I (GGTase I) (IC50 = 50 nM). FTI-277, the methyl ester derivative of FTI-276, was extremely potent (IC50 = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells. Treatment of H-Ras oncogene-transformed NIH 3T3 cells with FTI-277 blocked recruitment to the plasma membrane and subsequent activation of the serine/threonine kinase c-Raf-1 in cells transformed by farnesylated Ras (H-RasF), but not geranylgeranylated, Ras (H-RasGG). FTI-277 induced accumulation of cytoplasmic non-farnesylated H-Ras that was able to bind Raf and form cytoplasmic Ras/Raf complexes in which Raf kinase was not activated. Furthermore, FTI-277 blocked constitutive activation of mitogen-activated protein kinase (MAPK) in H-RasF, but not H-RasGG, or Raf-transformed cells. FTI-277 also inhibited oncogenic K-Ras4B processing and constitutive activation of MAPK, but the concentrations required were 100-fold higher than those needed for H-Ras inhibition. The results demonstrate that FTI-277 blocks Ras oncogenic signaling by accumulating inactive Ras/Raf complexes in the cytoplasm, hence preventing constitutive activation of the MAPK cascade. Uses: Radiation-sensitizing agents. Synonyms: FTI-277; FTI 277; FTI277. CAS No. 170006-73-2. Molecular formula: C22H29N3O3S2. Mole weight: 447.612. | |
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