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FTI-277

  Cat. No.:  DC23934   Featured
Chemical Structure
170006-73-2
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More than 5000 active chemicals with high quality for research!
Field of application
A peptide mimetic of the C-terminal Cys-Val-Ile-Met of K-Ras4B that potently inhibits FTase (Farnesyltransferase) with IC50 of 0.5 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 170006-73-2
Chemical Name: L-Methionine,N-[[5-[[(2R)-2-amino-3-mercaptopropyl]amino][1,1'-biphenyl]-2-yl]carbonyl]-,methyl ester
Synonyms: L-Methionine,N-[[5-[[(2R)-2-amino-3-mercaptopropyl]amino][1,1'-biphenyl]-2-yl]carbonyl]-,methyl ester;FTI 277;FTI-277 trifluoroacetate salt;L-Methionine,N-[[5-[[(2R)-2-amino-3-mercaptopropyl]amino][1,1'-biphenyl]-2-yl]carbonyl]-,methy...;FTI-277;N-[[5-[[(2R)-2-Amino-3-mercaptopropyl]amino][1,1'-biphenyl]-2-yl]carbonyl]-L-methionine methyl ester;METHYL[N-[2-PHENYL-4-N-[2(R)-AMINO-3-MERCAPTOPROPYLAMINO] BENZOYL]]-METHIONATE, TFA;N-[4-[2(R)-AMINO-3-MERCAPTOPROPYL]AMINO-2-PHENYLBENZOYL]METHIONINE METHYL ESTER TRIFLUOROACETATE SALT;N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl]methionine methyl ester trifluoroacetate salt
SMILES: CSCC[C@@H](C(=O)OC)NC(=O)C1C(=CC(NC[C@@H](N)CS)=CC=1)C2=CC=CC=C2.OC(=O)C(F)(F)F
Formula: C22H29N3O3S2
M.Wt: 561.63700
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: FTI-277 is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.
Target: FTase inhibitor
In Vivo: FTI-277 treatment prevented increased PTP-1B and PTEN protein expression in burned mice as compared with vehicle alone. In contrast, FTI-277 did not significantly alter protein expression of PTP-1B and PTEN in sham-burned mice [2].
In Vitro: Treatment with FTI-277 (20 microM) for 48 h prior to irradiation led to a significant decrease in survival of radioresistant cells expressing the 24-kDa isoform (HeLa 3A) but had no effect on the survival of control cells (HeLa PINA). The radiosensitizing effect of FTI-277 is accompanied by a stimulation of postmitotic cell death in HeLa 3A cells and by a reduction in G(2)/M-phase arrest in both cell types [1]. Treatment of PC-3 cells with GGTI-298 and FTI-277 inhibited migration and invasion in a time- and dose-dependent manner [3].
References: [1]. Cohen-Jonathan E, et al. The farnesyltransferase inhibitor FTI-277 suppresses the 24-kDa FGF2-induced radioresistance in HeLa cells expressing wild-type RAS. Radiat Res. 1999 Oct;152(4):404-11. [2]. Nakazawa H, et al. Role of protein farnesylation in burn-induced metabolic derangements and insulin resistance in mouse skeletal muscle. PLoS One. 2015 Jan 16;10(1):e0116633. [3]. Virtanen SS, et al. Inhibition of GGTase-I and FTase disrupts cytoskeletal organization of human PC-3 prostate cancer cells. Cell Biol Int. 2010 Aug;34(8):815-26.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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