F9803

FTI-277 trifluoroacetate salt

≥95% (HPLC), film

• Synonym(s): N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl]methionine methyl ester trifluoroacetate salt
• Empirical Formula (Hill Notation): C₂₂H₂₉N₃O₃S₂ · xC₂HF₃O₂
• CAS Number: 170006-73-2
• Molecular Weight: 447.61 (free base basis)
• NACRES: NA.77
• PubChem Substance ID: 329799790
• UNSPSC Code: 51111800
• MDL number: MFCD06795840

Properties

• assay: ≥95% (HPLC)
• form: film
• storage condition: desiccated
• solubility: H₂O: ≥2 mg/mL
• shipped in: dry ice
• storage temp.: −70°C
• SMILES string: OC(=O)C(F)(F)F.COC(=O)[C@H](CCSC)NC(=O)c1ccc(NC[C@@H](N)CS)cc1-c2ccccc2
• InChI: 1S/C22H29N3O3S2.C2HF3O2/c1-28-22(27)20(10-11-30-2)25-21(26)18-9-8-17(24-13-16(23)14-29)12-19(18)15-6-4-3-5-7-15;3-2(4,5)1(6)7/h3-9,12,16,20,24,29H,10-11,13-14,23H2,1-2H3,(H,25,26);(H,6,7)/t16-,20+;/m1./s1
• InChI key: GJEFFRDWFVSCOJ-PXPMWPIZSA-N

Description

Application

Farnesyltransferase inhibitor 277 (FTI-277) has been used to:

• inhibit protein farnesylation in breast cell lines.
• in marrow-isolated adult multilineage inducible cells (MIAMI).
• inhibition of farnesyl transferase in CV-1 in Origin with SV40 genes cells (COS-7).

Biochem/physiol Actions

Highly potent (pM/nM) Ras CAAX peptidomimetic which antagonizes both H and K-Ras oncogenic signaling. Inhibitor of farnesyltransferase (Ftase) IC₅₀ = 50 nM.

Farnesyltransferase inhibitor 277 (FTI-277) mediates apoptosis in multiple myeloma and is regarded as a potential therapeutic agent.

Packaging

Very hygroscopic material, package in a dry room with deoxygenated MeOH and pump down the solvent. Store with desiccant.

Safety Information

• pictograms: GHS07
• signalword: Warning
• hcodes: H315,H319,H335
• pcodes: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• target_organs: Respiratory system
• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable
• ppe: dust mask type N95 (US), Eyeshields, Gloves