Tipifarnib

SKU: orb1225809

Description

Tipifarnib ((IND 58359, R115777) is a potent and selective inhibitor of FTase (farnesyltransferase); inhibits the farnesylation of lamin B and K-RasB peptide substrates with IC50s of 0.86 nM and 7.9 nM, respectively; no activity for PGGT1(IC50>50 uM); shows sensiticity for tumor cell lines bearing H-ras or N-ras mutations; inhibits the growth of tumors bearing mice and orally bioavailable.Blood Cancer Phase 3 Clinical.

Key Properties

• CAS Number: 192185-72-1
• MW: 489.3958
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₂Cl₂N₄O
• SMILES: O=C1N(C)C2=C(C=C([C@@](C3=CC=C(Cl)C=C3)(N)C4=CN=CN4C)C=C2)C(C5=CC=CC(Cl)=C5)=C1
• Target: Ftase
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Animal model: GalN/LPS challenge mouse. Dosage: 10 mg/kg; while chanllenge with GalN (400 mg/kg; IP) and LPS (32 g/kg). Administration: IP; 60 min before challenge. Result: Protected primary hepatocytes from GalN/tumor necrosis factor-induced cell death. Inhibited caspase 3 activation and upregulating antiapoptotic proteins.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IND 58359 | R115777 | IND-58359 | IND58359 | R-115777 | R 115777

Quick Database Links

Gene Symbol

Ftase