FTI 277 hydrochloride

SKU: orb1223227

Description

FTI 277 hydrochloride is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.

Key Properties

• CAS Number: 180977-34-8
• MW: 484.07
• Purity: >98% (HPLC)
• Formula: C₂₂H₃₀ClN₃O₃S₂
• SMILES: COC(=O)[C@H](CCSC)NC(=O)c1c(cc(cc1)NC[C@H](CS)N)c1ccccc1.Cl
• Target: VEGFR
• Solubility: DMSO : ≥ 4.9 mg/mL; 10.12 mM

Bioactivity

• 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.
• 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. Treatment of PC-3 cells with GGTI-298 and FTI-277 inhibited migration and invasion in a time- and dose-dependent manner.

Storage & Handling

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

Quick Database Links

Gene Symbol

VEGFR