FTI-277 hydrochloride

SKU: orb1305148

Description

FTI-277 hydrochloride is a potent and selective farnesyltransferase (FTase) inhibitor with an IC50 of 500 pM, exhibiting approximately 100-fold selectivity over GGTase I. It is widely used in cancer research to study Ras signaling pathways and has been applied in both in vitro and in vivo models to investigate tumor growth inhibition.

Research Area

Cell Biology, Metabolism Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 180977-34-8
• MW: 484.07
• Purity: 98.19% (May vary between batches)
• Formula: C₂₂H₃₀ClN₃O₃S₂
• SMILES: Cl.Cl.COC(=O)C(CCSC)NC(=O)c1ccc(NCC(N)CS)cc1-c1ccccc1
• Target: Transferase,Apoptosis,Ras
• Solubility: DMSO:145 mg/mL (299.54 mM);H2O:14 mg/mL (28.92 mM);Ethanol:12 mg/mL (24.79 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.82 mM)

Bioactivity

• Target IC50:
  FTase:500 pM
• In Vivo:
  In drug-resistant myeloma cells, FTI-277 inhibits cell growth and induces apoptosis. It mitigates the toxicity induced by methamphetamine in SH-SY5Y cells through effects on cell degeneration, activation, the c-Jun N-terminal kinase cascade, and the Ras activation process. FTI-277 inhibits Ras processing (IC50: 100 nM) without affecting the overall cellular prenylation of Rap1A. Additionally, FTI-277 increases post-irradiation apoptosis and enhances the radiation sensitivity of H-ras transformed rat embryo cells.
• In Vitro:
  In mouse models infected with Hepatitis B Virus (HBV) and Hepatitis D Virus (HDV), FTI-277 administered intraperitoneally at a dosage of 50 mg/kg/day effectively clears Hepatitis D viremia.
• Cell Research:
  Cells are seeded at 8000–14 000 cells/well in 96-well plates. To establish a dose–response to FTI-277, cells are incubated for 96 h in two-fold serial dilutions ranging from 3.75 times 10-7 M to 1 times 10-5 M. Following continuous drug exposure, 50 μL MTT dye is added. The insoluble formazan complex is solubilized with DMSO and absorbance measured at 540 nm. IC50s and 95% confidence intervals are calculated by regression analysis of the linear portion of the dose–response curve. (Only for Reference)

Storage & Handling

• Storage: Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Farnesyl Transferase, GGTase I, FTI 277, FTI 277 HCl, FTI 277 Hydrochloride, FTI 277 hydrochloride, FTI277, FTI-277, FTI277 Hydrochloride, FTI277 hydrochloride, FTI-277 Hydrochloride, Ftase, Apoptosis, Ras

Compound Identifiers

PubChem CID

118797682