GNF-5

SKU: orb1224017

Description

GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).

Key Properties

• CAS Number: 778277-15-9
• MW: 418.37
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₇F₃N₄O₃
• SMILES: O=C(NCCO)C1=CC=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=C1
• Target: Bcr-Abl
• Solubility: Ethanol: 20 mg/mL warmed (47.8 mM); DMSO: 83 mg/mL (198.38 mM)

Bioactivity

• In Vivo:
  GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters. GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious In vivo but can observe relapses. GNF-5 (75 mg/kg, b. i. d) inhibits T315I Bcr-Abl combination with nilotinib In vivo. Animal model: Male Balb/c mice. Dosage: 5 mg/kg, 20 mg/kg. Administration: 5 mg/kg intravenously or 20 mg/kg orally. . Animal model: p210 xenograft model. Dosage: 50 or 100 mg/kg. Administration: oral, twice daily, for 7 days. Result: Could normalize blood counts and spleen size. Animal model: Bone marrow transduction/transplantation model. Dosage: 75 mg/kg. Administration: twice daily. Result: Showed no significant response (alone). Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib.
• In Vitro:
  GNF-5 has inhibition of wild-type Abl with an IC50 value of 0.22 μM but no inhibition for myristate site mutant E505K (IC50 >10 μM). Cell Viability Assay Cell line: wild type and mutant Bcr-Abl expressing Ba/F3 cells. Concentration: 0.2, 0.8 and 1.6 μM Incubation time: 48 h. Result: Inhibited wild-type Abl in a non-ATP competitive fashion.

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

GNF-5 | GNF 5 | GNF5.

Quick Database Links

Gene Symbol

Bcr-Abl