FIIN-2

SKU: orb1300421

Description

FIIN-2 is an irreversible pan-FGFR inhibitor exhibiting potent activity against FGFR1-4 with IC50 values of 3.09, 4.3, 27, and 45.3 nM, respectively. It is a valuable chemical probe for studying FGFR-driven pathologies in both cellular assays and preclinical cancer models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1633044-56-0
• MW: 634.73
• Purity: 97.82% (May vary between batches)
• Formula: C₃₅H₃₈N₈O₄
• SMILES: COc1cc(OC)cc(c1)N1Cc2cnc(Nc3ccc(cc3)N3CCN(C)CC3)nc2N(Cc2ccc(NC(=O)C=C)cc2)C1=O
• Target: FGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:64 mg/mL (100.83 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.15 mM)

Bioactivity

• Target IC50:
  FGFR2:4.3 nM|FGFR4:45.3 nM|FGFR3:27 nM|FGFR1:3.09 nM
• In Vivo:
  In a zebrafish developmental model, FIIN-2 causes mild or severe phenotypes to the tail morphogenesis by inhibiting FGFR.
• In Vitro:
  In FGFR1-4 Ba/F3 cells, FIIN-2 inhibits cell proliferation with EC50 in the single- to double-digit nanomolar range. FIIN-2 also shows excellent antiproliferative activity in a variety of backgrounds, including cell lines that have gatekeeper mutations in FGFR1 and that are dependent on FGFR4.
• Cell Research:
  NCI-H2077, NCI-H1581, H520, Kato III, AN3CA, RT112, A2780, 4T1, and SKOV-3 cells are treated with inhibitors 1 d after being plated at a density of 1,500 cells per well in 96-well plates. The gatekeeper mutation cell lines are generated by ectopically overexpressing FGFR1 V561M in either NCI-H2077 or NCI-H1581 cells via lentiviral transduction. Cell survival is assessed at 96 h following the addition of inhibitor using the Cell-Titer-Glo reagent according to the manufacturer's instructions. EC50 values are calculated using GraphPad Prism 5. SKOV-3 cells also are treated in the presence of FGF or EGF ligand. Proliferation measurements were made after 96 h using a luminometer. Data are shown as relative values: The luminescence of cells with indicated inhibitor dose is compared with that of untreated cells.(Only for Reference)

Storage & Handling

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

Alternative Names

Inhibitor, Fibroblast growth factor receptor, FGFR2, FGFR, FGFR1, FGFR4, FGFR3, FIIN 2, FIIN2, FIIN-2, inhibit

Compound Identifiers

PubChem CID

91825767