FIIN-1

SKU: orb1692895

Description

FIIN-1 is a potent, selective, and irreversible inhibitor of FGFR isoforms, demonstrating low nanomolar Kd and IC50 values for FGFR1-3. It is a valuable chemical probe for studying FGFR signaling in cancer research, applicable in both cellular and biochemical assays.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1256152-35-8
• MW: 656.6
• Purity: >99.99% (May vary between batches)
• Formula: C₃₂H₃₉Cl₂N₇O₄
• SMILES: C(N1C=2C(CN(C1=O)C3=C(Cl)C(OC)=CC(OC)=C3Cl)=CN=C(NCCCCN(CC)CC)N2)C4=CC(NC(C=C)=O)=CC=C4
• Target: FGFR
• Solubility: DMSO:45 mg/mL (68.53 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.05 mM)

Bioactivity

• Target IC50:
  FGFR4:120 nM (Kd)|FGFR4:189 nM (IC50)|FGFR3:11.9 nM (IC50)|FGFR3:5.4 nM (Kd)|FGFR1:2.8 nM (Kd)|FGFR1:9.2 nM (IC50)|FGFR2:6.2 nM (IC50)|FGFR2:6.9 nM (Kd)
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• In Vitro:
  FIIN-1 (14 nM-46 μM; 72 h; ) inhibits the proliferation of FGF signaling-sensitive cancer cell lines. The EC50s of 70 nM, 230 nM, 2.3 μM, for Bladder RT4, Pancreas A2.1, Bone RD-ES cells. EC50s of 0.22 and 4.6 μM for Ovary A2780 and PA-1 cells, respectively. EC50s of 0.08 and 4.5 μM for Lung SBC-3 and H520 cells, respectively. EC50s of 0.14 and 1.65 μM for Kidney G-401 and G-402 cells, respectively. EC50s of 0.014, 0.03, and 0.65 μM for Stomach KATO III, SNU-16, and FU97 cells, respectively. FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely. FIIN-1 binds to BLK, ERK5, KIT, MET, PDGFRB, and VEGFR2 with Kds of 65 nM, 160, 420, 1000, 480, and 210 nM, respectively. The IC50s for Blk and Flt1 are 381 nM and 661 nM respectively.
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Storage & Handling

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

Alternative Names

FIIN 1, FIIN1, FIIN-1, FGFR, FGFR irreversible inhibitor-1

Compound Identifiers

PubChem CID

53348188