1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. FIIN-1

FIIN-1 (Synonyms: FGFR irreversible inhibitor-1)

Cat. No.: HY-15813
Handling Instructions

FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively.

For research use only. We do not sell to patients.

FIIN-1 Chemical Structure

FIIN-1 Chemical Structure

CAS No. : 1256152-35-8

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Description

FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively[1].

IC50 & Target[1]

FGFR1

2.8 nM (Kd)

FGFR2

6.9 nM (Kd)

FGFR3

5.4 nM (Kd)

FGFR4

120 nM (Kd)

FGFR1

9.2 nM (IC50)

FGFR2

6.2 nM (IC50)

FGFR3

11.9 nM (IC50)

FGFR4

189 nM (IC50)

In Vitro

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[1].
FIIN-1 (14 nM-46 μM; 72 hours) inhibits proliferation of FGF signaling-sensitive cancer cell lines[1].
FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely.

Cell Proliferation Assay[1]

Cell Line: Stomach KATO III, SNU-16 and FU97 cells; Bladder RT4 cells; Kidney G-401 and G-402 cells; Lung SBC-3 and H520 cells; Pancreas A2.1 cells; Ovary A2780 and PA-1 cells; Bone RD-ES cells
Concentration:
Incubation Time: 72 hours
Result: The EC50 of 70 nM for Bladder RT4 cell.
The EC50 of 230 nM for Pancreas A2.1 cell.
The EC50 of 2.3 μM for Bone RD-ES cell.
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, FU97 cells, respectively.

Western Blot Analysis[1]

Cell Line: Serum-starved MCF10A cells that stably express iFGFR1
Concentration: 20 nM
Incubation Time: 30 minutes
Result: Blocked activation of iFGFR1 and phosphorylation of downstream effectors Erk1/2.
Molecular Weight

656.60

Formula

C₃₂H₃₉Cl₂N₇O₄

CAS No.

1256152-35-8

SMILES

C=CC(NC1=CC=CC(CN(C2=NC(NCCCCN(CC)CC)=NC=C2CN3C4=C(Cl)C(OC)=CC(OC)=C4Cl)C3=O)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

FIIN-1FGFR irreversible inhibitor-1FIIN1FIIN 1FGFR irreversible inhibitor1FGFR irreversible inhibitor 1FGFRFibroblast growth factor receptorirreversibleFGFR1FGFR2FGFR3FGFR4Flt1Flt4BLKERK5KITMETPDGFRBVEGFR2Inhibitorinhibitorinhibit

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FIIN-1
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HY-15813
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