Home Protein Tyrosine Kinase FGFR inhibitor FIIN-2 For research use only.

FIIN-2

FIIN-2 is an irreversible, pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively.

FIIN-2 Chemical Structure

FIIN-2 Chemical Structure

CAS No. 1633044-56-0

Purity & Quality Control

Batch: S771401 DMSO]69 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.83%
99.83

FIIN-2 Related Products

Signaling Pathway

FGFR Signaling Pathways

FGFR Signaling Pathway

Biological Activity

Description FIIN-2 is an irreversible, pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively.
Targets
FGFR1 [1]
(Cell-free assay)		 FGFR2 [1]
(Cell-free assay)		 FGFR3 [1]
(Cell-free assay)		 FGFR4 [1]
(Cell-free assay)
3.09 nM 4.3 nM 27 nM 45.3 nM
In vitro
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. [1]
Kinase Assay Biochemical assays
Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform.
Cell Research Cell lines NCI-H2077, NCI-H1581, H520, Kato III, AN3CA, RT112, A2780, 4T1, and SKOV-3 cells
Concentrations 1.0 μM
Incubation Time 96 h
Method 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.
In Vivo
In vivo In a zebrafish developmental model, FIIN-2 causes mild or severe phenotypes to the tail morphogenesis by inhibiting FGFR. [1]

Chemical Information & Solubility

Molecular Weight 634.73 Formula

C35H38N8O4
CAS No. 1633044-56-0 SDF Download FIIN-2 SDF
Smiles CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C4CN(C(=O)N(C4=N3)CC5=CC=C(C=C5)NC(=O)C=C)C6=CC(=CC(=C6)OC)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 69 mg/mL ( (108.7 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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