An inhibitor of FGFRs
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FIIN-3

Item No. 20709

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[[[(2,6-dichloro-3,5-dimethoxyphenyl)amino]carbonyl][6-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]methyl]phenyl]-2-propenamide
CAS Number
1637735-84-2
Molecular Formula
C34H36Cl2N8O4
Formula Weight
691.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: sparingly solubleMethanol: sparingly soluble
λmax
287 nm
SMILES
C=CC(NC(C=C1)=CC=C1CN(C(NC2=C(Cl)C(OC)=CC(OC)=C2Cl)=O)C3=NC=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=C3)=O
InChi Code
InChI=1S/C34H36Cl2N8O4/c1-5-30(45)40-24-8-6-22(7-9-24)20-44(34(46)41-33-31(35)26(47-3)18-27(48-4)32(33)36)29-19-28(37-21-38-29)39-23-10-12-25(13-11-23)43-16-14-42(2)15-17-43/h5-13,18-19,21H,1,14-17,20H2,2-4H3,(H,40,45)(H,41,46)(H,37,38,39)
InChi Key
SFLKJNSBBVSPFE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    FIIN-3 is an inhibitor of FGF receptors (FGFRs; IC50s = 13, 21, 31, and 35 nM for recombinant FGFR1-4, respectively).1 It is selective for FGFRs over a panel of 456 kinases at a concentration of 1 μM, however, it does inhibit EGFR (IC50 = 204 nM). FIIN-3 inhibits growth of Ba/F3 cells that are dependent on the kinase activity of wild-type FGFR1-4 as well as gatekeeper mutant FGFR2 and FGFR3 (EC50s = <1-69 nM) and inhibits FGFR-dependent signaling in a concentration-dependent manner in FGFR2TEL/V564M-dependent Ba/F3 cells. FIIN-3 also inhibits growth in a panel of cancer cell lines (EC50s = 1.4-499 nM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tan, L., Wang, J., Tanizaki, J., et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc. Natl. Acad. Sci. USA 111(45), E4869-E4877 (2014).