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FIIN-1 | FIIN-1 : Covalent inhibitor of FGFR1, FGFR2, FGFR3, FGFR4
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FGFR1
  • Kd:2.8 nM
  • IC50:9.2 nM
  • EC50:14 nM
  • INH:4 µM
FGFR2
  • Kd:6.9 nM
  • IC50:6.2
    FGFR3
    • Kd:5.4 nM
    • IC50:11.9 nM
    • EC50:10 nM
    FGFR4
    • Kd:120 nM
    • IC50:189 nM
      up to 200 nM

      Selectivity

      In Vitro Selectivity Assessment
      Potency Assay Off-Target:
      FIIN-1 and FRIN-1 were profiled against a panel of 402 different kinase binding assays using the Amb ...
      In Cell Selectivity Assessment
      Potency Assay Off-Target:
      FIIN-1 was profiled using a panel of various tyrosine kinase-transformed Ba/F3 cells. FIIN-1 was not ...

      Potency
      Cellular
      In Vitro

      FGFR1

      Mode of Action: Covalent Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1016/j.chembiol.2010.02.007

      FGFR2

      Mode of Action: Covalent Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1016/j.chembiol.2010.02.007

      FGFR3

      Mode of Action: Covalent Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1016/j.chembiol.2010.02.007

      FGFR4

      Mode of Action: Covalent Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1016/j.chembiol.2010.02.007

      Negative Control Compounds

      FRIN-1
      Notes: FRIN-1 is 24-fold less potent against Tel-FGFR1 (EC50 = 340 nM) and 100-fold less potent against Tel-FGFR3 (EC50 = 1040 nM)-transformed Ba/F3 cells. Assay of recombinant FGFR1 measured in Z′-lyte format demonstrated that FIIN-1 is approximately 2.3 times more potent than FRIN-1 in vitro.
      SMILES: CCC(Nc1cc(CN2C(N(Cc3c2nc(NCCCCN(CC)CC)nc3)c4c(Cl)c(OC)cc(OC)c4Cl)=O)ccc1)=O

      Chemical Information

      Molecular Formula C32H39Cl2N7O4
      SMILEs C=CC(=O)Nc1cccc(CN2C(=O)N(c3c(Cl)c(OC)cc(OC)c3Cl)Cc3cnc(NCCCCN(CC)CC)nc32)c1
      InChI InChI=1S/C32H39Cl2N7O4/c1-6-26(42)37-23-13-11-12-21(16-23)19-41-30-22(18-36-31(38-30)35-14-9-10-15-39(7-2)8-3)20-40(32(41)43)29-27(33)24(44-4)17-25(45-5)28(29)34/h6,11-13,16-18H,1,7-10,14-15,19-20H2,2-5H3,(H,37,42)(H,35,36,38)
      Molecular weight 655.24 Da
      AlogP 6.6058000000000066
      HBond acceptors 11
      HBond donors 2
      Atoms 84

      Vendors

      Note: This is not an exhaustive list and does not indicate endorsement by the Portal.

      Expert Reviews

      by SERP+
      (on 23 Sept 2024)
      Cellular Use Rating
      FIIN1 is a very potent covalent inhibitor for FGFR1 and FGFR3 with IC50 values below 15 nM (in vitro). Convincing proof of covalent binding mode by pharmacological and genetic controls. Selectivity of...
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