For research use only. Not for therapeutic Use.
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].
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.
| Catalog Number | R059763 |
| CAS Number | 1256152-35-8 |
| Synonyms | N-[3-[[3-(2,6-dichloro-3,5-dimethoxyphenyl)-7-[4-(diethylamino)butylamino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]methyl]phenyl]prop-2-enamide |
| Molecular Formula | C32H39Cl2N7O4 |
| Purity | ≥95% |
| 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) |
| InChIKey | DNVFTXQYIYFQBW-UHFFFAOYSA-N |
| SMILES | CCN(CC)CCCCNC1=NC=C2CN(C(=O)N(C2=N1)CC3=CC(=CC=C3)NC(=O)C=C)C4=C(C(=CC(=C4Cl)OC)OC)Cl |
| Reference | [1]. Wenjun Zhou, et al. A structure-guided approach to creating covalent FGFR inhibitors. Chem Biol. 2010 Mar 26;17(3):285-95. |
