Lirafugratinib |
Lirafugratinib : Covalent Inhibitor of FGFR2
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download
Probe Summary
More...
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| FGFR2 |
|
|
Covalent Inhibitor
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Within target family: RLY-4008 has >250-fold selectivity over FGFR1, and >80- and >5,000-fold select ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selectivity of RLY-4008 in cells was evaluated on the proliferation of FGFR2-dependent (KATO III, NC ...
Potency Cellular
In Vitro
FGFR2
Mode of Action: Covalent Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1158/2159-8290.CD-23-0475
In Vivo Validations
Mouse
Dose: 30 mg/kg twice daily
Target engagement assay:
≥90% pFGFR2 inhibition sustained throughout the 12-hour dosing interval
DOI Reference: 10.1158/2159-8290.CD-23-0475
Chemical Information
| Molecular Formula | C28H24FN7O2 |
| SMILEs | C=C(C)C(=O)Nc1ccc(-c2c(-c3ccc(Oc4nccc(C)n4)c(F)c3)c3c(N)ncnc3n2C)cc1 |
| InChI | InChI=1S/C28H24FN7O2/c1-15(2)27(37)35-19-8-5-17(6-9-19)24-22(23-25(30)32-14-33-26(23)36(24)4)18-7-10-21(20(29)13-18)38-28-31-12-11-16(3)34-28/h5-14H,1H2,2-4H3,(H,35,37)(H2,30,32,33) |
| Molecular weight | 509.20 Da |
| AlogP | 5.428920000000004 |
| HBond acceptors | 9 |
| HBond donors | 3 |
| Atoms | 62 |
References
Publications
Vendors
Note: This is not an exhaustive list and does not indicate endorsement by the Portal.