Fibroblast Growth Factor Receptor (FGFR)

Fazpilodemab (BFKB8488A) is a humanized bispecific antibody that targets and activates the Klotho β and fibroblast growth factor receptor 1c receptor complex.

Efruxifermin, a modified FGF21 with IgG1 Fc, has increased stability and affinity. Used in non-alcoholic steatohepatitis research.

A unique collection of 1016 tyrosine kinase inhibitors for high throughput screening and high content screening for drug discovery in tyrosine kinase related

Vosoritide (BMN 111), a CNP analogue, targets NPR-B, inhibits FGFR3, aiding achondroplasia, dwarfism study.

FGFR-IN-14 (compound 10h) is a pan-FGFR inhibitor. It effectively inhibits FGFR1, FGFR2, FGFR3, and the FGFR2V564F gatekeeper mutant, with IC50 values of 46, 41, 99, and 62 nM, respectively. Additionally, FGFR-IN-14 demonstrates strong antiproliferative effects on NCI-H520 lung cancer cells and SNU-16 and KATO III gastric cancer cells, with IC50 values of 19, 59, and 73 nM, respectively.

FGFR4-IN-20 (comp 11) is an orally active and selective FGFR4 inhibitor, demonstrating IC50 values of 19 nM against Huh7 cells and 36 nM for FGFR4 kinase. It is utilized in hepatocellular carcinoma research.

PNU-145156E, an angiogenesis blocker with anti-tumor effects in mice, inhibits growth factors in animal studies.

FGFR1 inhibitor-2, potent at 4.55 μM IC50 in MDA-MB-231, targets triple-negative breast cancer.

ODM-203 sodium is an orally bioavailable selective and efficient FGFR and VEGFR inhibitor with antitumor activity, used in solid tumor research.

Efimosfermin alfa is a humanized antibody targeting FGFR1.

PKCε (85-92) (ψεRACK) is a peptide and selective PKCε activator, induces a pro-angiogenic response, promotes FGF-2 cytosolization, regulates VEGF activity.

IMC-D11 (LY-3076226 antibody) is an IgG1 monoclonal antibody targeting FGFR3. It serves as the antibody component of LY3076226. For its isotype control, refer to Human IgG1 kappa, Isotype Control.

FGFR2 degrader1 (compound 28E) is a selective PROTACS degrader of FGFR2, with a DC50 of 0.645 nM. FGFR2 plays a significant role in cancer research.

BR-cpd7 is a PROTAC degrader of fibroblast growth factor receptors (FGFR1/2) with a DC50 of 10 nM. It is capable of arresting the cell cycle and inhibiting the proliferation of tumor cells with aberrant activation of FGFR1/2.

Arg-IN-1 is a selective covalent inhibitor targeting Arginine (Arg), with IC50 values of 9.7 nM and 30.4 nM for FGFR2 and FGFR3, respectively. This compound is designed to potentially avoid the off-target toxicity of FGFR1/4 and overcome acquired resistance, offering potential in cancer therapies targeting FGFR.

BW710 is an orally active inhibitor specifically targeting fibroblast growth factor receptor 2 (FGFR2). It effectively inhibits the proliferation of BaF3-FGFR2 cells with an IC50 value of 2.8 nM. BW710 completely suppresses FGFR2 enzymatic activity and demonstrates selectivity among 75 tyrosine kinases, including FGFR1, FGFR3, and FGFR4, at a 1 μM concentration. Additionally, BW710 impedes FGFR2 signaling and selectively inhibits the proliferation of cancer cells driven by FGFR2. It exhibits promising pharmacokinetic properties, with an oral bioavailability of 29% in mice.

PROTAC FGFR1 degrader-1 (compound S2H) is a targeted degrader of FGFR1, demonstrating an IC50 of 26.81 nM and a DC50 of 39.78 nM in KG1a cells. This compound is composed of a CRBN-type E3 ligase ligand (blue part) Pomalidomide, a target protein ligand (red part) FGFR1ligand-1, and a PROTAC linker (black part) 9-Bromononanoic acid, together forming the conjugate E3LigaseLigand-linker Conjugate 164.

Recifercept (TA-46) is a recombinant human soluble fibroblast growth factor receptor 3, a decoy protein that competes for ligands of mutant FGFR3.

E-7090 is a fibroblast growth factor receptor inhibitor. E-7090 is a selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3.