Recettore del fattore di crescita dei fibroblasti (FGFR)

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

U3-1784 is a humanized monoclonal antibody targeting CD334, with anti-cancer activity, used in liver cancer research.

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

FGFR1/VEGFR2-IN-1 (compound 2b) is an inhibitor of both FGFR1 and VEGFR2, applicable in cancer research [1].

Vofatamab (B-701) is a fully human monoclonal antibody targeting FGFR3, often used in combination with other compounds to treat cancer.

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

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

Bemarituzumab (FUT8-KO) is a humanized IgG1 monoclonal antibody targeting FGFR2b that lacks the FUT8 gene. The Fc domain glycan of the Bemarituzumab (FUT8-KO) antibody is devoid of core fucose, resulting in high affinity for human FcγRIIIa.

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.

Bemarituzumab: humanized IgG1 antibody inhibits FGFR2b, may be used in cancer research.

FGFR4-IN-19 (compound 8B) is a potent covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4) with an IC50 value of 1.2 nM. It achieves high efficiency and selectivity by covalently targeting the rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 is applicable for hepatocellular carcinoma (HCC) research.

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.

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

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.

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.

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

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.

IMC-D11 is a fully human anti-FGFR3 mAb that inhibits tumor cell proliferation by blocking ligand binding and receptor phosphorylation.

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

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