Fibroblast Growth Factor Receptor (FGFR)

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

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

<p>FGFR1 Inhibitor 7 (compound 5), a potent FGFR1 tyrosine kinase inhibitor, exhibits an IC50 of 0.33 nM against its target and demonstrates broad-spectrum</p>

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

<p>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.</p>

<p>Efimosfermin alfa is a humanized antibody targeting FGFR1.</p>

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

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

<p>LC-MB12 is a PROTAC FGFR2 compound that degrades FGFR2 and can be used to study gastric cancer.</p>

<p>Gunagratinib (ICP-192) is a pan-FGFR inhibitor, useful in research on FGFR-related diseases.</p>

<p>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.</p>

<p>FGFR4-IN-14 (Compound 27i) is a selective FGFR4 inhibitor with an IC50 of 2.4 nM, showing potent inhibition of cell proliferation in the V550L and N535K mutant</p>

<p>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.</p>

<p>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.</p>

<p>FGFR1 inhibitor-8 (Compound 9), an FGFR1 inhibitor with an IC50 of 0.5 nM, binds to the ATP-binding pocket of FGFR1 and exhibits anticancer activity [1].</p>

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

<p>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.</p>

<p>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.</p>

<p>NSC 12 is an orally active pan-FGF trap that binds FGF2 and interferes with its interaction with FGFR1 with potential FGF-dependent antitumor activity.</p>