Fibroblast Growth Factor Receptor (FGFR)

Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD (PF-05231023) is a long-acting fibroblast growth factor 21 (FGF21) analog and is an FGF21-receptor agonist.

Formononetin (Flavosil) is an O-methylated isoflavone and a phytoestrogen from the root of Astragalus membranaceus.

Ferulic Acid (Coniferic acid) is a highly abundant phenolic phytochemical and a organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong.

Lucitanib (E-3810) is a VEGFR/FGFR inhibitor targeting VEGFR1-3 and FGFR1-2 with IC50s 7-82.5 nM.

Amlexanox (AA673) treats ulcers by blocking leukotrienes, histamine, reducing inflammation, pain, and healing time.

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

Triamcinolone acetonide (Azmacort) is a Corticosteroid.

Pemigatinib (INCB054828) is an orally active, selective inhibitor of FGFR(IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively).

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity.

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

Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1/2/3. Pazopanib has antitumor activity. Cost-effective and quality-assured.

2,5-Dihydroxybenzoic acid (Gentisic acid) is an active metabolite of salicylic acid degradation with a broad spectrum of biological activity.

FGFR1/DDR2 inhibitor 1 is an inhibitor of discoindin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108

FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor with potent binding affinity, exhibiting an IC50 of 0.85 nM.

Si5-N14 is a key component of siloxane-linked lipid nanoparticles (SiLNP) with properties that enhance vascular repair and exhibit antitumor activity. In transgenic GFP mouse models, Si5-N14 mediates CRISPR-Cas9 editing. In Lewis lung carcinoma (LLC) tumor mouse models, it leads to the knockdown of vascular endothelial growth factor receptor 2 (VEGFR2), producing antitumor effects. Additionally, in mice with virus-induced lung injury, Si5-N14 facilitates the delivery of fibroblast growth factor-2 (FGF-2) mRNA, promoting vascular repair, oxygenation, and improved lung function. Si5-N14 shows potential for research in tumors, pneumonia, and cardiovascular diseases.

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

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].

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.

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

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.

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

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.

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

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

S6K2-IN-1 (Compound 2) is an inhibitor of S6K2 with an IC50 of 22 nM and also exhibits inhibitory activity against FGFR4 with an IC50 of 216 nM.

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

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

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.

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

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.

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.

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.

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.

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

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

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

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

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

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.

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.

SM27 is a fibroblast growth factor 2 (FGF2) inhibitor with anti-angiogenic activity and can be used to study tumours.