Fibroblast Growth Factor Receptor (FGFR)

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

FGFR-IN-11 (compound I-5) is an orally active, covalent inhibitor of FGFR, exhibiting IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (

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].

BLU9931 is the first selective small molecule inhibitor of FGFR4.

FGFR4-IN-4 is a FGFR4 inhibitor with anti-tumor activity.

EOC317 (ACTB-1003) is an oral kinase inhibitor (IC50: 6/2/4 nM, for FGFR1/VEGFR2/Tie-2).

Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34/13/13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69/37/

LY2874455 has been used in trials studying the treatment of Advanced Cancer.

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

AZ8010 (AZ12908010) serves as an effective inhibitor of FGFR1-3 and exhibits antiproliferative properties, making it useful for cancer research.

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3, blocking cellular phosphorylation of MET, AXL, and FGFRs.

Efimosfermin alfa is a humanized antibody targeting FGFR1.

ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1, 2, 3, and 4 with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L.

Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs.

Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively

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.

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.

SUN11602, an aniline compound, mimics the neuroprotective mechanisms of basic fibroblast growth factor.

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

ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).

Derazantinib (ARQ-087) is a potent, ATP-competitive, orally active tyrosine kinase inhibitor.Cost-effective and quality-assured.

Irpagratinib (ABSK011) is an FGFR4 antagonist with anticancer activity, inhibiting FGFR4 autophosphorylation and blocking downstream signaling pathways.

Fisogatinib (BLU-554) is a highly potent, selective, and orally active FGFR4 inhibitor.Cost-effective and quality-assured.

Sucralfate (Sucrose octasulfate-aluminum complex) is a cytoprotective agent, an oral gastrointestinal medication primarily indicated for the treatment of active

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

TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.

H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma, with antineoplastic activity.

ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

FIIN-4 is a covalent inhibitor of FGFR and can be used in studies about metastatic breast cancer.

Pazopanib HCl (Votrient) inhibits VEGFR1-3, PDGFR, FGFR, c-Kit, c-Fms with IC50 range 10-146 nM in cell-free assays.

Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally

Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity.

FGFR1inhibitor-17 (Compound 92) is a potent inhibitor of FGFR1, with promising applications in cancer research.

ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.

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.

Surfen dihydrochloride (Aminoquinuride dihydrochloride) is a heparin sulfate antagonist with antimicrobial properties and inhibits blockade of signaling.

PD 089828 inhibits FGFR1, PDGFRβ, EGFR (IC50s: 0.15-5.47 μM), and c-Src (IC50: 0.18 μM).

Fanregratinib is a fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor.

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

FGFR-IN-16 (compound 7N) is a potent inhibitor of FGFR1, FGFR2, and FGFR4, exhibiting IC50 values of 8 nM, 4 nM, and 3.8 nM respectively. It plays a crucial role in cancer research.

Masitinib mesylate (AB-1010 mesylate) is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;

SSR128129E free acid is an orally available and allosteric inhibitor of FGFR(IC50 of 1.9 μM for FGFR1).

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

FGFR2-IN-2 is a specific FGFR2 inhibitor that inhibits FGFR1, FGFR2, and FGFR3, and can be used in the study of cancer and cardiovascular disease.

PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively.

PD173074 inhibits FGFR1 (IC50: 25 nM) and VEGFR2 (100-200 nM); ~1000x more selective for FGFR1 over PDGFR/c-Src.

Ferulic acid sodium (Sodium ferulic) is an agent used in the treatment of cardiovascular and cerebrovascular diseases and to prevent thrombosis.

FGFR4-IN-1 is a potent FGFR4 inhibitor (IC50: 0.7 nM).

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

CP-547632 hydrochloride: oral VEGFR-2/FGF inhibitor (IC50: 11/9 nM), well-tolerated, antitumor.

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3, modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.

FGFR2/3-IN-2 (compound 10) is an orally active inhibitor targeting FGFR2 and FGFR3. It exhibits IC50 values of 3.7 nM for FGFR2 and 31.2 nM for FGFR3, with a pre-incubation time of 1 hour. FGFR2/3-IN-2 demonstrates selectivity over FGFR1/4 and other kinases, and does not cause diarrhea or increased serum phosphate in vivo. In the SNU-16 gastric cancer model, FGFR2/3-IN-2 can induce tumor stasis or regression.

DGY-06-116 is an selective and irreversible covalent inhibitor of Src and FGFR1 with IC50 value of 3nM and 8340 nM, respectively.

SSR128129E (SSR) is an allosteric and orally-active FGFR1 inhibitor (IC50: 1.9 μM), but not affecting other related RTKs.

FIIN-1 (FGFR irreversible inhibitor-1) is an irreversible and selective FGFR inhibitor with Kd of 2.8, 6.9, 5.4, 120, 32 and 120 nM for FGFR1, FGFR2, FGFR3,

PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R).

Aprutumab, a human FGFR2 monoclonal antibody, targets FGFR2-IIIB/C and is used in antibody-drug conjugates.

R1530 is a multikinase inhibitor with antineoplastic and antiangiogenesis activities.

TYRA-300 is an oral and selective FGFR3 inhibito, in the Ba/F3 cell line for the treatment of metastatic uroepithelial carcinomas (mUCs) and chondrodysplasia.

KHS101 is a TACC3 inhibitor and can selectively induce a neuronal differentiation phenotype.

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM.

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

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.

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor(KDR, Flt-1, FGFR1 and PDGFRα with IC50s of 4nM, 20nM, 4nM, 2 nM ,respectively)

FGFR4-IN-16 (CY-15-2) is a covalent inhibitor targeting FGFR-4, utilized in cancer research [1].

Rogaratinib (BAY1163877) is an aberrant inhibitor of fibroblast growth factor receptor (FGFR).

FGFR2-IN-3 is an orally active selective FGFR2 inhibitor[1].

Orantinib (NSC 702827) , a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation.