Fibroblast Growth Factor Receptor (FGFR)

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

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

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

<p>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</p>

<p>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.</p>

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

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

<p>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).</p>

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

<p>Triamcinolone acetonide (Azmacort) is a Corticosteroid.</p>

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

<p>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.</p>

<p>Bemarituzumab: humanized IgG1 antibody inhibits FGFR2b, may be used in cancer research.</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>FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor with potent binding affinity, exhibiting an IC50 of 0.85 nM.</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>Vofatamab (B-701) is a fully human monoclonal antibody targeting FGFR3, often used in combination with other compounds to treat cancer.</p>

<p>FGFR1/VEGFR2-IN-1 (compound 2b) is an inhibitor of both FGFR1 and VEGFR2, applicable in cancer research [1].</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>Efruxifermin, a modified FGF21 with IgG1 Fc, has increased stability and affinity. Used in non-alcoholic steatohepatitis research.</p>

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

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

<p>A unique collection of 1016 tyrosine kinase inhibitors for high throughput screening and high content screening for drug discovery in tyrosine kinase related</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>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>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>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>U3-1784 is a humanized monoclonal antibody targeting CD334, with anti-cancer activity, used in liver cancer research.</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>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>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.</p>

<p>LC-MB12 is a PROTAC FGFR2 compound that degrades FGFR2 and can be used to study gastric 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>(Z)-Orantinib, oral ATP-competitive blocker for Flk-1/KDR, PDGFRβ, FGFR1 (IC50: 2.1, 0.008, 1.2 μM), is a strong antiangiogenic, antitumor drug.</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>

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

<p>Dovitinib lactate (TKI-258 lactate)(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).</p>

<p>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/</p>

<p>PD-166866 is a selective FGFR tyrosine kinase inhibitor.</p>

<p>BO-264 is a highly potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3, IC50 of 188 nM and a Kd of 1.5 nM).</p>

<p>JK-P3: a pyrazole inhibitor of VEGFR-2 (IC50: 7.8 μM), stalls FGFR 1/3 in vitro, halts HUVEC wound healing/tube formation, not cell growth.</p>

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

<p>Roblitinib (FGF-401), an FGFR4 inhibitor, potentially blocks tumor growth by halting cell proliferation and survival.</p>

<p>SU4984 is a cell-permeable, ATP-competitive and reversible inhibitor of the fibroblast growth factor receptor 1 (FGFR1).</p>

<p>BLU9931 is the first selective small molecule inhibitor of FGFR4.</p>

<p>Heparan sulfate is a natural product, a linear polysaccharide. Heparan sulfate occurs as a proteoglycan (HSPG). Cost effective and quality assured.</p>

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

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

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

<p>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).</p>

<p>FIIN-3 is an irreversible inhibitor of FGFR.</p>

<p>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</p>

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

<p>LY2784544(Gandotinib (LY2784544)) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM).</p>

<p>FGFR2-IN-3 hydrochloride is a selective, orally active FGFR2 inhibitor.</p>

<p>Dovitinib lactate hydrate (TKI258) is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit).</p>

<p>KHS101 is a TACC3 inhibitor and can selectively induce a neuronal differentiation phenotype.</p>

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

<p>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;</p>

<p>KHS101 is a novel inhibitor of transforming acidic coiled-coil protein 3 (TACC3). It is a selective inducer of neuronal differentiation.</p>

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

<p>S49076 HCl (S-49076 Hydrochloride) is an effective inhibitor of MET, AXL/MER, and FGFR1/2/3.</p>

<p>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).</p>

<p>R1530 is a multikinase inhibitor with antineoplastic and antiangiogenesis activities.</p>

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

<p>Alofanib (RPT835) selectively inhibits FGFR2 in KATO III cells with IC50 &lt;10 nM; doesn’t affect FGFR1/3 or FGF2-FGFR2 binding.</p>

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

<p>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.</p>

<p>Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β</p>

<p>FIIN-2, an irreversible, pan-FGFR inhibitor, inhibits FGFR1/2/3/4 with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM, respectively.</p>

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

<p>LY2874455 has been used in trials studying the treatment of Advanced Cancer.</p>

<p>Erdafitinib (JNJ-42756493) is a quinoxaline derivative compound, acts on FGFR1/2/3/4.</p>

<p>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.</p>

<p>AZD4547 is an FGFR family inhibitor, and is able to act on FGFR1, FGFR2, FGFR3 and FGFR4. IC50:165 nM).Cost-effective and quality-assured.</p>

<p>CHIR-98014 (CT98014) is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.</p>

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

<p>SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.</p>

<p>FGFR4-IN-1 is a potent FGFR4 inhibitor (IC50: 0.7 nM).</p>

<p>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.</p>

<p>SUN11602, an aniline compound, mimics the neuroprotective mechanisms of basic fibroblast growth factor.</p>

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

<p>Dovitinib is an orally active, multi-targeted tyrosine kinase (RTK) inhibitor with anti-tumor effects.Cost-effective and quality-assured.</p>

<p>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）</p>

<p>Zoligratinib (CH5183284) is a selective and orally available FGFR inhibitor, which is for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.</p>

<p>Infigratinib (NVP-BGJ398) (BGJ398) is an orally bioavailable pan FGFR inhibitor (IC50: 0.9/1.4/1 nM for FGFR1/2/3), &gt;40-fold selective for FGFR versus FGFR4 and</p>

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

<p>PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (</p>

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

<p>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</p>

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