FGFR

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4 5.2 nM). Lenvatinib has strong anti-tumor activity.

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 37 108 nM), PDGFRα, and PDGFRβ (IC50=59 65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.

Heparan sulfate is a natural product, a linear polysaccharide. Heparan sulfate occurs as a proteoglycan (HSPG) that is tightly attached to cell surface or extracellular matrix proteins.

Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor targeting VEGFR1 2 3, FGFR1 2 3, and PDGFRα β.

TYRA-300 is an oral and selective FGFR3 inhibitor with an IC50 value of 11 nM and 25-fold, 14-fold, and 36-fold selectivity for FGFR1, FGFR2, and FGFR4, respectively, in the Ba F3 cell line for the treatment of metastatic uroepithelial carcinomas (mUCs) and chondrodysplasia.

Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFRα), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src).

Pemigatinib (INCB054828) is an orally active, selective inhibitor of FGFR, with IC50 values of 0.4 nM for FGFR1, 0.5 nM for FGFR2, 1.2 nM for FGFR3, and 30 nM for FGFR4.

Sulfatinib (KDR-IN-1) (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1 2 3, FGFR1 and CSF1R with IC 50 s ranging from 1 to 24 nM.

Infigratinib (NVP-BGJ398) (BGJ398) is an orally bioavailable pan FGFR inhibitor (IC50: 0.9 1.4 1 nM for FGFR1 2 3), >40-fold selective for FGFR versus FGFR4 and VEGFR2.

Lenvatinib mesylate (E7080 (mesylate)) is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.

Gunagratinib (ICP-192) is an orally active and highly effective pan-FGFR (fibroblast growth factor receptor) inhibitor, used in studies of FGFR-related diseases.

Erdafitinib (JNJ-42756493), a quinoxaline derivative, targets FGFR1 2 3 4.

PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.

Fisogatinib (BLU-554) is a highly potent, selective and orally active FGFR4 inhibitor with an IC50 value of 5 nM and significant anti-tumor activity in hepatocellular carcinoma models dependent on FGFR4 signaling.

Aprutumab (BAY 1179470) is a human FGFR2 monoclonal antibody with affinity to FGFR2 isoforms FGFR2-IIIB and FGFR2-IIIC. Aprutumab is commonly used to synthesize antibody-drug conjugates.

Resigratinib (KIN-3248) is a FGFR tyrosine kinase inhibitor exhibiting antineoplastic activity [1].

Futibatinib (TAS-120) is an orally active, potent, selective, highly bioavailable, and irreversible FGFR inhibitor with IC50 values ​​of 3.9, 1.3, 1.6, and 8.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. [2]

AZD4547 is an FGFR family inhibitor. AZD4547 selectively inhibits FGFR1 phosphorylation and suppresses cancer cell proliferation through inhibition of FGFR1 signaling, and is able to act on FGFR1 (IC50:0.2 nM), FGFR2 (IC50:2.5 nM), FGFR3 (IC50:1.8 nM) and FGFR4 (IC50:165 nM). IC50:165 nM).[2]

Fazpilodemab (BFKB8488A) is a fully humanized bispecific antibody selectively targeting and activating the Klotho β and fibroblast growth factor receptor 1c receptor complex, which can be used to study non-alcoholic fatty liver disease (NAFLD).

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

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

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

Dovitinib is an orally active, multi-targeted tyrosine kinase (RTK) inhibitor with anti-tumor effects.

Ferulic Acid (Coniferic acid) is a highly abundant phenolic phytochemical and a type of organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong.It can be absorbed by the small intestine and excreted through the urine.

Brivanib (BMS-540215) is an ATP-competitive inhibitor targeting VEGFR2 with an IC50 of 25 nM, exhibiting moderate potency against VEGFR-1 and FGFR-1, and over 240-fold selectivity against PDGFR-β. Phase 3.

Dovitinib lactate hydrate (TKI258) is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3 c-Kit) with IC50 of 1 nM 2 nM, also potent to class IV (FGFR1 3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

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

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor that acts on KDR, Flt-1, FGFR1, and PDGFRα with IC50 values of 4 nM, 20 nM, 4 nM, and 2 nM, respectively.

Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.

Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms (IC50=10 30 47 84 74 140 146 nM). Pazopanib has antitumor activity.

Roblitinib (FGF-401) is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4) with potential antineoplastic activity. Upon administration, Roblitinib binds to and inhibits FGFR4, leading to the inhibition of tumor cell proliferation in FGFR4-overexpressing cells. It is a receptor tyrosine kinase upregulated in certain tumor cells and involved in proliferation, differentiation, angiogenesis, and survival.

Lucitanib (E-3810) is a novel and potent inhibitor of VEGFR and FGFR, selectively targeting VEGFR1, VEGFR2, VEGFR3, FGFR1, and FGFR2 with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.

Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

Pazopanib Hydrochloride (Votrient HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.

SU11274 (Met Kinase Inhibitor)(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2.

FGFR1 DDR2 inhibitor 1 is an inhibitor of discoidin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM, and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

Ponatinib Hydrochloride (AP-24534 Hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

BLU9931 is the first selective small molecule inhibitor of FGFR4.

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

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 (CSF1R), Ret and Yes.

Derazantinib (ARQ-087) is a potent, ATP-competitive, orally active tyrosine kinase inhibitor with IC50 values ​​of 4.5 1.8 4.35 3.4 nM for chondrocyte FGFR1 FGFR2 FGFR3 FGFR4, respectively.

Tinengotinib is a multikinase inhibitor targeting a series of kinases involved in cancer cell proliferation, angiogenesis, and regulation of immune response, including Aurora kinase A B, Janus kinase (JAK1 2), fibroblast growth factor receptor (FGFR1 2 3), vascular endothelial growth factor receptors (VEGFRs), and other tyrosine kinases. Tinengotinib has shown good tolerability and preliminary efficacy in clinical trials in a variety of advanced solid tumors.

Masitinib mesylate (AB-1010 mesylate) is a selective, orally bioavailable c-Kit inhibitor with an IC50 of 200 nM for human recombinant c-Kit, and IC50 values of 540 800 nM and 510 nM for PDGFRα β and LynB, respectively.

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

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

R1530 is a multikinase inhibitor with antineoplastic and antiangiogenesis activities.

CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.

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