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.

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

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.

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]

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.

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

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

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

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).

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.

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

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.

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.

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.

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

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

EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50 values of 6 nM, 2 nM, and 4 nM for FGFR1, VEGFR2, and Tie-2, respectively.

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.

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]

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

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.

PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.

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.

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.

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.

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.

PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 = 0.18 µM)

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

LY2784544(Gandotinib (LY2784544)) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3.

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.

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.

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.

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

Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.

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).

Mubritinib (TAK-165) (TAK-165) is a potent inhibitor of HER2 ErbB2 with IC50 of 6 nM.

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.

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.

ZM323881 hydrochloride (ZM 323881 HCl) is a potent and selective VEGFR2 inhibitor.

2,5-Dihydroxybenzoic acid (Gentisic acid) is an active metabolite of salicylic acid degradation with a broad spectrum of biological activity, such as anti-inflammatory, antirheumatic and antioxidant properties.

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

TAK-632, a potent pan-Raf inhibitor (GenScript, 2020), is characterized by its molecular weight [M] for [C 22 H 19 FN 2 O 2] of 362.4 by LC-MS, with a purity of 99% (HPLC). The compound exhibits white to off-white solid form and has a melting point [M] ranging from 178°C to 182°C (GenScript, 2020). Its solubility profile includes DMSO, in which it is soluble to 100mM (GenScript, 2020).

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.

KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.

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.