FGFR2-IN-1 is an FGFR inhibitor that inhibits FGFR1, FGFR2, and FGFR3 with IC50s of 460, 140, and 2200 nM, respectively.FGFR2-IN-1 can be used for the study of cancers associated with FGFR2.CAS 번호13460-73-81-1

FGFR-IN-2 (compound 1) is a potent inhibitor of FGFR, acting on FGFR1 (IC50: 7.3 nM), FGFR2 (IC50: 4.3 nM), FGFR3 (IC50: 7.6 nM) and FGFR4 (IC50: 11 nM).

FGFR1 inhibitor-2 (with an IC50 of 4.55 μM in MDA-MB-231 cells) is a potent inhibitor of FGFR1. It is specifically useful for studying metastatic triple-negative breast cancer.

FGFR1/VEGFR2-IN-1 (compound 2b) is an inhibitor of both FGFR1 and VEGFR2, applicable in cancer research [1].

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.

FGFR2-IN-3 hydrochloride is a selective, orally active FGFR2 inhibitor.

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, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

FGFR3-IN-2 (compound 18b) is a potent and selective FGFR3 inhibitor that inhibits FGFR3 (IC50: 4.1 nM) and VEGFR2 (IC50: 570 nM).

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

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

AZD4547, a new-type specific FGFR inhibitor, targets for FGFR1/2/3 (IC50: 0.2/2.5/1.8 nM in cell-free assays).

Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR than PDGFRβ, lack of activity against InsR, EGFR, and FGFR. Semaxanib reversibly inhibits ATP binding to the tyrosine kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2), which may inhibit VEGF-stimulated endothelial cell migration and proliferation and reduce the tumor microvasculature.

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.

JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50: 7.8 μM). JK-P3 inhibits FGFR 1/3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endo

Multi-kinase-IN-2 is an orally active inhibitor of angiokinases. multi-kinase-IN-2 significantly inhibits the activity of angiokinases such as VEGFR-1/2/3, PDGFRα/β, FGFR-1, LYN and c-KIT kinases. -IN-2 significantly attenuates phosphorylation of AKT and ERK proteins, induces apoptosis and has anticancer effects.

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.

NSC 12 is an extracellular trap for fibroblast growth factor 2 (FGF2) that binds FGF2 (Kd = 51 μM) and interferes with its interaction with FGFR1, without affecting the ability of FGF2 to bind heparin or heparin sulfate proteoglycans (HSPGs). NSC 12 also binds several other, but not all, FGF isoforms with Kd values ranging between 16 and 120 μM, preventing them from forming HSPG/FGF/FGFR ternary complexes. NSC 12 inhibits FGF-dependent angiogenesis and tumor cell proliferation in vitro and reduces tumor growth in mice.

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

SUN11602, an aniline compound, mimics the neuroprotective mechanisms of basic fibroblast growth factor. It mimics the neuroprotective effects of bFGF and prevents glutamate-induced neuronal death. It also increases levels of CALB1 gene expression in cerebrocortical neurons and triggers phosphorylation of FGFR and ERK1/2.

S49076 HCl (S-49076 Hydrochloride) is an effective inhibitor of MET, AXL/MER, and FGFR1/2/3. S49076 HCl potently blocked cellular phosphorylation of MET, AXL, and FGFRs and inhibited downstream signaling in vitro and in vivo. In cell models, S49076 HCl inhibited the proliferation of MET- and FGFR2-dependent gastric cancer cells blocked MET-driven migration of lung carcinoma cells, and inhibited colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 HCl was established and correlated well with impact on tumor growth.

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).

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.

ARQ 069 (3.8-60 μM; for 2 hours) reduces the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin. ARQ 069 shows an affinity for FGFR2 of 5.2 μM. ARQ 069 inhibits FGFR phosphorylation in K

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.

Rogaratinib (BAY1163877) is an aberrant inhibitor of fibroblast growth factor receptor (FGFR). Rogaratinib is as an orally available, selective and potent inhibitor of FGFR-1, -2 and -3 kinase activity.

FGF/PDGF/VEGF RTK Inhibitor is a potent, reversible, atp-competitive inhibitor against pdgfrβ, fgfr-1, and vegfr-2 (ic50 = 20, 90, and 240 nm, respectively) and effectively suppresses vegf-stimulated proliferation of hmvecs (ec50 = 420 nm).