fgfr1 autophosphorylation

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

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. It also inhibits the PDGFR, EGFR, and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively.

Orantinib (NSC 702827) , a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little effect against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2 and does not suppresses EGFR.

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)

Anti-FGFR1/CD331 Antibody is a humanized monoclonal antibody targeting fibroblast growth factor receptor 1 (FGFR1/CD331). FGFR1 is a member of the receptor tyrosine kinase (RTK) family, playing a pivotal role in regulating cell proliferation, survival, migration, and angiogenesis. This antibody specifically binds to the extracellular domain of FGFR1, competitively blocking FGF ligand binding and subsequently inhibiting receptor autophosphorylation and the activation of downstream signaling pathways such as MAPK/ERK and PI3K/Akt. This mechanism effectively suppresses tumor growth and pathological hyperplasia driven by aberrant FGFR1 signaling, making it a valuable tool in research on solid tumors and the development of targeted cancer therapies.