ZM 306416 (CB 676475), a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).

KDR:100 nM, EGFR:<10 nM, VEGFR1:0.33 μM, FLT1:2 μM

When acting on human thyroid follicular cells, ZM306416 (1 μM) decreased nuclear distribution and increased follicle formation; a significant increase in cell death was observed at 3 μM.ZM306416 weakly inhibited VEGF secretion and increased PlGF production.ZM306416 (<10 μM) had a significant inhibitory effect on steady-state phosphorylation of p42/44 MAPK but had no effect on the non phosphorylated forms, but had no effect on the expression of non-phosphorylated forms. In human thyroid follicular cells, ZM306416 (300 nM) completely inhibited PAA secretion, stimulated [125I] uptake, and silenced pVEGFR2 (Y1214) expression. ZM-306416 exhibited selective antiproliferative effects (IC50: 0.09 μM and 0.072 μM) when acting on the epidermal growth factor receptor-naïve non-small cell (type) lung cancer cell lines H3255 and HCC4011. When acting on GeneBLAzer T-Rex RORγ-UAS-bla HEK293T cell line, ZM-306416 had a significant inhibitory effect on ERRα assay (IC50: 7.3 μM).ZM-306416 inhibited granule formation (IC50: 0.67 μM).