PDGFR酪氨酸激酶抑制剂III是酪氨酸激酶PDGFR家族的细胞可渗透，有效，选择性和ATP竞争性抑制剂（PDGFR-α为IC | 50 | = 50 nM，PDGFR-β为80 nM，PDGFR-β为50 nM c-Kit，Flt-3 / Flk-2为230 nM）。PDGFR酪氨酸激酶抑制剂III仅在更高浓度下（EGFR，FGFR，Src，PKA和PKC的IC50>30μM）才抑制其他激酶的活性。有报道阻止PDGF-BB诱导的猪主动脉平滑肌细胞增殖（IC | 50 | = 250 nM）。 PDGFR Tyrosine Kinase Inhibitor III is a cell-permeable, potent, selective, and ATP-competitive inhibitor of the PDGFR family of tyrosine kinases (IC|50|= 50 nM for PDGFR-α, 80 nM for PDGFR-β, 50 nM for c-Kit, and 230 nM for Flt-3/Flk-2). PDGFR Tyrosine Kinase Inhibitor III inhibits the activities of other kinases only at much higher concentrations (IC50 > 30μM for EGFR, FGFR, Src, PKA, and PKC). Reported to block PDGF-BB-induced proliferation of porcine aorta smooth muscle cells (IC|50|= 250 nM).