KBP-7018

KBP-7018 is an orally active, tyrosine kinase-selective multi-kinase inhibitor with an IC₅₀ value of 10 nM against c-KIT, 7.6 nM against RET, and 25 nM against human PDGFR. KBP-7018 improves survival rates in a mouse model of pulmonary fibrosis. KBP-7018 can be used in research related to idiopathic pulmonary fibrosis^[1][2]. IC50 & Target:IC50: c-KIT (10 nM), PDGFR (7.6 nM), and RET (25 nM)^[1].
In Vitro:KBP-7018 potently and selectively inhibits c-KIT (IC₅₀ = 10 nM), RET (IC₅₀ = 7.6 nM) and PDGFR (IC₅₀ = 25 nM) in cell-free kinase assays. Meanwhile, it shows extremely weak inhibitory activity against hERG K⁺ and exhibits high kinome selectivity^[1].
KBP-7018 inhibits h-PDGF-bb-stimulated proliferation of 3T3 fibroblasts in cell-based assays, with an IC₅₀ of 100 nM^[1].
KBP-7018 potently inhibits purified PDGFRα (IC₅₀ = 26 nM) and PDGFRβ (IC₅₀ = 34 nM)^[2].
KBP-7018 (0.05-80 μM; 10 min) potently inhibits human CYP3A4 (testosterone probe, IC₅₀ = 0.087 μM), weakly inhibits human CYP2C9 (IC₅₀ = 35.2 μM), and shows no inhibitory effect on human CYP1A2, CYP2C19 or CYP2D6 at concentrations up to 80 μM^[2]. In Vivo:KBP-7018 (10-100 mg/kg; p.o.; once daily; for 28 consecutive days) dose-dependently improves the 28-day survival rate of Bleomycin (HY-108345)-induced pulmonary fibrosis model in C57 mice^[1].