Denfivontinib

G-749 is a potent, oral active and ATP competitive FLT3 inhibitor, with IC₅₀s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. G-749 can be used for the research of drug resistance for acute myeloid leukemia (AML)^[1]. IC50 & Target:IC50: 0.4 nM (FLT3-WT), 0.6 nM (FLT3-D835Y)^[1] In Vitro: G-749 shows potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays^[1].
G-749 inhibits autophosphorylation of FLT3 with an IC₅₀ value of ≤8 nM in FLT3-WT bearing RS4-11 and in FLT3-ITD harboring MV4-11 and Molm-14 cells^[1].
G-749 (0.0001-10 nM; 72 hours) shows strong antiproliferation of leukemia cells addicted to FLT3-ITD (MV4-11 and Molm-14) in a dose-dependent manner^[1].
G-749 (25-100 nM; 36 hours) causes antiproliferative activity through apoptosis^[1].
G-749 (1.6-1000 nM; 2 hours) shows more potent inhibition of p-FLT3, p-ERK1/2, and p-AKT than AC220 and PKC412^[1].
In Vivo: G-749 (3-30 mg/kg; p.o.; daily; for 28 days) shows effective antitumor activity in mouse models^[1].