IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride is an orally active, potent and selective IRAK / pan-FLT3 kinase inhibitor with IC50 s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively. IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride can be used for research on AML [1].
In Vivo, IRAK1/4/pan-FLT3 Kinase-IN-1 (Compound 31) (10 mg/kg; i.p.; 5th a week) hydrochloride produces significant prolongation of survival relative to vehicle in a mouse xenograft model of AML[1].
In Vitro, IRAK1/4/pan-FLT3 Kinase-IN-1 (Compound 31) hydrochloride exhibits Kds of 0.53 nM, 0.096 nM and 0.074 nM against IRAK1, IRAK4 and FLT3, respectively[1]. IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride exhibits IC50s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively[1]. IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride inhibits phosphorylation of FLT3 or IRAK substrates in MOLM14 (D835Y) or THP1 cells[1].
In Vivo, IRAK1/4/pan-FLT3 Kinase-IN-1 (Compound 31) (10 mg/kg; i.p.; 5th a week) hydrochloride produces significant prolongation of survival relative to vehicle in a mouse xenograft model of AML[1].
In Vitro, IRAK1/4/pan-FLT3 Kinase-IN-1 (Compound 31) hydrochloride exhibits Kds of 0.53 nM, 0.096 nM and 0.074 nM against IRAK1, IRAK4 and FLT3, respectively[1]. IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride exhibits IC50s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively[1]. IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride inhibits phosphorylation of FLT3 or IRAK substrates in MOLM14 (D835Y) or THP1 cells[1].