IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib.
靶点:
IRAK4:0.003 μM (IC50)
体外研究:
IRAK4-IN-14 (i.v. or p.o.) shows good PK parameters with oral bioavailability of 66% for mouse[1]. Pharmacokinetic Parameters of IRAK4-IN-14 in Male Han Wistar rats, male CD1 mice, male Cynomolgus monkeys[1].
体内研究:
IRAK4-IN-14 (compound 28) shows cell pIRAK4 potencies with an IC50 of 0.11 µM. IRAK4-IN-14 (compound 28) shows selectivity with IC50s of 0.003,1.4, >8, >9, 0.053, 0.27, 0.76, 0.27 µM for IRAK4, IRAK1, BTK, Flt3, PI3Kδ, TRKa, TRKb, TRKc, respectively.