IRAK4-IN-14 (compound 28) 是一种有效的、选择性的、具有口服活性的IRAK4抑制剂，IC50为 0.003 μM。IRAK4-IN-14 在大鼠和小鼠中显示出良好的 PK 参数。IRAK4-IN-14 与 Acalabrutinib 联合使用对 MyD88/CD79 双突变体 ABC-DLBCL 具有协同体外活性。

IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC 50 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 [1].

IRAK4-IN-14 (compound 28) shows cell pIRAK4 potencies with an IC 50 of 0.11 μM [1]. IRAK4-IN-14 (compound 28) shows selectivity with IC 50 s 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 [1].

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]. parameter Value A2B P app 31 Efflux ratio 1.4 Solubility (μM) 800 Rat/mouse/monkey/human %free 21/16/33/21 Rat LM/H CL int 16/5.6 Mouse LM/H CL int 13/11 Minipig LM/H CL int 18/8.2 Dog LM/H CL int 21/4.5 Monkey LM/H CL int 35/4.7 Rat CL 15 Vd ss 4.3 t 1/2 5.2 F% 55% Mouse CL 17 Vd ss 4.1 t 1/2 4.2 F% 66% Monkey CL 68 Vd ss 8.6 t 1/2 1.4 Male Han Wistar rats; 1 mg/kg i.v.; 2 mg/kg p.o.; Male CD1 mice; 0.5 mg/kg i.v.; 1 mg/kg p.o.; Male Cynomolgus monkeys; 1 mg/kg i.v. [1].

2667681-71-0

C25H28FN9O

489.55

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years