产品
编 号：F754480
分子式：C25H28FN9O
分子量：489.55
分子式：C25H28FN9O
分子量：489.55
产品类型
规格
价格
是否有货
结构图
CAS No: 2667681-71-0
产品详情
生物活性：
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.
体内研究：
IRAK4-IN-14 (i.v. or p.o.) shows good PK parameters with oral bioavailability of 66% for mouse.Pharmacokinetic Parameters of IRAK4-IN-14 in Male Han Wistar rats, male CD1 mice, male Cynomolgus monkeys.parameterValue
A2B Papp 31
Efflux ratio 1.4
Solubility (μM) 800
Rat/mouse/monkey/human %free21/16/33/21
Rat LM/H CLint 16/5.6
Mouse LM/H CLint13/11
Minipig LM/H CLint 18/8.2
Dog LM/H CLint 21/4.5
Monkey LM/H CLint 35/4.7
Rat CL15
Vdss4.3
t1/2 5.2
F%55%
Mouse CL17
Vdss4.1
t1/2 4.2
F%66%
Monkey CL68
Vdss8.6
t1/2 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..
体外研究：
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.
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.
体内研究：
IRAK4-IN-14 (i.v. or p.o.) shows good PK parameters with oral bioavailability of 66% for mouse.Pharmacokinetic Parameters of IRAK4-IN-14 in Male Han Wistar rats, male CD1 mice, male Cynomolgus monkeys.parameterValue
A2B Papp 31
Efflux ratio 1.4
Solubility (μM) 800
Rat/mouse/monkey/human %free21/16/33/21
Rat LM/H CLint 16/5.6
Mouse LM/H CLint13/11
Minipig LM/H CLint 18/8.2
Dog LM/H CLint 21/4.5
Monkey LM/H CLint 35/4.7
Rat CL15
Vdss4.3
t1/2 5.2
F%55%
Mouse CL17
Vdss4.1
t1/2 4.2
F%66%
Monkey CL68
Vdss8.6
t1/2 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..
体外研究：
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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备