IRAK4-IN-14

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

IRAK4-IN-14 

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

IRAK4-IN-14 Chemical Structure

CAS No. : 2667681-71-0

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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[1].

IC50 & Target[1]

IRAK4

0.003 μM (IC50)

体外研究
(In Vitro)

IRAK4-IN-14 (compound 28) shows cell pIRAK4 potencies with an IC50 of 0.11 µM[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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 Papp 31
Efflux ratio 1.4
Solubility (µM) 800
Rat/mouse/monkey/human %free 21/16/33/21
Rat LM/H CLint 16/5.6
Mouse LM/H CLint 13/11
Minipig LM/H CLint 18/8.2
Dog LM/H CLint 21/4.5
Monkey LM/H CLint 35/4.7
Rat CL 15
Vdss 4.3
t1/2 5.2
F% 55%
Mouse CL 17
Vdss 4.1
t1/2 4.2
F% 66%
Monkey CL 68
Vdss 8.6
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.[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

489.55

Formula

C25H28FN9O
CAS 号

2667681-71-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Degorce SL, et al. Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors. Bioorg Med Chem. 2020 Dec 1;28(23):115815.

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