2. Immunology/Inflammation
  3. IRAK
  4. 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。

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IRAK4-IN-14 Chemical Structure

IRAK4-IN-14 Chemical Structure

CAS No. : 2667681-71-0

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IRAK4-IN-14 相关抗体

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IRAK1 IRAK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IRAK4-IN-14 相关抗体:
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

489.55

Formula

C25H28FN9O
CAS 号
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.
纯度 & 产品资料
参考文献

IRAK4-IN-14 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IRAK4-IN-142667681-71-0IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseorally activeAcalabrutinibintrinsic clearanceMyD88/CD79ABC-DLBCLCaco2 cellsInhibitorinhibitorinhibit

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产品名称：
IRAK4-IN-14
目录号：
HY-146112
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