IRAK4-IN-15

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IRAK4-IN-15 

IRAK4-IN-15 (compound 35) 是一种有效的选择性 IRAK4 抑制剂,IC50 为 0.002 µM。IRAK4-IN-15 显示出良好的人类 PK 预测且具有低内在清除率。IRAK4-IN-15 与 Acalabrutinib 联用显示出对 MyD88/CD79 双突变体 ABC-DLBCL 的显著协同体外活性。

IRAK4-IN-15

IRAK4-IN-15 Chemical Structure

CAS No. : 2667681-85-6

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生物活性

IRAK4-IN-15 (compound 35) is a potent and selective IRAK4 inhibitor with an IC50 of 0.002 µM. IRAK4-IN-15 shows good human PK predictions with low intrinsic clearance. IRAK4-IN-15 shows great synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib. [1].

IC50 & Target[1]

IRAK4

0.002 μM (IC50)

体外研究
(In Vitro)

IRAK4-IN-15 (compound 35) shows cell pIRAK4 potencies with an IC50 of 0.21 µM[1].
IRAK4-IN-15 (compound 35) shows selectivity with IC50s of 0.002,1.2, >10,1.5, 0.23, 0.48, 0.93, 0.57 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.

分子量

488.56

Formula

C25H29FN10

CAS 号

2667681-85-6

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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