IRAK4-IN-15

Names

[ CAS No. ]:
2667681-85-6

[ Name ]:
IRAK4-IN-15

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Immunology/Inflammation >> IRAK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IRAK

[Target]

IRAK4:0.002 μM (IC50)


[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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H29FN10

[ Molecular Weight ]:
488.56

Related Compounds