IRAK4-IN-13

Names

[ CAS No. ]:
2667681-57-2

[ Name ]:
IRAK4-IN-13

Biological Activity

[Description]:

IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg[1].

[Related Catalog]:

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

[Target]

IRAK4:0.6 nM (IC50)


[In Vitro]

IRAK4-IN-13 (compound 21) shows cell pIRAK4 potencies with an IC50 of 0.024 µM[1]. IRAK4-IN-13 (compound 21) shows selectivity with IC50s of 0.0006, 0.002, 0.044, 1.2, 0.018, 0.019, 0.082, 0.036 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 ]:
C24H27N9O

[ Molecular Weight ]:
457.53

Related Compounds