1820787-94-7

1820787-94-7 structure

Name: IRAK4-IN-1
Chemical Name: IRAK4-IN-1
CAS Number: 1820787-94-7
Molecular Formula: C₁₉H₂₃N₅O
Molecular Weight: 337.42
Catalog: Signaling Pathways Immunology/Inflammation IRAK
Create Date: 2018-05-30 19:02:10
Modify Date: 2024-01-11 12:41:11
IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.

Name	IRAK4-IN-1

Description	IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> IRAK Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IRAK Research Areas >> Inflammation/Immunology
Target	IC50: 7 nM (IRAK4)[1]
In Vitro	The in vitro metabolic stability profiles of IRAK4-IN-1 (Compound 23) is measured, with EC50 of 2300 nM for the rat whole blood (RWB) [1].
In Vivo	Oral pharmacokinetic studies of IRAK4-IN-1 (Compound 23) show it to have high bioavailability of 73% and low plasma clearance(Clp=22 mL/min/kg) leading to a reasonable half-life of 1.3 h[1].
Animal Admin	Rats[1] In the TLR driven in vivo model, female Lewis rats are dosed with either vehicle or IRAK4-IN-1 (Compound 23; 3, 10, 30, and 100 mg/kg; p.o.) dosed at 1 h prior to stimulation with Resiquimod, R848 (5 mg/kg, IP). At 1.5 h post R848 stimulation, blood samples are obtained from the animals and cytokine levels are measured.
References	[1]. Smith GF, et al. Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2721-2726.