2170694-05-8

2170694-05-8 structure
2170694-05-8 structure
  • Name: IRAK4-IN-22
  • Chemical Name: IRAK4-IN-22
  • CAS Number: 2170694-05-8
  • Molecular Formula: C28H28FN7O2
  • Molecular Weight: 513.57
  • Catalog: Signaling Pathways Immunology/Inflammation IRAK
  • Create Date: 2022-10-13 22:02:37
  • Modify Date: 2024-01-30 22:40:37
  • IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].

Name IRAK4-IN-22
Description IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].
Related Catalog
In Vitro IRAK4-IN-21 (a 4-fold serial dilution from 10 µM; 1 h) decreases the levels of IL-23 (in THP-1 and DC cells), IL-6 (in HUVEC cells) and MIP-1β (in human whole blood)[1]. Cell Viability Assay[1] Cell Line: THP-1, DC cells (are primed with IFN-γ) Concentration: 10 µM (a 4-fold serial dilution from 10 µM) Incubation Time: 1 h (pre-incubate) Result: Inhibited the levels of IL-23 in the supernatant of THP-1 and DC cells with IC50 of 0.10 and 0.11 µM, respectively. Cell Viability Assay[1] Cell Line: HUVEC cells (IL-1β-stimulated) Concentration: 10 µM (a 4-fold serial dilution from 10 µM) Incubation Time: 1 h (pre-incubate) Result: Inhibited the level of IL-6 in the supernatant of HUVEC cells with an IC50 of 0.11 µM. Cell Viability Assay[1] Cell Line: Human whole blood (IL-1β-stimulated) Concentration: 10 µM (a 4-fold serial dilution from 10 µM) Incubation Time: 1 h (pre-incubate) Result: Inhibited the level of MIP-1β in the human whole blood with an IC50 of 0.51 µM.
In Vivo IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production[1]. Animal Model: BALB/c mice (acute mouse model; IL-1β-stimulated)[1]. Dosage: 75 mg/kg Administration: Oral administration; single (pre-treat). Result: Showed 64% inhibition of IL-6, plasma concentrations was 6817 ng/mL at 0.5 h and 700 ng/mL at 2 h.
References

[1]. Chen Y, et al. Discovery of 5-Aryl-2,4-diaminopyrimidine Compounds as Potent and Selective IRAK4 Inhibitors. ACS Med Chem Lett. 2022 Apr 4;13(4):714-719.

Molecular Formula C28H28FN7O2
Molecular Weight 513.57