AZ1495

• CAT Number: I019539
• CAS Number: 2196204-23-4
• Molecular Formula: C₂₁H₃₁N₅O₂
• Molecular Weight: 385.5
• Purity: ≥95%
• Target: IRAK
• IUPAC Name: N-(4-morpholin-4-ylcyclohexyl)-5-(oxan-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
• InChI: 1S/C21H31N5O2/c1-3-17(26-7-11-28-12-8-26)4-2-16(1)25-21-19-18(15-5-9-27-10-6-15)13-22-20(19)23-14-24-21/h13-17H,1-12H2,(H2,22,23,24,25)
• InChIKey: DJVYXMINSBMUHH-UHFFFAOYSA-N
• SMILES: C1CC(CCC1NC2=NC=NC3=C2C(=CN3)C4CCOCC4)N5CCOCC5

AZ1495 (Cat No.: I019539) is a potent, orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4), exhibiting an IC50 of 5 nM. It also inhibits IRAK1 with an IC50 of 23 nM. AZ1495 has demonstrated efficacy in preclinical studies, particularly against diffuse large B-cell lymphoma (DLBCL) with the MYD88L265P mutation. In combination with the Bruton’s tyrosine kinase (BTK) inhibitor ibrutinib, AZ1495 led to tumor regression in an ABC-DLBCL mouse model. These findings suggest its potential as a therapeutic agent for certain lymphomas.

Reference

[1]. Scott JS, et al. Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma. J Med Chem. 2017 Dec 28;60(24):10071-10091.