Formulation: A solid
Formal Name: N-[5-[(3R)-3-hydroxy-1-pyrrolidinyl]-2-(4-morpholinyl)oxazolo[4,5-b]pyridin-6-yl]-2-(2-methyl-4-pyridinyl)-4-oxazolecarboxamide
Purity: ≥98%
Formula Markup: C24H25N7O5
Formula Weight: 491,5
Shelf life (days): 1460
CAS Number: 1801344-14-8
Notes: Emavusertib is an inhibitor of IL-1 receptor-associated kinase 4 (IRAK4; IC50 = 31.7 nM).{62802} It is selective for IRAK4 over FMS-related tyrosine kinase 3 (FLT3), cyclin-dependent kinase 2 (Cdk2), Aurora A kinase, glycogen synthase kinase 3β (GSK3β), and muscle-associated receptor tyrosine kinase (MUSK) at 1 µM. Emavusertib inhibits IL-6 release mediated by toll-like receptor 2 (TLR2), TLR5, or IL-1 receptor (IL-1R) in isolated human whole blood (IC50s = 989, 696, and 1,375 nM, respectively). In vivo, emavusertib (25-200 mg/kg) reduces tumor volume in an OCI-Ly3 diffuse large B cell lymphoma (DLBCL) mouse xenograft model.
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