Emavusertib

Emavusertib is an inhibitor of IL-1 receptor-associated kinase 4 (IRAK4, IC50 = 31.7 nM). It is selective for IRAK4 over FMS-related tyrosine kinase 3 (FLT3), cyclin-dependent kinase 2 (Cdk2), Aurora A kinase, glycogen synthase kinase 3beta (GSK3beta), 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.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. CAS Number: 1801344-14-8. Synonyms: CA-4948. Molecular Formula: C24H25N7O5. Formula Weight: 491.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 260, 345 nm. SMILES: O=C(C1=COC(C2=CC=NC(C)=C2)=N1)NC3=C(N4CC[C@@H](O)C4)N=C5C(OC(N6CCOCC6)=N5)=C3. InChi Code: InChI=1S/C24H25N7O5/c1-14-10-15(2-4-25-14)23-27-18(13-35-23)22(33)26-17-11-19-20(28-21(17)31-5-3-16(32)12-31)29-24(36-19)30-6-8-34-9-7-30/h2,4,10-11,13,16,32H,3,5-9,12H2,1H3,(H,26,33)/t16-/m1/s1. InChi Key: SJHNWSAWWOAWJH-MRXNPFEDSA-N.