AVL-292

AVL-292 is a covalent inhibitor of Bruton's tyrosine kinase (BTK, IC50 = 5.9 nM). It is selective for BTK over a panel of 61 kinases when used at a concentration of 1 µM but does inhibit the additional Tec family kinases BMX, Itk, Tec, and TXK (IC50s = 0.7, 36, 6.2, and 8.9 nM, respectively). AVL-292 inhibits naïve human B cell proliferation (EC50 = 3 nM). It reduces joint damage, pannus formation, cartilage degradation, and bone erosion in a mouse model of rheumatioid arthritis induced by collagen when used at doses of 3, 10, and 30 mg/kg.Formal Name: N-[3-[[5-fluoro-2-[[4-(2-methoxyethoxy)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-2-propenamide. CAS Number: 1202757-89-8. Synonyms: CC-292, Spebrutinib. Molecular Formula: C22H22FN5O3. Formula Weight: 423.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:30): 0.03 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 271 nm. SMILES: FC(C(NC1=CC(NC(C=C)=O)=CC=C1)=N2)=CN=C2NC3=CC=C(OCCOC)C=C3. InChi Code: InChI=1S/C22H22FN5O3/c1-3-20(29)25-16-5-4-6-17(13-16)26-21-19(23)14-24-22(28-21)27-15-7-9-18(10-8-15)31-12-11-30-2/h3-10,13-14H,1,11-12H2,2H3,(H,25,29)(H2,24,26,27,28). InChi Key: KXBDTLQSDKGAEB-UHFFFAOYSA-N.