Zanubrutinib

Zanubrutinib is a potent and covalent inhibitor of Bruton's tyrosine kinase (BTK, IC50 = 0.3 nM). It is selective for BTK over a panel of 304 kinases at 1 µM but does inhibit EGFR, Tec, Blk, BMX, HER4, and TXK (IC50s = 0.62-33 nM). Zanubrutinib inhibits phosphorylation of BTK at Y233 (IC50 = 1.8 nM) in Ramos cells and reduces viability of REC-1 cells (IC50 = 0.36 nM). In vivo, zanubrutinib (2.5 and 7.5 mg/kg) reduces tumor volume in an OCI-LY10 diffuse large B cell lymphoma (DLBCL) mouse xenograft model.Formal Name: (7S)-4,5,6,7-tetrahydro-7-[1-(1-oxo-2-propen-1-yl)-4-piperidinyl]-2-(4-phenoxyphenyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide. CAS Number: 1691249-45-2. Synonyms: BGB-3111. Molecular Formula: C27H29N5O3. Formula Weight: 471.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml, DMSO: 5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 242 nm. SMILES: O=C(C=C)N1CCC([C@]2([H])CCNC3=C(C(N)=O)C(C4=CC=C(OC5=CC=CC=C5)C=C4)=NN32)CC1. InChi Code: InChI=1S/C27H29N5O3/c1-2-23(33)31-16-13-18(14-17-31)22-12-15-29-27-24(26(28)34)25(30-32(22)27)19-8-10-21(11-9-19)35-20-6-4-3-5-7-20/h2-11,18,22,29H,1,12-17H2,(H2,28,34)/t22-/m0/s1. InChi Key: RNOAOAWBMHREKO-QFIPXVFZSA-N.