Description
A BTK inhibitor (IC50 = 8.9 nM); selective for BTK over a panel of 233 kinases at 1 μM; inhibits BTK in PBMCs (IC50 = 61 nM); inhibits B cell activation and proliferation in vitro (IC50s = 18.4 and 10.9 nM, respectively); inhibits mast cell degranulation in a mouse model of passive cutaneous anaphylaxis at 3.95, 19.8, and 39.5 mg/kg; reduces cartilage destruction in a rat model of collagen-induced arthritis at 1 and 3 mg/kg; decreases proteinuria, interstitial inflammation, and the number of glomerular lesions and preserves kidney function in a mouse model of SLE
Formal name: 1-[4-[[[6-amino-5-(4-phenoxyphenyl)-4-pyrimidinyl]amino]methyl]-1-piperidinyl]-2-propen-1-one
Synonyms:
Molecular weight: 429.5
CAS: 1415823-73-2
Purity: ≥98%
Formulation: A crystalline solid