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

Evobrutinib – 1 mg

Brand:
Cayman
CAS:
1415823-73-2
Storage:
-20
UN-No:
Non-Hazardous - /

Evobrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 8.9 nM).{50414} It is selective for BTK over a panel of 233 kinases at 1 μM. It inhibits BTK in peripheral blood mononuclear cells (PBMCs; IC50 = 61 nM). Evobrutinib inhibits B cell activation and proliferation in vitro (IC50s = 18.4 and 10.9 nM, respectively).{46591} It inhibits mast cell degranulation in a mouse model of passive cutaneous anaphylaxis when administered at doses of 3.95, 19.8, and 39.5 mg/kg. Evobrutinib (1 and 3 mg/kg) reduces cartilage destruction in a rat model of collagen-induced arthritis. It also decreases proteinuria, interstitial inflammation, and the number of glomerular lesions and preserves kidney function in a mouse model of systemic lupus erythematosus (SLE).  

 

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SKU: 29029 - 1 mg Category:

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

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