A BTK inhibitor (IC50 = 0.5 nM); greater than 20-fold selective for BTK over a panel of 384 kinases; inhibits BCR stimulation-induced calcium flux in Ramos B cells (IC50 = 9 nM)

BMS 986142 – 1 mg

Brand:
Cayman
CAS:
1643368-58-4
Storage:
-20
UN-No:
- 3077 / 9

BMS 986142 is a Bruton’s tyrosine kinase (BTK) inhibitor (IC50 = 0.5 nM).{61007} It is greater than 20-fold selective for BTK over a panel of 384 kinases. BMS 986142 inhibits calcium flux in Ramos B cells induced by B cell receptor (BCR) stimulation (IC50 = 9 nM), as well as BCR stimulation-induced proliferation of, and CD86 surface expression in, peripheral B cells (IC50s = 3 and 4 nM, respectively). It inhibits TNF-α production in human peripheral blood mononuclear cells (PBMCs) induced by Fcγ receptor stimulation (IC50 = 3 nM). BMS 986142 (30 mg/kg per day) reduces the percentage of mice with severe proteinuria and increases survival in an NZB/W lupus-prone mouse model. It reduces hind paw tibiotarsal joint bone resorption and inflammation in a mouse model of collagen antibody-induced arthritis (CAIA) when administered at doses of 5 and 20 mg/kg.{61000}  

 

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Description

A BTK inhibitor (IC50 = 0.5 nM); greater than 20-fold selective for BTK over a panel of 384 kinases; inhibits BCR stimulation-induced calcium flux in Ramos B cells (IC50 = 9 nM), as well as BCR stimulation-induced proliferation of, and CD86 surface expression in, peripheral B cells (IC50s = 3 and 4 nM, respectively); inhibits by Fcγ receptor stimulation-induced TNF-α production in human PBMCs (IC50 = 3 nM); reduces the percentage of mice with severe proteinuria and increases survival in an NZB/W lupus-prone mouse model at 30 mg/kg per day; reduces hind paw tibiotarsal joint bone resrption and inflammation in a CAIA mouse model at 5 and 20 mg/kg

Formal name: (2S,5R)-6-fluoro-5-[(3S)-3-(8-fluoro-1,4-dihydro-1-methyl-2,4-dioxo-3(2H)-quinazolinyl)-2-methylphenyl]-2,3,4,9-tetrahydro-2-(1-hydroxy-1-methylethyl)-1H-carbazole-8-carboxamide

Synonyms: 

Molecular weight: 572.6

CAS: 1643368-58-4

Purity: ≥98%

Formulation: A crystalline solid

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