For research use only.

Catalog No.S8381

BMS-986142 Chemical Structure

CAS No. 1643368-58-4

BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK with an IC50 of 0.5 nM. In a panel of 384 kinases, only five kinases were inhibited by BMS-986142 with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX).

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Biological Activity

Description BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK with an IC50 of 0.5 nM. In a panel of 384 kinases, only five kinases were inhibited by BMS-986142 with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX).
BTK [1]
(Cell-free assay)
0.5 nM
In vitro

In B cells stimulated through the B cell receptor (BCR), BMS-986142 potently inhibits signaling and functional end points, including calcium flux (IC50 = 9 nM), production of cytokines, proliferation, and surface expression of the costimulatory molecule CD86 (IC50 = 3−4 nM). In T cells, ITK-catalyzed phosphorylation of PLCγ1 stimulated through the T cell receptor (TCR) is at least 45-fold less potently inhibited by BMS-986142 than BTK-dependent signaling end points in B cells, as expected based on the 30-fold selectivity for BTK over ITK in the enzymatic assays[2].

In vivo

In multispecies pharmacokinetic studies, the absolute oral bioavailability of BMS-986142 is 93% in mice, 67% in rats, 33% in cynomolgus monkeys, and 100% in dogs. The total body plasma clearance of BMS-986142 is low in all species. The large steady-state volume of distribution observed is indicative of extravascular distribution, in spite of the high protein binding. However, brain penetration is very low in rats (<5% of plasma concentration). BMS-986142 blocks the increase in severe proteinuria in a female NZB/W lupus-prone mouse model in vivo. Treatment with BMS-986142 provides robust protection against tubulo-interstitial and glomerular nephritis, as well as inflammatory infiltration[2].


Kinase Assay:


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Human Recombinant BTK Enzyme Assay:

To V-bottom 384-well plates were added test compounds, human recombinant BTK (1 nM), fluoresceinated peptide (1.5 μM), ATP (20 μM), and assay buffer (20 mM HEPES at pH 7.4, 10 mM MgCl2, 0.015% Brij 35 surfactant, and 4 mM DTT in 1.6% DMSO), with a final volume of 30 μL. After incubating at room temperature for 60 min, the reaction was terminated by adding 45 μL of 35 mM EDTA to each sample. The reaction mixture was analyzed by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to control reactions with no enzyme (for 100% inhibition) and controls with no inhibitor (for 0% inhibition). Dose−response curves were generated to determine the concentration required for inhibiting 50% of BTK activity (IC50). Compounds were dissolved at 10 mM in DMSO and evaluated at 11 concentrations.
Cell Research:


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  • Cell lines: Ramos B cells
  • Concentrations: 0.4, 1.6, 6, 25, 100 and 400 nM
  • Incubation Time: 1 h
  • Method:

    B-cell receptor (BCR)-stimulated phospholipase C (PLC)-γ2 phosphorylation in Ramos B cells: After 1 hour of pre-incubation of Ramos B cells in media containing 10% fetal bovine serum (FBS) with varying concentrations of BMS-986142 at 37°C, the cells are stimulated with AffiniPure F(ab’)2 fragment goat anti-human immunoglobulin (Ig)M at 50 μg/mL for exactly 2 minutes at 37°C, followed by addition of ice-cold phosphate-buffered saline for quenching. The cells are pelleted and lysed, and PLCγ2 levels are measured by immunoblot using rabbit anti-human phosphoY759-PLCγ2 and analyzed using the Odyssey Infrared Imaging System with normalization to an actin control to ensure consistent loading.

    (Only for Reference)
Animal Research:


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  • Animal Models: female NZB/W lupus-prone mouse model
  • Dosages: 30 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (174.64 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 572.60


CAS No. 1643368-58-4
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C=CC=C1N2C(=O)C3=C(C(=CC=C3)F)N(C2=O)C)C4=C(C=C(C5=C4C6=C(N5)CC(CC6)C(C)(C)O)C(=O)N)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02638948 Completed Drug: BMS-986142|Drug: Placebo|Drug: Methotrexate Rheumatoid Arthritis Bristol-Myers Squibb February 16 2016 Phase 2
NCT02257151 Completed Drug: BMS-986142|Drug: Placebo Healthy Adult Bristol-Myers Squibb September 2014 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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BTK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID