A BTK inhibitor
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BMS 986142

Item No. 30927

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
1643368-58-4
Molecular Formula
C32H30F2N4O4
Formula Weight
572.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/mlEthanol: 15 mg/ml
λmax
222 nm
SMILES
CC(C)(O)C(C1)CCC2=C1NC3=C2C(C4=CC=CC(N5C(N(C)C(C(F)=CC=C6)=C6C5=O)=O)=C4C)=C(F)C=C3C(N)=O
InChi Code
InChI=1S/C32H30F2N4O4/c1-15-17(7-6-10-24(15)38-30(40)19-8-5-9-21(33)28(19)37(4)31(38)41)25-22(34)14-20(29(35)39)27-26(25)18-12-11-16(32(2,3)42)13-23(18)36-27/h5-10,14,16,36,42H,11-13H2,1-4H3,(H2,35,39)
InChi Key
ZRYMMWAJAFUANM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $90

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    1 mg

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    Product Description

    BMS 986142 is a Bruton’s tyrosine kinase (BTK) inhibitor (IC50 = 0.5 nM).1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Watterson, S.H., De Lucca, G.V., Shi, Q., et al. Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A reversible inhibitor of Bruton’s tyrosine kinase (BTK) conformationally constrained by two locked atropisomers. J. Med. Chem. 59(19), 9173-9200 (2016).

    2. Gillooly, K.M., Pulicicchio, C., Pattoli, M.A., et al. Bruton’s tyrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care. PLoS One 12(7), e0181782 (2017).