A covalent BTK inhibitor
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BIIB129

Item No. 43712

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-methyl-N-[cis-3-methyl-3-[[6-(1-methyl-1Hpyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]oxy]cyclobutyl]-2-propenamide
CAS Number
2770960-52-4
Molecular Formula
C19H22N6O2
Formula Weight
366.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
C[C@](C[C@H]1N(C)C(C=C)=O)(C1)OC2=NC(C(C=N3)=CN3C)=CN4C2=CC=N4
InChi Code
InChI=1S/C19H22N6O2/c1-5-17(26)24(4)14-8-19(2,9-14)27-18-16-6-7-20-25(16)12-15(22-18)13-10-21-23(3)11-13/h5-7,10-12,14H,1,8-9H2,2-4H3/t14-,19+
InChi Key
WBFSPPPOPIJCLF-DHFPXDALSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $91

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    10 mg

    $172

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    25 mg

    $406

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    50 mg

    $632

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    Product Description

    BIIB129 is a covalent inhibitor of Bruton's tyrosine kinase (BTK).1 It is selective for BTK over a panel of 403 additional kinases at 1 µM. BIIB129 inhibits CD69 activation in isolated human whole blood (IC50 = 7.9 nM). In vivo, BIIB129 inhibits anti-myelin oligodendrocyte glycoprotein (MOG) antibody-induced microglia activation in mice (ED50 = 1.5 mg/kg).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Himmelbauer, M.K., Bajrami, B., Basile, R., et al. Discovery and preclinical characterization of BIIB129, a covalent, selective, and brain-penetrant BTK inhibitor for the treatment of multiple sclerosis. J. Med. Chem. 67(10), 8122-8140 (2024).