A potent and covalent BTK inhibitor
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Zanubrutinib

Item No. 28924

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(7S)-4,5,6,7-tetrahydro-7-[1-(1-oxo-2-propen-1-yl)-4-piperidinyl]-2-(4-phenoxyphenyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide
CAS Number
1691249-45-2
Synonyms
  • BGB-3111
Molecular Formula
C27H29N5O3
Formula Weight
471.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS (pH 7.2) (1:5): 0.16 mg/mlDMSO: 5 mg/mlEthanol: 5 mg/ml
λmax
242 nm
SMILES
O=C(C=C)N1CCC([C@]2([H])CCNC3=C(C(N)=O)C(C4=CC=C(OC5=CC=CC=C5)C=C4)=NN32)CC1
InChi Code
InChI=1S/C27H29N5O3/c1-2-23(33)31-16-13-18(14-17-31)22-12-15-29-27-24(26(28)34)25(30-32(22)27)19-8-10-21(11-9-19)35-20-6-4-3-5-7-20/h2-11,18,22,29H,1,12-17H2,(H2,28,34)/t22-/m0/s1
InChi Key
RNOAOAWBMHREKO-QFIPXVFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $263

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    10 mg

    $493

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    25 mg

    $1,062

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    Product Description

    Zanubrutinib is a potent and covalent inhibitor of Bruton's tyrosine kinase (BTK; IC50 = 0.3 nM).1 It is selective for BTK over a panel of 304 kinases at 1 μM but does inhibit EGFR, Tec, Blk, BMX, HER4, and TXK (IC50s = 0.62-33 nM). Zanubrutinib inhibits phosphorylation of BTK at Y233 (IC50 = 1.8 nM) in Ramos cells and reduces viability of REC-1 cells (IC50 = 0.36 nM). In vivo, zanubrutinib (2.5 and 7.5 mg/kg) reduces tumor volume in an OCI-LY10 diffuse large B cell lymphoma (DLBCL) mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Guo, Y., Liu, Y., Hu, N., et al. Discovery of zanubrutinib (BGB-3111), a novel, potent, and selective covalent inhibitor of bruton’s tyrosine kinase. J. Med. Chem. 62(17), 7923-7940 (2019).