A potent, selective BTK inhibitor
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CGI1746

Item No. 18414

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[4,5-dihydro-4-methyl-6-[[4-(4-morpholinylcarbonyl)phenyl]amino]-5-oxo-2-pyrazinyl]-2-methylphenyl]-4-(1,1-dimethylethyl)-benzamide
CAS Number
910232-84-7
Molecular Formula
C34H37N5O4
Formula Weight
579.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 0.25 mg/ml
λmax
234, 355 nm
SMILES
O=C(C1=CC=C(NC2=NC(C3=CC=CC(NC(C4=CC=C(C(C)(C)C)C=C4)=O)=C3C)=CN(C)C2=O)C=C1)N5CCOCC5
InChi Code
InChI=1S/C34H37N5O4/c1-22-27(7-6-8-28(22)37-31(40)23-9-13-25(14-10-23)34(2,3)4)29-21-38(5)33(42)30(36-29)35-26-15-11-24(12-16-26)32(41)39-17-19-43-20-18-39/h6-16,21H,17-20H2,1-5H3,(H,35,36)(H,37,40)
InChi Key
JIFCFQDXHMUPGP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $94

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    10 mg

    $125

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    25 mg

    $271

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    Product Description

    CGI1746 is a potent, selective inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 1.9 nM), a non-receptor tyrosine kinase that is important in B lymphocyte development.1,2 It blocks both auto-and trans-phosphorylation of BTK by occupying an SH3 binding pocket in the un-phosphorylated enzyme. CGI1746 prevents B-cell antigen receptor-mediated B lymphocyte proliferation and suppresses FCγRIII-induced TNFα, IL-1β, and IL-6 production in macrophages.1 It reduces cytokine levels within joints and ameliorates symptoms in a mouse model of autoantibody-induced arthritis.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. di Paolo, J.A., Huang, T., Balazs, M., et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nat. Chem. Biol. 7(1), 41-50 (2011).

    2. Akinleye, A., Chen, Y., Mukhi, N., et al. Ibrutinib and novel BTK inhibitors in clinical development. J. Hematol. Oncol. 6(59), (2013).