A potent, selective, and irreversible BTK inhibitor
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CNX-774

Item No. 21475

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[[5-fluoro-4-[[3-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-2-pyrimidinyl]amino]phenoxy]-N-methyl-2-pyridinecarboxamide
CAS Number
1202759-32-7
Molecular Formula
C26H22FN7O3
Formula Weight
499.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH 7.2)(1:6): 0.14 mg/mlDMSO: 25 mg/ml
λmax
272 nm
SMILES
[H]N(C(C=C)=O)C1=CC(N([H])C2=NC(N(C3=CC=C(OC4=CC(C(N(C)[H])=O)=NC=C4)C=C3)[H])=NC=C2F)=CC=C1
InChi Code
InChI=1S/C26H22FN7O3/c1-3-23(35)31-17-5-4-6-18(13-17)32-24-21(27)15-30-26(34-24)33-16-7-9-19(10-8-16)37-20-11-12-29-22(14-20)25(36)28-2/h3-15H,1H2,2H3,(H,28,36)(H,31,35)(H2,30,32,33,34)
InChi Key
VVLHQJDAUIPZFH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $40

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    5 mg

    $132

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    10 mg

    $246

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    25 mg

    $516

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    Product Description

    CNX-774 is a potent, selective, and irreversible inhibitor of Bruton’s tyrosine kinase (BTK), an important kinase in the B cell antigen receptor pathway, with IC50 values of <1 nM in biochemical assays and 1-10 nM in cellular assays.1 It inhibits proliferation in HMC-1.1 and HMC-1.2 cells (IC50 = 2.82 and 0.38 µM) but has no effect on cell cycle progression.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

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

    2. Smilijkovic, D., Blatt, K., Stefanzl, G., et al. BTK inhibition is a potent approach to block IgE-mediated histamine release in human basophils. Allergy 1-11 (2017).