An IRAK4 inhibitor
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IRAK4 Inhibitor 28

Item No. 40167

Technical Information
Formal Name
N-[trans-4-(4-morpholinyl)cyclohexyl]-5-(tetrahydro-2H-pyran-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
CAS Number
2196204-23-4
Synonyms
  • IL-1 Receptor-associated Kinase 4 Inhibitor 28
  • Interleukin-1 Receptor-associated Kinase 4 Inhibitor 28
  • IRAK-IN-28
Molecular Formula
C21H31N5O2
Formula Weight
Purity
≥95%
A solid
Chloroform: SolubleDMSO: Soluble
SMILES
N1([C@@H]2CC[C@@H](NC3=C4C(NC=C4C5CCOCC5)=NC=N3)CC2)CCOCC1
InChi Code
InChI=1S/C21H31N5O2/c1-3-17(26-7-11-28-12-8-26)4-2-16(1)25-21-19-18(15-5-9-27-10-6-15)13-22-20(19)23-14-24-21/h13-17H,1-12H2,(H2,22,23,24,25)/t16-,17-
InChi Key
DJVYXMINSBMUHH-QAQDUYKDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    IRAK4 inhibitor 28 is an inhibitor of IL-1 receptor-associated kinase 4 (IRAK4; IC50 = 0.005 µM).1 It is selective for IRAK4 over IRAK1, CDC-like kinase 1 (Clk1), and Clk3 (IC50s = 0.023, 0.05, and >1 µM, respectively) but does inhibit Clk2, Clk4, and haspin (IC50s = 0.005, 0.008, and 0.004 µM, respectively). IRAK4 inhibitor 28 (0.12-3.3 µM) inhibits IκBα phosphorylation in OCI-LY10 diffuse large B cell lymphoma (DLBCL) cells. In vivo, IRAK4 inhibitor 28 (12.5 mg/kg) reduces tumor volume in an OCI-LY10 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Scott, J.S., Degorce, S.L., Anjum, R., et alDiscovery and optimization of pyrrolopyrimidine inhibitors of interleukin-1 receptor associated kinase 4 (IRAK4) for the treatment of mutant MYD88L265P diffuse large B-cell lymphoma. J. Med. Chem. 60(24), 10071-10091 (2017).