An IRAK4 inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

AS-2444697 (hydrochloride)

Item No. 29505

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-(aminocarbonyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]-2-(2-methyl-4-pyridinyl)-4-oxazolecarboxamide, monohydrochloride
CAS Number
1287665-60-4
Molecular Formula
C19H20N6O4 • HCl
Formula Weight
432.9
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
271 nm
SMILES
O=C(N)C1=NN(C2CCOCC2)C=C1NC(C3=COC(C4=CC=NC(C)=C4)=N3)=O.Cl
InChi Code
InChI=1S/C19H20N6O4.ClH/c1-11-8-12(2-5-21-11)19-23-15(10-29-19)18(27)22-14-9-25(24-16(14)17(20)26)13-3-6-28-7-4-13;/h2,5,8-10,13H,3-4,6-7H2,1H3,(H2,20,26)(H,22,27);1H
InChi Key
FGNHLIIFEDYNFZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $38

    Add

    5 mg

    $147

    Add

    10 mg

    $274

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50 = 21 nM).1 It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (IC50s = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (ED50s = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Haynes, J.J., and Nair, S.K. Advances in the discovery of small-molecule IRAK4 inhibitors. Annual Reports in Medicinal Chemistry 49, 117-133 (2014).

    2. Kondo, M., Tahara, A., Hayashi, K., et al. Renoprotective effects of novel interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 through anti-inflammatory action in 5/6 nephrectomized rats. Naunyn Schmiedebergs Arch. Pharmacol. 287(10), 909-919 (2014).