An IRAK4 inhibitor
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Emavusertib

Item No. 36845

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-[(3R)-3-hydroxy-1-pyrrolidinyl]-2-(4-morpholinyl)oxazolo[4,5-b]pyridin-6-yl]-2-(2-methyl-4-pyridinyl)-4-oxazolecarboxamide
CAS Number
1801344-14-8
Synonyms
  • CA-4948
Molecular Formula
C24H25N7O5
Formula Weight
491.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
260, 345 nm
SMILES
O=C(C1=COC(C2=CC=NC(C)=C2)=N1)NC3=C(N4CC[C@@H](O)C4)N=C5C(OC(N6CCOCC6)=N5)=C3
InChi Code
InChI=1S/C24H25N7O5/c1-14-10-15(2-4-25-14)23-27-18(13-35-23)22(33)26-17-11-19-20(28-21(17)31-5-3-16(32)12-31)29-24(36-19)30-6-8-34-9-7-30/h2,4,10-11,13,16,32H,3,5-9,12H2,1H3,(H,26,33)/t16-/m1/s1
InChi Key
SJHNWSAWWOAWJH-MRXNPFEDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $54

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    10 mg

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    25 mg

    $149

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    50 mg

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    Product Description

    Emavusertib is an inhibitor of IL-1 receptor-associated kinase 4 (IRAK4; IC50 = 31.7 nM).1 It is selective for IRAK4 over FMS-related tyrosine kinase 3 (FLT3), cyclin-dependent kinase 2 (Cdk2), Aurora A kinase, glycogen synthase kinase 3β (GSK3β), and muscle-associated receptor tyrosine kinase (MUSK) at 1 µM. Emavusertib inhibits IL-6 release mediated by toll-like receptor 2 (TLR2), TLR5, or IL-1 receptor (IL-1R) in isolated human whole blood (IC50s = 989, 696, and 1,375 nM, respectively). In vivo, emavusertib (25-200 mg/kg) reduces tumor volume in an OCI-Ly3 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. Gummadi, V.R., Boruah, A., Ainan, B.R., et al. Discovery of CA-4948, an orally bioavailable IRAK4 inhibitor for treatment of hematologic malignancies. ACS Med. Chem. Lett. 11(12), 2374-2381 (2020).