Emavusertib (maleate)

Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib (HY-135317) . Emavusertib maleate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib maleate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib maleate exhibits antitumor activity in mouse model[1][2][3].

Product Specifications

CAS Number

[2376399-39-0]

Product Name Alternative

CA-4948 (maleate)

UNSPSC

12352005

Target

Apoptosis; FLT3; IRAK; MyD88; NF-κB

Related Pathways

Apoptosis; Immunology/Inflammation; NF-κB; Protein Tyrosine Kinase/RTK

Field of Research

Cancer; Inflammation/Immunology

Smiles

OC(/C=C\C(O)=O)=O.O=C(C1=COC(C2=CC=NC(C)=C2)=N1)NC3=C(N4CC[C@H](C4)O)N=C5C(OC(N6CCOCC6)=N5)=C3

Molecular Formula

C28H29N7O9

Molecular Weight

607.57

References & Citations

[1]Wiese MD, et al. Investigational IRAK-4 inhibitors for the treatment of rheumatoid arthritis. Expert Opin Investig Drugs. 2020 Apr 17:1-8.|[2]Guidetti F, et al. Targeting IRAK4 with Emavusertib in Lymphoma Models with Secondary Resistance to PI3K and BTK Inhibitors. J Clin Med. 2023 Jan 4;12 (2) :399. |[3]Parrondo RD, et al. IRAK-4 inhibition: emavusertib for the treatment of lymphoid and myeloid malignancies. Front Immunol. 2023 Oct 26;14:1239082.