4-Oxazolecarboxamide, N-[5-[(3R)-3-hydroxy-1-pyrrolidinyl]-2-(4-morpholinyl)oxazolo[4,5-b]pyridin-6-yl]-2-(2-methyl-4-pyridinyl)-, (2Z)-2-butenedioate (1:1)

Uses

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].

References

[1] Wiese MD, et al. Investigational IRAK-4 inhibitors for the treatment of rheumatoid arthritis. Expert Opin Investig Drugs. 2020 Apr 17:1-8. DOI:10.1080/13543784.2020.1752660
[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. DOI:10.3390/jcm12020399
[3] Parrondo RD, et al. IRAK-4 inhibition: emavusertib for the treatment of lymphoid and myeloid malignancies. Front Immunol. 2023 Oct 26;14:1239082. DOI:10.3389/fimmu.2023.1239082