Emavusertib (hydrochloride)

Emavusertib hydrochloride (CA-4948 tosylate) is the hydrochloride salt form of Emavusertib (HY-135317) . Emavusertib hydrochloride is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib hydrochloride 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 hydrochloride exhibits antitumor activity in mouse model[1][2][3].

Product Specifications

CAS Number

[2376399-42-5]

Product Name Alternative

CA-4948 (hydrochloride)

UNSPSC

12352005

Target

Apoptosis; FLT3; IRAK; MyD88; NF-κB

Type

Reference compound

Related Pathways

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

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/emavusertib-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C24H26ClN7O5

Molecular Weight

527.96

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.