Emavusertib

• Description:

  Emavusertib is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib 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 exhibits antitumor activity in mouse model

• Product Name Alternative:

  CA-4948

• UNSPSC:

  12352005

• Hazard Statement:

  H315, H317, H319, H335

• Target:

  Apoptosis; FLT3; IRAK; MyD88; NF-κB

• Type:

  Reference compound

• Related Pathways:

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

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer; Inflammation/Immunology

• Assay Protocol:

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

• Purity:

  99.97

• Solubility:

  DMSO : 50 mg/mL (ultrasonic)

• Smiles:

  O=C(C1=COC(C2=CC(C)=NC=C2)=N1)NC3=C(N4C[C@H](O)CC4)N=C5C(OC(N6CCOCC6)=N5)=C3

• Molecular Formula:

  C24H25N7O5

• Molecular Weight:

  491.50

• Precautions:

  H315, H317, H319, H335

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• Isoform:

  IRAK4

• CAS Number:

  [1801344-14-8]