2376399-41-4
Chemical Structure
Emavusertib tosylate
Synonym(s): CA-4948 tosylate
- CAS No.: 2376399-41-4
- Formula:C31H33N7O8S
- Molecular Weight:663.70
InChIKey: XJMGSZLODKNAJQ-PKLMIRHRSA-N
SMILES: O=S(O)(C1=CC=C(C=C1)C)=O.O=C(C2=COC(C3=CC=NC(C)=C3)=N2)NC4=C(N5CC[C@H](C5)O)N=C6C(OC(N7CCOCC7)=N6)=C4
Biological Activity: Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib (HY-135317). Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib tosylate 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 tosylate exhibits antitumor activity in mouse model[1][2][3].
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Emavusertib tosylate | Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib (HY-135317). Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib tosylate 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 tosylate exhibits antitumor activity in mouse model. | |||||||||||||||||||||
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- [1]. Wiese MD, et al. Investigational IRAK-4 inhibitors for the treatment of rheumatoid arthritis. Expert Opin Investig Drugs. 2020 Apr 17:1-8. [Content Brief]
- [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. [Content Brief]
- [3]. Parrondo RD, et al. IRAK-4 inhibition: emavusertib for the treatment of lymphoid and myeloid malignancies. Front Immunol. 2023 Oct 26;14:1239082. [Content Brief]
Keywords
