Emavusertib phosphate
Based on 7 publication(s) in Google Scholar
Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib (HY-135317). Emavusertib phosphate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib phosphate 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 phosphate exhibits antitumor activity in mouse model.
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- CAS No.: 2376399-38-9
- Formula: C24H28N7O9P
- Molecular Weight:589.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Emavusertib phosphate
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Cell Proliferation/Viability Assay
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WB
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In Vivo Efficacy Study
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IHC
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Bio/Physico-chemical Assay
Biological Activity
Chemical Information
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CAS No. 2376399-38-9
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Molecular Weight 589.49
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Formula C24H28N7O9P
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SMILES
O=P(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
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Synonyms
CA-4948 phosphate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (7)
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Journal Impact Factor
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Most Recent
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Blood
2023 Sep 14;142(11):989-1007. PMID: 37172199
Emavusertib phosphate purchased from MedChemExpress. Usage Cited in: Blood. 2023 Sep 14;142(11):989-1007. [Abstract]
IC50 curves for CA-4948 (Emavusertib) (0.01-10000 nM; 24 h) and PF-06650833 in an assay measuring NF-kB activity upon TLR2 stimulation with PAM3CSK4 in THP1 NF-kB reporter cells.
Emavusertib phosphate purchased from MedChemExpress. Usage Cited in: Blood. 2023 Sep 14;142(11):989-1007. [Abstract]
Immunoblots for phospho-IRAK1, total IRAK1, IRAK2, and IRAK4 in MDSL and AML (1714) treated for 24 hours with CA-4948 (Emavusertib) (10 μM). The results showed that treatment with CA-4948 resulted in increased IRAK1 phosphorylation.
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Leukemia
Targeting of IRAK4 and GSPT1 enhances therapeutic efficacy in AML via c-Myc destabilization. [Abstract]2025 Sep;39(9):2163-2173. PMID: 40670672
Emavusertib phosphate purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Sep;39(9):2163-2173. [Abstract]
Cell viability was determined in THP1 and HL60 cells cultured with 10 µM CA-4948 (Emavusertib) or in OCI-AML3 and K562 cultured with 1 µM CA-4948 or vehicle (n = 4) for 14 days and then treated with CC-885 (n = 4).
Emavusertib phosphate purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Sep;39(9):2163-2173. [Abstract]
Immunoblots for c-MYC in the patient-derived AML samples (AML1794, AML1714) cultured with CA-4948 (Emavusertib) (10 µM) or vehicle for 14 days and then treated with CC-885 (50 nM) for 4 h.
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Cell Rep
Disruption of fibroblast MYD88 signaling promotes antitumor immunity in pancreatic ductal adenocarcinoma. [Abstract]2025 Sep 24;44(10):116347. PMID: 41004339
Emavusertib phosphate purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Sep 24;44(10):116347. [Abstract]
Harvested tumor weights by treatment condition (n = 8 per condition).Tumor growth studies demonstrated statistically significant inhibition with both CA-4948 (Emavusertib) (50 mg/kg; oral gavage; once daily) alone and ICB alone.
Emavusertib phosphate purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Sep 24;44(10):116347. [Abstract]
H&E and trichrome staining of tumors by treatment condition (Emavusertib (50 mg/kg; oral gavage; once daily), ect.) at 10× magnification. The scale bar represents 100 μm.
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Front Immunol
Activation of Toll-Like Receptor 7 Signaling Pathway in Primary Sjögren's Syndrome-Associated Thrombocytopenia. [Abstract]2021 Mar 9:12:637659. PMID: 33767707 -
Curr Issues Mol Biol
FLT3 and IRAK4 Inhibitor Emavusertib in Combination with BH3-Mimetics in the Treatment of Acute Myeloid Leukemia. [Abstract]2024 Mar 29;46(4):2946-2960. PMID: 38666914 -
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Purity & Documentation
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. [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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)