Emavusertib (CA-4948) is a potent and orally bioavailable inhibitor of interleukin-1 receptor-associated kinase 4/FMS-like Tyrosine Kinase 3 (IRAK4/FLT3) with anti-tumor activity.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of interleukin 1 receptor associated kinase 4
Product Description
Information
Emavusertib (CA-4948) Emavusertib (CA-4948) is a potent and orally bioavailable inhibitor of interleukin-1 receptor-associated kinase 4/FMS-like Tyrosine Kinase 3 (IRAK4/FLT3) with anti-tumor activity.
Targets
IRAK4 ; FLT3
In vitro
Emavusertib (CA-4948) is over 500-fold more selective for IRAK-4 compared to IRAK-1. Emavusertib (CA-4948) reduces TNF-α, IL-1β, IL-6 and IL-8 release from TLR-Stimulated THP-1 Cells with an IC50 <250 nM. Emavusertib (CA-4948) has antiproliferative activity due to inhibition of receptor-type tyrosine-protein kinase FLT3.
In vivo
Emavusertib (CA-4948) has anti-tumour activity in animal models including tumours containing MyD88 gene mutations.
1.Gummadi VR, Boruah A, Ainan BR, Vare BR, Manda S, Gondle HP, Kumar SN, Mukherjee S, Gore ST, Krishnamurthy NR et al.. (2020) Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies.. ACS Med Chem Lett, 11 (12):(2374-2381). [PMID:33335659]
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I2207493