Emavusertib (CA-4948)

For research use only.

Catalog No.S9779

Emavusertib (CA-4948) Chemical Structure

CAS No. 1801344-14-8

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.

Purity & Quality Control

Choose Selective IRAK Inhibitors

Biological Activity

Description 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 [1]
()		 FLT3 [1]
()
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.[3]
In vivo

Emavusertib (CA-4948) has anti-tumour activity in animal models including tumours containing MyD88 gene mutations.[2]

Protocol

Cell Research:

[3]
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  • Cell lines: THP-1 cells
  • Concentrations: 0.1 μM-10 μM
  • Incubation Time: 60 min
  • Method:

    Cells are treated with Emavusertib for 60 minutes. Cells treated with 0.5% DMSO serves as unstimulated control. After 60 minutes, 20 µl of 10X LTA (10µg/ml) is added to Emavusertib treated and DMSO treated control wells and the plates are incubated at 37°C for 5 hours in a CO2 incubator. After 5 hours, the plates are centrifuged at 300 x g for 5 min and supernatants are collected and analyzed for TNFα levels using the human TNF-alpha ELISA Kit.


    (Only for Reference)
Animal Research:

[2]
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  • Animal Models: Mice bearing DLBCL PDX tumors
  • Dosages: 37.5 mg/kg or 75 mg/kg (BID), 75 mg/kg or 150 mg/kg (QD)
  • Administration: PO
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 49 mg/mL (99.69 mM)
Water Insoluble
Ethanol '''''''2 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 491.50
Formula

C24H25N7O5
CAS No. 1801344-14-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04278768 Recruiting Drug: CA-4948|Drug: Azacitidine|Drug: Venetoclax Acute Myelogenous Leukemia|Myelodysplastic Syndrome Curis Inc. July 6 2020 Phase 1|Phase 2
NCT03328078 Recruiting Drug: CA-4948|Drug: ibrutinib Relapsed Hematologic Malignancy|Refractory Hematologic Malignancy Curis Inc. December 28 2017 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID