Emavusertib (CA-4948)

Catalog No.S9779

For research use only.

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.

Emavusertib (CA-4948) Chemical Structure

CAS No. 1801344-14-8

Selleck's Emavusertib (CA-4948) has been cited by 1 Publication

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 (from reference)

Cell Research:

[3]

  • 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.

Animal Research:

[2]

  • 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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 491.50
Formula

C24H25N7O5

CAS No. 1801344-14-8
Storage 3 years -20°C powder
2 years -80°C in solvent

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05178342 Not yet recruiting Drug: CA-4948 Myelodysplastic Syndromes|Anemia University of Leipzig|Curis Inc. January 1 2022 Phase 2
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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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