Home Immunology & Inflammation IRAK inhibitor - FLT3 inhibitor Emavusertib (CA-4948) For research use only.

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.

Emavusertib (CA-4948) Chemical Structure

Emavusertib (CA-4948) Chemical Structure

CAS No. 1801344-14-8

Purity & Quality Control

Batch: S977901 DMSO]49 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.88%
99.88

Emavusertib (CA-4948) Related Products

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
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]
Cell Research 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.
In Vivo
In vivo

Emavusertib (CA-4948) has anti-tumour activity in animal models including tumours containing MyD88 gene mutations.[2]
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05178342 Terminated
Myelodysplastic Syndromes|Anemia
University of Leipzig|Curis Inc.
 January 1 2022 Phase 2
NCT04278768 Recruiting
Acute Myelogenous Leukemia|Myelodysplastic Syndrome
Curis Inc.
 July 6 2020 Phase 1|Phase 2
NCT03328078 Recruiting
Relapsed Hematologic Malignancy|Refractory Hematologic Malignancy|Relapsed Primary Central Nervous System Lymphoma|Refractory Primary Central Nervous System Lymphoma
Curis Inc.
 December 28 2017 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 491.50 Formula

C24H25N7O5
CAS No. 1801344-14-8 SDF --
Smiles CC1=NC=CC(=C1)C2=NC(=CO2)C(=O)NC3=C(N=C4N=C(OC4=C3)N5CCOCC5)N6CCC(O)C6
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 49 mg/mL ( (99.69 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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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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