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: 1801344-14-8

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

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

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
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 Recruiting
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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Emavusertib (CA-4948) | Emavusertib (CA-4948) supplier | purchase Emavusertib (CA-4948) | Emavusertib (CA-4948) cost | Emavusertib (CA-4948) manufacturer | order Emavusertib (CA-4948) | Emavusertib (CA-4948) distributor