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Emavusertib (CA-4948) IRAK inhibitor

Name: Emavusertib (CA-4948)
Brand: Selleck Chemicals
SKU: S9779
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S9779

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.

Chemical Structure

Molecular Weight: 491.50

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.88

Related Targets	Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor TNF-alpha ROS Parasite PD-1/PD-L1 TLR Prostaglandin Receptor IFN CXCR Nrf2 NOS CCR NLRP3 eIF STING AhR IL Receptor Complement System β-lactamase IDO/TDO PGES NADPH-oxidase FKBP LTR
Related Products	Zimlovisertib (PF-06650833) IRAK4-IN-1 IRAK-1-4 Inhibitor I

Chemical Information, Storage & Stability

Molecular Weight	491.50	Formula	C₂₄H₂₅N₇O₅	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1801344-14-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=NC=CC(=C1)C2=NC(=CO2)C(=O)NC3=C(N=C4N=C(OC4=C3)N5CCOCC5)N6CCC(O)C6

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.54mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	IRAK4 ^[1] FLT3 ^[1]
In vitro	Emavusertib (CA-4948) is over 500-fold more selective for IRAK-4 compared to IRAK-1. This compound reduces TNF-α, IL-1β, IL-6 and IL-8 release from TLR-Stimulated THP-1 Cells with an IC50 <250 nM. It 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]
References	https://pubmed.ncbi.nlm.nih.gov/32255710/ https://ashpublications.org/blood/article/132/Supplement%201/4168/275778/Preclinical-Activity-of-IRAK4-Kinase-Inhibitor-CA https://pubmed.ncbi.nlm.nih.gov/33335659/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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