Emavusertib (CA-4948)

Catalog No.S9779 Batch:S977901

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Technical Data

Formula

C24H25N7O5
Molecular Weight 491.50 CAS No. 1801344-14-8
Solubility (25°C)* In vitro DMSO 49 mg/mL (99.69 mM)
Ethanol 2 mg/mL (4.06 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.25mg/ml 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. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[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

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

CD163+ M2 macrophages promote fibrosis in IgG4-related disease via TLR7/IRAK4/NF-κB signaling [ Arthritis Rheumatol, 2021, 10.1002/art.42043] PubMed: 34907668

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.