Emavusertib (CA-4948)

Name: Emavusertib (CA-4948)
Brand: Selleck Chemicals
SKU: S9779
Rating: 5 (0 reviews)

For research use only.

Catalog No.S9779

Emavusertib (CA-4948) Chemical Structure

CAS No. 1801344-14-8

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.

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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

Cell Research:

^[3]

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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.

(Only for Reference)

Animal Research:

^[2]

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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
(Only for Reference)

References

Solubility (25°C)

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

* 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.

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
Synonyms	N/A

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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.

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

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