AS 2444697

Name: AS 2444697
Brand: Tocris Bioscience
SKU: 5430
Rating: 5 (0 reviews)

Tocris Bioscience a Bio-Techne Brand

Catalog # 5430

Citations (1)

(3)

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Key Product Details

Description:	Potent and selective IRAK4 inhibitor
Chemical Name:	N-[3-Aminocarbonyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]-2-(2-methyl-4-pyridinyl)-4-oxazolecarboxamide hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	432.86

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Biological Activity for AS 2444697

AS 2444697 is a potent and selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor (IC₅₀ = 21 nM). Displays 30-fold selectivity for IRAK4 over IRAK1. Inhibits LPS-induced TNF-α and IL-6 production in PBMCs in vitro. Renoprotective and anti-inflammatory in a rodent model of chronic kidney disease.

Compound Libraries for AS 2444697

AS 2444697 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for AS 2444697

M. Wt	432.86
Formula	C₁₉H₂₀N₆O₄.HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	1287665-60-4
PubChem ID	118719434
InChi Key	FGNHLIIFEDYNFZ-UHFFFAOYSA-N
Smiles	O=C(N)C2=NN(C=C2NC(C3=COC(C4=CC=NC(C)=C4)=N3)=O)C1CCOCC1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for AS 2444697

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	8.66	20 with gentle warming

Preparing Stock Solutions for AS 2444697

The following data is based on the product molecular weight 432.86.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	11.55 mL	57.76 mL	115.51 mL
1 mM	2.31 mL	11.55 mL	23.10 mL
2 mM	1.16 mL	5.78 mL	11.55 mL
10 mM	0.23 mL	1.16 mL	2.31 mL

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References for AS 2444697

References are publications that support the biological activity of the product.

Chaudhary Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders. J.Med.Chem. 2015 PMID: 25479567
Kondo Renoprotective effects of novel interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 through anti-inflammatory action in 5/6 nephrectomized rats. Naunyn Schmiedebergs Arch.Pharmacol. 2014 PMID: 25052043
Schmaderer and Heemann Blocking innate immunity to slow the progression of chronic kidney disease. Naunyn Schmiedebergs Arch.Pharmacol. 2014 PMID: 25107563

Citations for AS 2444697 (1)

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Citations are publications that use Bio-Techne products. Selected citations for AS 2444697 include:

Zhang et al. (2018) Tumor-Stroma IL1β-IRAK4 Feedforward Circuitry Drives Tumor Fibrosis, Chemoresistance, and Poor Prognosis in Pancreatic Cancer. Cancer Res. 78:1700
PMID: 29363544

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Customer Reviews for AS 2444697 (3)

4.7 out of 5

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0.5 % methylcellulose solution

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Product Documents for AS 2444697

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.