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AS 2444697

Cat. No. 5430 1 Citation Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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)
Datasheet
Citations (1)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

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 Data for AS 2444697

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 23.1 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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Product Datasheets for AS 2444697

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for AS 2444697

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

Chaudhary (2015) 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. 58 96 PMID: 25479567

Kondo et al (2014) 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. 387 909 PMID: 25052043

Schmaderer and Heemann (2014) Blocking innate immunity to slow the progression of chronic kidney disease. Naunyn Schmiedebergs Arch.Pharmacol. 387 905 PMID: 25107563

If you know of a relevant reference for AS 2444697, please let us know.

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Keywords: AS 2444697, AS 2444697 supplier, AS2444697, potent, selective, interleukin-1, receptor-associated, kinase, 4, IRAK4, inhibitors, inhibits, anti-inflammatory, renoprotective, Cytokines, IRAK, 5430, Tocris Bioscience

1 Citation for AS 2444697

Citations are publications that use Tocris 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

Do you know of a great paper that uses AS 2444697 from Tocris? Please let us know.

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