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Submit ReviewAS 2444697
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)
Biological Activity
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
AS 2444697 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data
| 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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.66 | 20 with gentle warming |
Preparing Stock Solutions
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 | 23.1 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
References
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.
Reviews for AS 2444697
Average Rating: 5 (Based on 1 Review.)
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oral admingistration.
By
Anonymous on 11/29/2018
Assay Type: In Vivo
Species: Mouse
0.5 % methylcellulose solution
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