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AS-2444697 (hydrochloride)

Catalog No.GC46013

AS-2444697 (hydrochloride) is an orally active IRAK-4 inhibitor with an IC50 of 21 nM.

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AS-2444697 (hydrochloride) Chemical Structure

Cas No.: 1287665-60-4

Size Price Stock Qty
1mg
$30.00
In stock
5mg
$121.00
In stock
10mg
$195.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50 = 21 nM).1 It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (IC50s = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (ED50s = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.2

|2. Kondo, M., Tahara, A., Hayashi, K., et al. 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. 287(10), 909-919 (2014).

Chemical Properties

Cas No. 1287665-60-4 SDF
Canonical SMILES O=C(N)C1=NN(C2CCOCC2)C=C1NC(C3=COC(C4=CC=NC(C)=C4)=N3)=O.Cl
Formula C19H20N6O4.HCl M.Wt 432.9
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.31 mL 11.55 mL 23.1 mL
5 mM 0.462 mL 2.31 mL 4.62 mL
10 mM 0.231 mL 1.155 mL 2.31 mL
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