AS 1517499

Name: AS 1517499
Brand: Tocris Bioscience
SKU: 7636

Tocris Bioscience, part of Bio-Techne | Catalog # 7636

Citations (2)

COA / SDS

STAT6 inhibitor

Key Product Details

Description:	STAT6 inhibitor
Chemical Name:	2-[[2-(3-Chloro-4-hydroxyphenyl)ethyl]amino]-4-[(phenylmethyl)amino]-5-pyrimidinecarboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	397.86

View Full Technical Details for AS 1517499

Technical Data
Citations

Biological Activity for AS 1517499

AS 1517499 is a potent STAT6 inhibitor (IC₅₀ = 21 nM). In vitro, it inhibits IL-4-induced Th2 differentiation of mouse spleen T cells (IC₅₀ = 2.3 nM), without influencing Th1 differentiation induced by IL-12. In a mouse model of allergic bronchial asthma, treatment with AS 1517499 reduces mouse airway IL-3 production and partly inhibits the RhoA upregulation in bronchial smooth muscles.

Technical Data for AS 1517499

M. Wt	397.86
Formula	C₂₀H₂₀ClN₅O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	919486-40-1
PubChem ID	10340781
InChi Key	OZRMEKAUZBKTTC-UHFFFAOYSA-N
Smiles	O=C(N)C1=CN=C(N=C1NCC=2C=CC=CC2)NCCC3=CC=C(O)C(Cl)=C3

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 1517499

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	19.89	50
	ethanol	3.98	10

Preparing Stock Solutions for AS 1517499

The following data is based on the product molecular weight 397.86.

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
0.5 mM	5.03 mL	25.13 mL	50.27 mL
2.5 mM	1.01 mL	5.03 mL	10.05 mL
5 mM	0.50 mL	2.51 mL	5.03 mL
25 mM	0.10 mL	0.50 mL	1.01 mL

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References for AS 1517499

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

Nagashima Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine- 5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors. Bioorg.Med.Chem. 2008 PMID: 18534856
Nagashima Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors. Bioorg.Med.Chem. 2007 PMID: 17071093
Chiba A novel STAT6 inhibitor AS1517499 ameliorates antigen-induced bronchial hypercontractility in mice. Am.J.Respir.Cell Mol.Biol. 2009 PMID: 19202006