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Submit ReviewAS 1517499
Description: STAT6 inhibitor
Chemical Name: 2-[[2-(3-Chloro-4-hydroxyphenyl)ethyl]amino]-4-[(phenylmethyl)amino]-5-pyrimidinecarboxamide
Purity: ≥98% (HPLC)
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 Data 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 | 0.5 mL | 2.51 mL | 5.03 mL |
| 25 mM | 0.1 mL | 0.5 mL | 1.01 mL |
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Product Datasheets for AS 1517499
References for AS 1517499
References are publications that support the biological activity of the product.
Chiba et al (2009) A novel STAT6 inhibitor AS1517499 ameliorates antigen-induced bronchial hypercontractility in mice. Am.J.Respir.Cell Mol.Biol. 41 516 PMID: 19202006
Nagashima et al (2008) Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine- 5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors. Bioorg.Med.Chem. 16 6509 PMID: 18534856
Nagashima et al (2007) Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors. Bioorg.Med.Chem. 15 1044 PMID: 17071093
If you know of a relevant reference for AS 1517499, please let us know.
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Keywords: AS 1517499, AS 1517499 supplier, AS1517499, STAT6, inhibitors, inhibits, In, vivo, potent, asthma, STAT, 7636, Tocris Bioscience
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