AS 1517499

Pricing Availability   Qty
Description: STAT6 inhibitor
Chemical Name: 2-[[2-(3-Chloro-4-hydroxyphenyl)ethyl]amino]-4-[(phenylmethyl)amino]-5-pyrimidinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
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Pathways (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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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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


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Citations for AS 1517499

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Pathways for AS 1517499

JAK-STAT Signaling Pathway

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.