A STAT6 inhibitor (IC50 = 21 nM in a reporter assay); inhibits IL-4-induced Th2 differentiation of mouse spleen T cells (IC50 = 2.3 nM); inhibits bronchial smooth muscle hyperresponsiveness and IL-13 production in ovalbumin-sensitized mice at 10 mg/kg; inhibits STAT6 phosphorylation and TEC hyperplasia and decreases serum levels of T3 and T4 in a mouse model of Graves’ disease at 10 mg/kg per day; inhibits tumor growth and liver metastasis in a murine orthotopic 4T1 mammary carcinoma model at 20 mg/kg twice weekly

AS1517499 – 10 mg

Brand:
Cayman
CAS:
919486-40-1
Storage:
-20
UN-No:
Non-Hazardous - /

AS1517499 is a STAT6 inhibitor (IC50 = 21 nM in a reporter assay).{52065} It inhibits IL-4-induced Th2 differentiation (IC50 = 2.3 nM), but not IL-12-induced Th1 differentiation, of mouse spleen T cells. AS1517499 (10 mg/kg) inhibits bronchial smooth muscle hyperresponsiveness and IL-13 production in ovalbumin-sensitized mice when administered one hour prior to antigen exposure.{52067} It inhibits STAT6 phosphorylation and thyroid epithelial cell (TEC) hyperplasia and decreases serum levels of 3,3′,5-triiodo-L-thyronine (T3; Item No. 16028) and thyroxine (T4) in a mouse model of Graves’ disease when administered at a dose of 10 mg/kg per day.{52068} AS1517499 (20 mg/kg twice weekly) also inhibits tumor growth and liver metastasis in a murine orthotopic 4T1 mammary carcinoma model.{52066}  

 

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Description

A STAT6 inhibitor (IC50 = 21 nM in a reporter assay); inhibits IL-4-induced Th2 differentiation of mouse spleen T cells (IC50 = 2.3 nM); inhibits bronchial smooth muscle hyperresponsiveness and IL-13 production in ovalbumin-sensitized mice at 10 mg/kg; inhibits STAT6 phosphorylation and TEC hyperplasia and decreases serum levels of T3 and T4 in a mouse model of Graves’ disease at 10 mg/kg per day; inhibits tumor growth and liver metastasis in a murine orthotopic 4T1 mammary carcinoma model at 20 mg/kg twice weekly

Formal name: 2-[[2-(3-chloro-4-hydroxyphenyl)ethyl]amino]-4-[(phenylmethyl)amino]-5-pyrimidinecarboxamide

Synonyms: 

Molecular weight: 397.9

CAS: 919486-40-1

Purity: ≥98%

Formulation: A solid

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