AS1517499

AS1517499 is a STAT6 inhibitor (IC50 = 21 nM in a reporter assay). 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. It inhibits STAT6 phosphorylation and thyroid epithelial cell (TEC) hyperplasia and decreases serum levels of 3,3',5-triiodo-L-thyronine (T3, Cay-16028) and thyroxine (T4) in a mouse model of Graves' disease when administered at a dose of 10 mg/kg per day. AS1517499 (20 mg/kg twice weekly) also inhibits tumor growth and liver metastasis in a murine orthotopic 4T1 mammary carcinoma model.Formal Name: 2-[[2-(3-chloro-4-hydroxyphenyl)ethyl]amino]-4-[(phenylmethyl)amino]-5-pyrimidinecarboxamide. CAS Number: 919486-40-1. Molecular Formula: C20H20ClN5O2. Formula Weight: 397.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 25mg/mL, DMF:PBS (pH 7.2) (1:6): 0.14mg/mL, DMSO: 15mg/mL, Ethanol: 5mg/mL. lambdamax: 232, 263, 306 nm. SMILES: OC1=C(Cl)C=C(CCNC2=NC(NCC3=CC=CC=C3)=C(C(N)=O)C=N2)C=C1. InChi Code: InChI=1S/C20H20ClN5O2/c21-16-10-13(6-7-17(16)27)8-9-23-20-25-12-15(18(22)28)19(26-20)24-11-14-4-2-1-3-5-14/h1-7,10,12,27H,8-9,11H2,(H2,22,28)(H2,23,24,25,26). InChi Key: OZRMEKAUZBKTTC-UHFFFAOYSA-N.