whi-p154

Description: WHI-P154 is a novel, potent and selective JAK3 (Janus kinase) inhibitor with potential antitumor activity. It inhibits JAK3 with an IC50 of 1.8 uM and exhibits no activity against JAK1 or JAK2, it also inhibits EGFR (IC50 = 4 nM), Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation. WHI-P154 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. It also inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro.

References: Blood. 2008 Feb 15; 111(4):2155-7; Clin Cancer Res. 1998 Oct; 4(10):2463-71.

Janex1; WHIP-154; WHI P154; WHIP154

Chemical Name: 2-Bromo-4-[(6, 7-dimethoxy-4-quinazolinyl)amino]phenol

InChi Key: CBIAKDAYHRWZCU-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H14BrN3O3/c1-22-14-6-10-12(7-15(14)23-2)18-8-19-16(10)20-9-3-4-13(21)11(17)5-9/h3-8, 21H, 1-2H3, (H, 18, 19, 20)

SMILES Code: OC1=CC=C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1Br