Potent and selective JAK2 inhibitor (IC50
< 3 nM). Exhibits >50-fold selectivity for JAK2 over JAK3. Exhibits antitumor effects and inhibits formation of lung metastases in a mouse renal cancer model. Also inhibits STAT3 signaling, tumor angiogenesis and myeloid cell migration in vivo
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Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.
Ioannidis S et al.
Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480.
Xin et al.
Cancer Res., 2011;71:6601