2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one
P6
Pyridone 6 Off-white solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A potent cell-permeable, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50 = 15 nM for murine JAK1), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC50 = 1 nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5; and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401). Purity: ≥98% by HPLC. CAS 457081-03-7. Ref.: Pedranzini, L., et al. 2006. Cancer Res. 66, 9714. Lucet, I.S., et al. 2005. Blood 107, 176. Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 1219. |
