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A JAK1 inhibitor
AZD 4205 is a JAK1 inhibitor (IC50 = 0.07 ?M).1 It is selective for JAK1 over JAK2 (IC50 = >15 ?M). AZD 4205 inhibits the phosphorylation of STAT3 in H1975 non-small cell lung cancer (NSCLC) cells (IC50 = 0.13 ?M). It enhances the antitumor activity of osimertinib in an H1975 mouse xenograft model when administered at a dose of 50 mg/kg.
1.Su, Q., Banks, E., Bebernitz, G., et al.Discovery of (2R)- N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1 H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a potent and selective Janus kinase 1 inhibitorJ. Med. Chem.63(9)4517-4527(2020)
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