Ruxolitinib phosphate是Ruxolitinib (INCB018424, INC424)的磷酸盐形式。Ruxolitinib是具有口服活性、第一个应用到临床的选择性JAK1/2抑制剂,IC50值为3.3 nM/2.8 nM,其选择性是作用于Tyk2的6倍,是JAK3的130倍。Ruxolitinib用于治疗中间或高危骨髓纤维化,并且具有强效的抗肿瘤和免疫调节活性。Ruxolitinib选择性抑制Ba/F3-EpoR-JAK2 V617F细胞增殖,而且会导致磷酸化JAK2和STAT5信号转导和激活剂水平降低。
参考文献
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