AZD1480

AZD1480是一种新型的JAK小分子抑制剂。AZD1480能够阻止细胞增殖，诱导骨髓瘤细胞凋亡。在基质细胞和肿瘤细胞中，AZD1480可以有效抑制由STAT3介导的肿瘤血管生成与转移。AZD1480对各种骨髓瘤细胞有效，如RPMI 8226、OPM-2、NCI-H929、Kms.18、MM1.S和IM-9，以及各种原发性骨髓瘤细胞。AZD1480可以诱导在HS-5骨髓（BM）基质细胞存在下的Kms.11细胞死亡，并抑制Kms.11异种移植小鼠模型的肿瘤生长，同时抑制磷酸化FGFR3、磷酸化JAK2、磷酸化STAT3和Cyclin D2的水平。相对于Jak3，AZD1480对Jak2具有选择性，特别是在高浓度ATP下，其对Jak2的选择性稍高于Jak1（Km ATP水平下）。

参考文献：
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