alisertib

Alisertib (MLN 8237) 是一种 Aurora A 激酶抑制剂 (IC50=1.2 nM)，具有口服活性和选择性。Alisertib 具有抗肿瘤活性，可以诱导细胞凋亡和自噬，诱导细胞周期阻滞。

Alisertib sodium (MLN 8237) is a potent and specific inhibitor (IC50 = 1.2 nM) of Aurora A kinase, an enzyme involved in cell division. By binding to Aurora A kinase, Alisertib sodium disrupts the formation of the mitotic spindle and causes abnormal cell division. At the molecular level, it acts on the AKT mTOR AMPK p38 pathway, leading to the induction of apoptosis and autophagy in leukemic cells. This compound exhibits significant antitumor activity.

Alisertib sodium hydrate is a salt of Alisertib --- an inhibitor of Aurora A kinase with potential antineoplastic activity. Alisertib binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation.

dAURK-4，Alisertib 的衍生物，为高效AURKA (Aurora A)选择性降解剂，具抗癌作用。

JB170是一种高效和特异性的Aurora A降解剂 (DC50=28 nM)，PROTAC由Alisertib和Thalidomide组成，对AURORA-A的EC50值是AURORA-B的十倍，能够引起细胞生长的S期阻滞并抑制AURORA-A激酶的非催化功能。