alisertib

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

Alisertib Sodium (MLN 8237 Sodium)is a selective Aurora A inhibitor that causes G2/M phase arrest and chromosomal misalignment, leading to tumour cell apoptosis, and can also inhibit STAT3 Tyr705 phosphorylation, resulting in downregulation of c-Myc expression.

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, a derivative of Alisertib, functions as a potent and selective degrader of AURKA (Aurora A), exhibiting anticancer properties [1].

JB170 is a highly efficient and specific Aurora A degradator (DC50 = 28 nM). The PROTAC is composed of Alisertib and Thalidomide, with an EC50 value for AURORA-A that is ten times that of AURORA-B. It induces S-phase arrest in cell growth and inhibits the non-catalytic function of the AURORA-A kinase.

6K465 is a novel and potent small molecule inhibitor based on a pyrimidine scaffold that selectively targets Aurora A kinase.6K465 demonstrates superior ability to reduce the levels of the c-MYC and N-MYC oncoproteins compared to the established inhibitor alisertib; in a comprehensive analysis of its antiproliferative effects, the sensitivities of various small cell lung cancer (SCLC) and breast cancer cell lines to 6K465 were strongly correlated with the baseline protein expression levels of c-MYC and/or N-MYC.