tcsc0106 Alisertib

Alisertib (MLN 8237) is a selective Aurora A inhibitor with an IC₅₀ of 1.2 nM.

IC50 & Target: IC50: 1.2 nM (Aurora A)^[3]

In Vitro: Alisertib leads the MM cells to mitotic spindle abnormalities, mitotic accumulation, as well as inhibition of cell proliferation through apoptosis and senescence. Alisertib up-regulates p53 and tumor suppressor genes p21 and p27^[1]. The decreased activity of MLN8054/Alisertib for the T217D/W277E Aurora A/TPX2 complex may reflect the increased affinity for ATP induced by cofactor binding to Aurora A^[2]. Alisertib inhibits cell proliferation with IC₅₀ values ranging from 15 to 469 nM in different tumer cell lines^[3].

In Vivo: Alisertib (Alisertib, 30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM^[1]. Alisertib (20, 30 mg/kg, p.o.) causes tumor growth inhibition in solid tumor xenograft models and regressions in in vivo models of lymphoma, and reduces FLT uptake in HCT-116 xenograft tumors^[3].