Alisertib (MLN 8237) sodium is an orally active and selectiveAurora Akinaseinhibitor (IC₅₀=1.2 nM), which binds toAurora Akinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium inducesapoptosisandautophagythrough targeting theAKT/mTOR/AMPK/p38pathway in leukemic cells. Antitumor activity^[1][2][3].

Alisertib (MLN 8237) 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 Alisertib (MLN 8237) for the T217D/W277E Aurora A/TPX2 complex may reflect the increased affinity for ATP induced by cofactor binding to Aurora A^[2].
Alisertib (MLN 8237) inhibits cell proliferation with IC₅₀s ranging from 15 to 469 nM in different tumer cell lines^[4].

Alisertib (MLN 8237) (30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM^[1].
Alisertib (3-30 mg/kg; P.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models^[4].

540.91

C₂₇H₁₉ClFN₄NaO₄

1028486-06-7

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