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Alisertib

CAS No. : 1028486-01-2

MCE 国际站：Alisertib

产品活性：Aliertib (MLN 8237) 是一种口服活性和选择性的 Aurora A 激酶抑制剂 (IC₅₀=1.2 nM)，与Aurora A 激酶结合，导致有丝分裂纺锤体异常、有丝分裂累积。Aliertib (MLN 8237) 通过靶向白血病细胞中的 AKT/mTOR/AMPK/p38 途径诱导其凋亡和自噬。具有抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Autophagy  |  Apoptosis

作用靶点：Aurora Kinase  |  Autophagy  |  Apoptosis

In Vitro: 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.
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.
Alisertib (MLN 8237) inhibits cell proliferation with IC₅₀s ranging from 15 to 469 nM in different tumer cell lines.

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

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