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Alisertib sodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Alisertib sodium图片
CAS NO:1028486-06-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
MLN 8237 sodium
产品介绍
Aliertib (MLN 8237) sodium 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 sodium 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。
生物活性

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].

IC50& Target[3]

Aurora A

12.5 nM (IC50)

Aurora B

396.5 nM (IC50)

体外研究
(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[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].

体内研究
(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[1].
Alisertib (3-30 mg/kg; P.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models[4].

Animal Model:Nude mice bearing HCT-116 colon tumor xenograft[4]
Dosage:3, 10, or 30 mg/kg
Administration:P.o.; once daily for 3 weeks
Result:Resulted in a dose-dependent TGI (tumor growth inhibition) of 43.3%, 84.2%, and 94.7% for the 3, 10, and 30 mg/kg groups,respectively.
Clinical Trial
分子量

540.91

Formula

C27H19ClFN4NaO4

CAS 号

1028486-06-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.