Alisertib sodium(Synonyms: MLN 8237 sodium)

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Alisertib sodium (Synonyms: MLN 8237 sodium)

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。

Alisertib sodium(Synonyms: MLN 8237 sodium)

Alisertib sodium Chemical Structure

CAS No. : 1028486-06-7

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Alisertib sodium 的其他形式现货产品:

Alisertib

生物活性

Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.
参考文献

  • [1]. Güllü G, et al. A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma Blood June 24, 2010 vol. 115 no. 25 5202-5213.

    [2]. Sloane DA, et al. Drug-Resistant Aurora A Mutants for Cellular Target Validation of the Small Molecule Kinase Inhibitors MLN8054 and MLN8237 ACS Chem. Biol., 2010, 5 (6), pp 563-576.

    [3]. Bavetsias V, et al. Aurora Kinase Inhibitors: Current Status and Outlook. Front Oncol. 2015 Dec 21;5:278.

    [4]. Manfredi MG, et al. Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.Clin Cancer Res. 2011 Dec 15;17(24):7614-7624.

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