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Alisertib sodium

Catalog No. T38428 CAS 1028486-06-7

Synonyms: MLN 8237 sodium

Alisertib sodium (MLN 8237) is a potent and specific inhibitor (IC50 = 1.2 nM) of Aurora A kinase, an enzyme involved in cell division. By binding to Aurora A kinase, Alisertib sodium disrupts the formation of the mitotic spindle and causes abnormal cell division. At the molecular level, it acts on the AKT/mTOR/AMPK/p38 pathway, leading to the induction of apoptosis and autophagy in leukemic cells. This compound exhibits significant antitumor activity.

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Alisertib sodium, CAS 1028486-06-7

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,970.00
50 mg	8-10 weeks	$ 2,580.00
100 mg	8-10 weeks	$ 3,400.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	Alisertib sodium (MLN 8237) is a potent and specific inhibitor (IC50 = 1.2 nM) of Aurora A kinase, an enzyme involved in cell division. By binding to Aurora A kinase, Alisertib sodium disrupts the formation of the mitotic spindle and causes abnormal cell division. At the molecular level, it acts on the AKT/mTOR/AMPK/p38 pathway, leading to the induction of apoptosis and autophagy in leukemic cells. This compound exhibits significant antitumor activity.
Targets&IC50	Aurora A:12.5 nM (IC50), Aurora B:396.5 nM (IC50)
In vitro	Alisertib (MLN 8237) induces mitotic spindle abnormalities and accumulation in MM cells, leading to inhibition of cell proliferation via apoptosis and senescence. It also enhances the expression of p53 and the tumor suppressor genes p21 and p27[1]. The diminished efficacy of Alisertib (MLN 8237) against the T217D/W277E Aurora A/TPX2 complex might be due to the increased ATP affinity caused by cofactor binding to Aurora A[2]. Furthermore, Alisertib (MLN 8237) demonstrates inhibitory effects on various tumor cell lines with IC 50 values ranging from 15 to 469 nM[4].
In vivo	Alisertib (MLN 8237), administered at 30 mg/kg orally, significantly lowers tumor burden and enhances overall survival in a xenograft murine model of human multiple myeloma (MM)[1]. Additionally, when given orally at doses ranging from 3 to 30 mg/kg daily for a duration of three weeks, Alisertib demonstrated the capacity to inhibit tumor growth in models of solid tumor xenografts[4]. In a specific study involving nude mice with HCT-116 colon tumor xenografts, dosage levels of 3, 10, or 30 mg/kg administered orally once daily for three weeks yielded a dose-dependent tumor growth inhibition (TGI) of 43.3%, 84.2%, and 94.7%, respectively, indicating a potent anti-tumor activity across varying doses[4].

Synonyms	MLN 8237 sodium
Molecular Weight	541.92
Formula	C27H20ClFN4NaO4
CAS No.	1028486-06-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Keywords

Alisertib sodium 1028486-06-7 MLN 8237 sodium inhibitor inhibit

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