Alisertib sodium (Synonyms: MLN 8237 sodium)

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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.

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Alisertib sodium Chemical Structure

CAS No. : 1028486-06-7

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38 Publications Citing Use of MCE Alisertib sodium

IHC

: Alisertib sodium purchased from MedChemExpress. Usage Cited in: FASEB J. 2018 May;32(5):2735-2746. [Abstract]; Representative immunofluorescence (IF) image and graph with frequency of ciliated WT or Pkd12/2 murine renal epithelial cells at 2 h after treatment with vehicle (V), Ganetespib (G), or Alisertib (A) to inhibit AURKA, or (C) combination of Alisertib and Ganetespib. On IF, acetylated a-tubulin (red); g-tubulin (green); DAPI (blue).

: Alisertib sodium purchased from MedChemExpress. Usage Cited in: College of Medicine. Drexel University. 2016 Nov.; Alisertib enhances FRAX1036 inhibitory effect on PAK1 phosphorylation in BT474 xenograft model.

: Alisertib sodium purchased from MedChemExpress. Usage Cited in: College of Medicine. Drexel University. 2016 Nov.; Alisertib and combination treatment suppress proliferation in BT474 orthotopic tumors as shown by decrease in Ki-67, which is statistically significantly different between vehicle and combination treatment, FRAX1036 and Alisertib, and FRAX1036 and combination treatment.

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Description

IC₅₀ & Target^[3]

Aurora A

12.5 nM (IC₅₀)

Aurora B

396.5 nM (IC₅₀)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) 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

Molecular Weight

540.91

Formula

C₂₇H₁₉ClFN₄NaO₄

CAS No.

1028486-06-7

SMILES

O=C(C1=CC=C(C=C1OC)NC2=NC=C3CN=C(C4=CC(Cl)=CC=C4C3=N2)C5=C(C=CC=C5F)OC)O[Na]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

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

[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. [Content Brief]

Alisertib sodium Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Alisertib1028486-06-7MLN 8237MLN8237MLN-8237Aurora KinaseAutophagyApoptosiscytotoxicitycell-cyclearrestmultiplemyelomamitoticspindlecancerInhibitorinhibitorinhibit

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