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Reagents and instruments for immunology, cell biology and molecular biology.

Alisertib [1028486-01-2]

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Cat# HY-10971-5mg

Size : 5mg

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Description

Alisertib (MLN 8237) 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 (MLN 8237) 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

1.2 nM (IC₅₀)

Aurora B

396.5 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	GI₅₀	0.03 μM Compound: 10, alisertib	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay	[PMID: 26101564]
HCT-116	IC₅₀	1.5 μM Compound: 10, alisertib	Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis	[PMID: 26101564]
HCT-116	IC₅₀	32 μM Compound: MLN-8237	Antiproliferative activity against human HCT116 cells measured after 96 hrs by Brdu incorporation-based ELISA Antiproliferative activity against human HCT116 cells measured after 96 hrs by Brdu incorporation-based ELISA	[PMID: 31381325]
HCT-116	IC₅₀	7 nM Compound: 10, alisertib	Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis	[PMID: 26101564]
HCT-116	IC₅₀	95 nM Compound: 29, MLN-8237	Antiproliferative activity against human HCT116 cells after 72 hrs by WST8 assay Antiproliferative activity against human HCT116 cells after 72 hrs by WST8 assay	[PMID: 25625617]
HCT-15	IC₅₀	740 nM Compound: 29, MLN-8237	Antiproliferative activity against human HCT15 cells after 72 hrs by WST8 assay Antiproliferative activity against human HCT15 cells after 72 hrs by WST8 assay	[PMID: 25625617]
HL-60	IC₅₀	74 nM Compound: 29, MLN-8237	Antiproliferative activity against human HL60 cells after 72 hrs by WST8 assay Antiproliferative activity against human HL60 cells after 72 hrs by WST8 assay	[PMID: 25625617]
HT-29	IC₅₀	330 nM Compound: 29, MLN-8237	Antiproliferative activity against human HT-29 cells after 72 hrs by WST8 assay Antiproliferative activity against human HT-29 cells after 72 hrs by WST8 assay	[PMID: 25625617]
LC-2-ad	IC₅₀	77 nM Compound: 29, MLN-8237	Antiproliferative activity against human LC2/ad cells after 72 hrs by WST8 assay Antiproliferative activity against human LC2/ad cells after 72 hrs by WST8 assay	[PMID: 25625617]
LU-99A	IC₅₀	62 nM Compound: 29, MLN-8237	Antiproliferative activity against human LU99A cells after 72 hrs by WST8 assay Antiproliferative activity against human LU99A cells after 72 hrs by WST8 assay	[PMID: 25625617]
MIA PaCa-2	IC₅₀	130 nM Compound: 29, MLN-8237	Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST8 assay Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST8 assay	[PMID: 25625617]
MKN-45	IC₅₀	93 nM Compound: 29, MLN-8237	Antiproliferative activity against human MKN45 cells after 72 hrs by WST8 assay Antiproliferative activity against human MKN45 cells after 72 hrs by WST8 assay	[PMID: 25625617]
MRC5	IC₅₀	> 10000 nM Compound: 29, MLN-8237	Antiproliferative activity against human MRC5 cells after 72 hrs by WST8 assay Antiproliferative activity against human MRC5 cells after 72 hrs by WST8 assay	[PMID: 25625617]
MV4-11	IC₅₀	1.2 nM Compound: 17	Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation of cells at G2/M phase measured after 12 hrs Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation of cells at G2/M phase measured after 12 hrs	[PMID: 36306471]
NCI-H358	IC₅₀	100 nM Compound: 29, MLN-8237	Antiproliferative activity against human NCI-H358 cells after 72 hrs by WST8 assay Antiproliferative activity against human NCI-H358 cells after 72 hrs by WST8 assay	[PMID: 25625617]
PC-14	IC₅₀	170 nM Compound: 29, MLN-8237	Antiproliferative activity against human PC14 cells after 72 hrs by WST8 assay Antiproliferative activity against human PC14 cells after 72 hrs by WST8 assay	[PMID: 25625617]
Sf9	IC₅₀	1 nM Compound: 10, alisertib	Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP	[PMID: 26101564]

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.

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (48.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9271 mL	9.6354 mL	19.2708 mL
5 mM	0.3854 mL	1.9271 mL	3.8542 mL
10 mM	0.1927 mL	0.9635 mL	1.9271 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (4.01 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.01 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation

Purity: 99.84%

Data Sheet (283 KB) SDS (393 KB)

COA (260 KB) HNMR (175 KB) LCMS (435 KB) Elemental Analysis Report (118 KB)

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]

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Alisertib [1028486-01-2]

Cat# HY-10971-5mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

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