Alisertib [1028486-01-2]

Cat# HY-10971-5mg

Size : 5mg

Brand : MedChemExpress

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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
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.
Purity & Documentation
References

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