1. Cell Cycle/DNA Damage Epigenetics Autophagy Apoptosis
  2. Aurora Kinase Autophagy Apoptosis
  3. Alisertib

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.

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Alisertib Chemical Structure

Alisertib Chemical Structure

CAS No. : 1028486-01-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 42 publication(s) in Google Scholar

Other Forms of Alisertib:

Top Publications Citing Use of Products

39 Publications Citing Use of MCE Alisertib

IF
IHC
WB

    Alisertib 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 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.

    Alisertib 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.

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    • Biological Activity

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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)

    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

    518.92

    Formula

    C27H20ClFN4O4

    CAS No.
    Unlabeled CAS

    Appearance

    Solid

    Color

    Light yellow to light pink

    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    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.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.84%

    References

    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.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9271 mL 9.6354 mL 19.2708 mL 48.1770 mL
    5 mM 0.3854 mL 1.9271 mL 3.8542 mL 9.6354 mL
    10 mM 0.1927 mL 0.9635 mL 1.9271 mL 4.8177 mL
    15 mM 0.1285 mL 0.6424 mL 1.2847 mL 3.2118 mL
    20 mM 0.0964 mL 0.4818 mL 0.9635 mL 2.4088 mL
    25 mM 0.0771 mL 0.3854 mL 0.7708 mL 1.9271 mL
    30 mM 0.0642 mL 0.3212 mL 0.6424 mL 1.6059 mL
    40 mM 0.0482 mL 0.2409 mL 0.4818 mL 1.2044 mL
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      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.

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