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

Alisertib (Synonyms: MLN 8237)

Cat. No.: HY-10971 Purity: 99.22%
Handling Instructions

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.

For research use only. We do not sell to patients.

Alisertib Chemical Structure

Alisertib Chemical Structure

CAS No. : 1028486-01-2

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10 mM * 1 mL in DMSO USD 82 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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5 mg USD 72 In-stock
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10 mg USD 120 In-stock
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50 mg USD 290 In-stock
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100 mg USD 450 In-stock
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200 mg USD 850 In-stock
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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of Alisertib:

Top Publications Citing Use of Products

    Alisertib purchased from MCE. Usage Cited in: FASEB J. 2018 May;32(5):2735-2746.

    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 MCE. 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 MCE. 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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    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].

    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].

    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.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (48.18 mM; Need ultrasonic)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 2.5 mg/mL (4.82 mM); Clear solution

    • 2.

      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

    • 3.

      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

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.01 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.84%

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