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

Alisertib (Synonyms: MLN 8237)

Cat. No.: HY-10971 Purity: 99.84%
Handling Instructions

Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor with an IC50 of 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 82 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 290 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg USD 850 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 17 publication(s) in Google Scholar

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.

    View All Aurora Kinase Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor with an IC50 of 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[4].
    Alisertib (MLN 8237) inhibits cell proliferation with IC50s ranging from 15 to 469 nM in different tumer cell lines[5].

    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 (MLN 8237) (20, 30 mg/kg, p.o.) causes tumor growth inhibition in solid tumor xenograft models and regressions in in vivo models of lymphoma, and reduces FLT uptake in HCT-116 xenograft tumors[5].

    Clinical Trial
    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 : 9.33 mg/mL (17.98 mM; Need ultrasonic and warming)

    H2O : < 0.1 mg/mL (insoluble)

    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:  10% DMSO    90% corn oil

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

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (4.82 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [2]

    To measure Aurora A activity, 25 ng (12.5 mM final concentration) or 250 ng (125 nM final concentration) of purified bacterially expressed Aurora A is assayed in the presence of the appropriate inhibitors (MLN8054, Alisertib), using Histone H3 as substrate for 20 min at 30°C in the presence of 100 μM [γ-32P] ATP. For Aurora A/TPX2 assays, 50 ng of a TPX2 [1-43] peptide, representing a 2-fold molar excess over Aurora A, is included. The Aurora A/TPX2 complex is preformed in kinase reactions prior to subsequent addition of inhibitors and ATP.

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

    Cell Assay
    [1]

    MM cell lines are incubated with DMSO or Alisertib (0.125-0.5 μM) in combination with conventional anti-MM agents for 72 hours. Cell viability is measured by MTT assay. The combination index (CI) is determined by isobologram analysis using CalcuSyn software, Version 2.0 (CI < 1 indicates synergistic effect; CI=1, additive effect; and CI > 1, no significant combination effect).

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

    Animal Administration
    [1]

    Mice are irradiated (200 cGy), and then 5×106 MM1.S cells are inoculated subcutaneously in the right flank. When tumor growth is measurable (2 weeks after the injection), mice are assigned into 4 groups (10 mice each) receiving vehicle orally (100 μL of 10% 2-hydroxypropyl-β-cyclodextrin/1% sodium bicarbonate) or Alisertib (7.5 mg/kg, 15 mg/kg, and 30 mg/kg in a final formulation in 10% 2-hydroxypropyl-β-cyclodextrin/1% sodium bicarbonate) for 21 consecutive days. The maximal tolerated dose of Alisertib in most mouse strains (continuous dosing for 21 days) is approximately 20 mg/kg twice a day (40 mg/kg per day). Tumor volumes are measured by a Vernier caliper every alternate day and calculated using the following formula: length×width2×0.5. Mice are killed at the end of the treatment, 2 hours after the last treatment, or when tumor reaches 2 cm3; tumors are immediately collected from mice and evaluated for induction of apoptosis and cell death by TdT-mediated dUTP nick end labeling (TUNEL) assay.

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

    References
    Molecular Weight

    518.92

    Formula

    C₂₇H₂₀ClFN₄O₄

    CAS No.

    1028486-01-2

    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

    Purity: 99.84%

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    Product Name:
    Alisertib
    Cat. No.:
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    Cat. No.: HY-10971