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

Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC50s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.

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

Reversine Chemical Structure

Reversine Chemical Structure

CAS No. : 656820-32-5

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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Reversine purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2018 Feb 26;11:1025-1035.  [Abstract]

    Reversine inhibits the expression levels of Cyclin A2, Cyclin B1, and p-Rb, but promotes p21 expression.

    Reversine purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2018 Feb 26;11:1025-1035.  [Abstract]

    Reversine inhibits the expression levels of Cyclin A2, Cyclin B1, and p-Rb, but promotes p21 expression.

    Reversine purchased from MedChemExpress. Usage Cited in: Chinese Pharmacological Bulletin, 2018, 34(12): 1740-1744.

    Western analysis of Cleaved-PARP, beta-tubulin, Bcl-2, Bcl-xL, Bax protein expression in the treatment of Reversine with different concentrations.

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    Description

    Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC50s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.

    IC50 & Target[1]

    Aurora A

    400 nM (IC50)

    Aurora B

    500 nM (IC50)

    Aurora C

    400 nM (IC50)

    In Vitro

    Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells. Reversine is a potent inhibitor of Aurora A and B and is also an inhibitor of Aurora C kinase. Aurora A and B activities are inhibited by 80% and Aurora kinase C by 55%, already at a concentration of 0.5 μM, whereas no inhibition or only modest inhibition is observed on others kinases tested. In a second round of experiments, the IC50 of Reversine is determined on Aurora kinase A to be 400 nM, whereas Aurora kinase B and C IC50 are 500 and 400 nM, respectively. The IC50 is also determined on MEK1 is >1.5 μM and that the IC50 on muscle myosin (an analogue of nonmuscle myosin II) is 350 nM[1].

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

    In Vivo

    The combination of Reversine and Aspirin can more efficiently induce cell cycle arrest and apoptosis. To evaluate the anti-tumor effect of this combination, a xenograft nude mouse model is established by s.c. injection. Mice inoculated with cervical cancer cells have lost about 10 % of their initial body weight by about 16 days after tumor inoculation. However, tumor growth (tumor weight) is reduced and the mice survive longer in the combination group[2].

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

    Molecular Weight

    393.49

    Formula

    C21H27N7O

    CAS No.
    Appearance

    Solid

    Color

    Light green to green

    SMILES

    C1(NC2=CC=C(N3CCOCC3)C=C2)=NC(NC4CCCCC4)=C5C(NC=N5)=N1

    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 : 20 mg/mL (50.83 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 2.5414 mL 12.7068 mL 25.4136 mL
    5 mM 0.5083 mL 2.5414 mL 5.0827 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.

    • Molarity Calculator

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    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.
    Purity & Documentation

    Purity: 99.22%

    References
    Cell Assay
    [1]

    HCT116 and HL60 cells are incubated with either 5 μmol/L Reversine or DMSO 0.01%. Cells are harvested and fixed in 70% ethanol overnight. After double washing with PBS, cells are labeled with cell cycle staining reagent PBS, 0.1% Triton X-100, 200 μg/mL DNase-free RNase, and 25 μg/mL propidium iodide and incubated at room temperature in the dark for 30 min. DNA content is analyzed using FACSCalibur. Cell viability of different tumor cell lines is assessed using ATPlite 1step. Briefly, 2×104 cells for each well are plated in a 96-well plate in presence of crescent quantity of Reversine. After 72 h, the plates are recovered and 100 μL ATPlite solution is added to each well. The plates are shaken for 2 min at 700 rpm and luminescence is measured using EnVision Multilabel plate reader. Each sample is analyzed in triplicate[1].

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

    Animal Administration
    [2]

    Mice[2]
    Female athymic 6-8 weeks old BALB/c nude mice are used. U14 cell suspension (5×106 cells in 100 μL of RPMI-1640 medium) is injected subcutaneously. The purpose of developing cervical tumors is to generate histological intact tumors for drug therapy. When the diameter of tumors reached up to about 1 cm, Reversine, aspirin or their combinations are administrated by intraperitoneal injection per 3 days, twenty-five of these mice are randomly assigned into one of the following five groups: (a) mice treated with RPMI-1640 medium, (b) mice treated with DMSO, (c) mice treated with Reversine (10 mg/kg), (d) mice treated with aspirin (1 μg/kg) and (e) mice treated with a Reversine and aspirin combination. Body weight and tumor size at the site of inoculation are measured three times a week. Tumor size is measured every 3 days from two diameters, tumor volume is estimated using the formula L×S2/2(L as the longest diameter, S as the shortest diameter).

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

    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 2.5414 mL 12.7068 mL 25.4136 mL 63.5340 mL
    5 mM 0.5083 mL 2.5414 mL 5.0827 mL 12.7068 mL
    10 mM 0.2541 mL 1.2707 mL 2.5414 mL 6.3534 mL
    15 mM 0.1694 mL 0.8471 mL 1.6942 mL 4.2356 mL
    20 mM 0.1271 mL 0.6353 mL 1.2707 mL 3.1767 mL
    25 mM 0.1017 mL 0.5083 mL 1.0165 mL 2.5414 mL
    30 mM 0.0847 mL 0.4236 mL 0.8471 mL 2.1178 mL
    40 mM 0.0635 mL 0.3177 mL 0.6353 mL 1.5884 mL
    50 mM 0.0508 mL 0.2541 mL 0.5083 mL 1.2707 mL
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    Cat. No.:
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