1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase

Reversine 

Cat. No.: HY-14711 Purity: 99.25%
Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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].

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].

Solvent & Solubility
In Vitro: 

10 mM in 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
10 mM 0.2541 mL 1.2707 mL 2.5414 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

393.49

Formula

C₂₁H₂₇N₇O

CAS No.

656820-32-5

SMILES

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

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

Room temperature in continental US; may vary elsewhere

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Product Name:
Reversine
Cat. No.:
HY-14711
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Reversine

Cat. No.: HY-14711