[CAS NO. 656820-32-5] Reversine
PRODUCTS SPECIFICATIONS [656820-32-5]
DESCRIPTION [656820-32-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 393.49 |
| Molecular Formula | C21H27N7O |
| SMILES | C1(NC2=CC=C(N3CCOCC3)C=C2)=NC(NC4CCCCC4)=C5C(NC=N5)=N1 |
8 Publications Citing Use of MCE
- [1]Cancer Res. 2021 Aug 1;81(15):4079-4093.
- [2]Cell Rep. 2018 Nov 27;25(9):2317-2328.e5.
- [3]J Biol Chem. 2019 Feb 8;294(6):2021-2035.
- [4]Onco Targets Ther. 2018 Feb 26;11:1025-1035.
- [5]Biochem Biophys Res Commun. 2020 Jul 12;528(1):105-111.
- [6]Chinese Pharmacological Bulletin, 2018, 34(12): 1740-1744.
- [7]Patent. US20180263995A1.
- [8]bioRxiv. Nov. 20, 2017.
Summary
Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC 50 s of 400, 500 and 400 nM for Aurora A , Aurora B and Aurora C , respectively.
IC50 & Target
|
Aurora A 400 nM (IC 50 ) |
Aurora B 500 nM (IC 50 ) |
Aurora C 400 nM (IC 50 ) |
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 IC 50 of Reversine is determined on Aurora kinase A to be 400 nM, whereas Aurora kinase B and C IC 50 are 500 and 400 nM, respectively. The IC 50 is also determined on MEK1 is >1.5 μM and that the IC 50 on muscle myosin (an analogue of nonmuscle myosin II) is 350 nM [1] .
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : 20 mg/mL ( 50.83 mM ; Need ultrasonic)
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 |
References
- [1] D'Alise AM, et al. Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells. Mol Cancer Ther. 2008 May;7(5):1140-9.
- [2] Qin HX, et al. Synergistic antitumor activity of reversine combined with aspirin in cervical carcinoma in vitro and in vivo. Cytotechnology. 2013 Aug;65(4):643-53.
Synonyms