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Reversine
A3 adenosine receptor antagonist,ARK-1/-2/-3 inhibitor

Reversine

Catalog No. A3760
Size Price Stock Qty
10mM (in 1mL DMSO) $77.00 In stock
5mg $70.00 In stock
10mg $90.00 In stock
25mg $180.00 In stock
50mg $250.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Reversine

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Chemical Properties

Cas No. 656820-32-5 SDF Download SDF
Chemical Name 6-N-cyclohexyl-2-N-(4-morpholin-4-ylphenyl)-7H-purine-2,6-diamine
Canonical SMILES C1CCC(CC1)NC2=NC(=NC3=C2NC=N3)NC4=CC=C(C=C4)N5CCOCC5
Formula C21H27N7O M.Wt 393.49
Solubility >19.7mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

IC50: 150, 500 and 400 nM for Aurora Kinase A, B and C respectively

Reversine is a novel Aurora kinases inhibitor. Aurora kinases are serine/threonine kinases playing a key role in mitotic regulation. Aurora A kinase resides at spindle poles during mitosis and is implicated in the control of centrosome maturation, duplication, and separation. Aurora B is part of a chromosome passenger complex and is implicated directly in the control of microtubule kinetochore attachment. Aurora kinases have emerged as valuable targets in cancer therapy.

In vitro: Reversine could be used to induce dedifferentiation of murine myoblasts. Previous reports also showed that reversine had a role in regeneration. Moreover, a recent report indicated reversine had anti-tumor capabilities for a myeloma cell line, as demonstrated by that reversine could suppress the expression of cell cycle related proteins Aurora kinase A and Aurora kinase B [1].

In vivo: The effects of reversine on tumor weight and volume were assessed using a murine model of cervical cancer with U14 cells, separately or combined with aspirin. The inhibition rate of cells in the combination group significantly increased; moreover, such combination could synergistically inhibit the proliferation of five cervical cancer cell lines. In the mouse model, tumor weight and volume of cervical cancer bearing mice were more reduced [1].

Clinical trial: N/A

Reference:
[1] Qin HX,Yang J,Cui HK,Li SP,Zhang W,Ding XL,Xia YH.  Synergistic antitumor activity of reversine combined with aspirin in cervical carcinoma in vitro and in vivo. Cytotechnology.2013 Aug;65(4):643-53.