Reversine
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 393.49 |
| Cas No. | 656820-32-5 |
| Formula | C21H27N7O |
| Solubility | insoluble in H2O; ≥19.65 mg/mL in DMSO; ≥6.69 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 6-N-cyclohexyl-2-N-(4-morpholin-4-ylphenyl)-7H-purine-2,6-diamine |
| SDF | Download SDF |
| Canonical SMILES | C1CCC(CC1)NC2=NC(=NC3=C2NC=N3)NC4=CC=C(C=C4)N5CCOCC5 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Mouse cervical carcinoma cell line U14, as well as human cervical carcinoma cell lines HeLa, Siha, Caski and C33A |
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Reaction Conditions |
10 μmol/L reversine for 48 h incubation |
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Applications |
The inhibition rate of cells in the combination group (10 μmol/L reversine, 10 mmol/L aspirin) increased significantly in comparison to that when the drugs were used alone. Moreover, this combination could synergistically inhibit the proliferation of five cervical cancer cell lines (HeLa, U14, Siha, Caski and C33A). |
| Animal experiment:[1] | |
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Animal models |
A murine model of cervical cancer with U14 cells subcutaneously administered into the neck |
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Dosage form |
10 mg/kg Administrated by intraperitoneal injection per 3 days |
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Applications |
In the therapeutic mouse model, tumor weight and tumor volume of cervical cancer bearing mice were more reduced when compared with the control agents in tumor-bearing mice. The combination of reversine and aspirin exerted synergistic growth inhibition and apoptosis induction on cervical cancer cells. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Qin HX, Yang J, Cui HK, et al. Synergistic antitumor activity of reversine combined with aspirin in cervical carcinoma in vitro and in vivo. Cytotechnology, 2013, 65(4): 643-653. |
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