Reversine
(Synonyms: 逆转素) 目录号 : GC14651
A purine derivative
Cas No.:656820-32-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
|
Cell experiment: |
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]. |
|
Animal experiment: |
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). |
|
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. |
|
| Cas No. | 656820-32-5 | SDF | |
| 别名 | 逆转素 | ||
| 化学名 | 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 | ||
| 分子式 | C21H27N7O | 分子量 | 393.49 |
| 溶解度 | ≥ 19.65 mg/mL in DMSO, ≥ 6.69 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet