Reversine

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Reversine

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

656820-32-5

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议

产品介绍

化学性质

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
Canonical SMILES	C1CCC(CC1)NC2=NC(=NC3=C2NC=N3)NC4=CC=C(C=C4)N5CCOCC5
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

IC50：作用于Aurora激酶A、B和C的IC50分别为150、500和400 nM。

Reversine是一种新型Aurora激酶抑制剂。Aurora激酶是丝氨酸/苏氨酸激酶，在有丝分裂调控中起关键作用。Aurora A激酶在有丝分裂期间存在于纺锤极，控制中心体的成熟、复制和分离。Aurora B是染色体移动复合物的一部分，并与微管着丝点附着的控制直接相关。Aurora激酶已成为癌症治疗中有价值的靶点。

体外：Reversine可用于诱导小鼠成肌细胞的去分化。前期报告还显示，reversine有再生作用。此外，近期一份报告指出，reversine对骨髓瘤细胞系具有抗肿瘤功能，reversine能抑制细胞周期相关蛋白Aurora激酶A和Aurora激酶B的表达[1]。

体内：使用具有U14细胞的宫颈癌小鼠模型评估reversine单独用药或与阿司匹林联合用药对肿瘤重量和体积的影响。联合用药组的细胞抑制率显著增加；此外，这种联合用药能协同抑制五个宫颈癌细胞系的增殖。在小鼠模型中，携带宫颈癌小鼠的肿瘤重量和体积进一步减小[1]。

临床试验：N/A

参考文献：
[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.

试验操作

Cell experiment:[1]
Cell lines	Mouse cervical carcinoma cell line U14, as well as human cervical carcinoma cell lines HeLa, Siha, Caski and C33A
Reaction Conditions	10 μmol/L reversine for 48 h incubation
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]
Animal models	A murine model of cervical cancer with U14 cells subcutaneously administered into the neck
Dosage form	10 mg/kg Administrated by intraperitoneal injection per 3 days
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.
Note	The technical data provided above is for reference only.
	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.