Reversine
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。 |
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. |
质量控制和MSDS
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