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CAS RN: 186692-46-6 | 产品编码: R0207
产品编码 | R0207 |
纯度/分析方法 | >98.0%(HPLC)(qNMR) |
分子式/分子量 | C__1__9H__2__6N__6O = 354.46 |
外观与形状(20°C) | 固体 |
储存温度 | 冷冻 (-20°C) |
储存在惰性气体下 | 存放于惰性气体之中 |
应避免的情况 | 空气,加热 |
CAS RN | 186692-46-6 |
Reaxys-RN | 7694281 |
MDL编号 | MFCD02266401 |
技术规格
Appearance | White to Light yellow powder to crystal |
Purity(HPLC) | min. 98.0 area% |
Purity(qNMR) | min. 98.0 % |
Specific rotation | +50.0 to +56.0 deg(C=1, CHCL3) |
NMR | confirm to structure |
物性(参考值)
熔点 | 108 °C |
水溶性 | 不溶 |
溶解性(可溶于) | 丙酮, 乙醇 |
GHS
相关法规
RTECS# | EL5610000 |
运输信息
HS编码* | 2933.59-000 |
应用
Roscovitine: A Broad-Range Purine Analog CDK Inhibitor
Cyclin-dependent kinases (CDKs) are key regulatory proteins that control the cell cycle and are therefore promising targets for cancer research. Roscovitine (CYC202) has been reported to be a potent CDK inhibitor that competes for ATP binding sites on these kinases, reducing tumor growth and inducing cell death. Roscovitine inhibits CDK1, CDK2, CDK5, CDK7 and CDK9 (IC50 ~0.2-0.7 µM) but is a poor inhibitor for CDK4, CDK6 and CDK8 (IC50 >100 µM). (The product is for research purpose only.)
References
- Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2, and cdk5
- Inhibition of Cyclin-Dependent Kinases by Purine Analogues: Crystal Structure of Human cdk2 Complexed with Roscovitine
- In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine)
- Seliciclib (CYC202, R-Roscovitine) Induces Cell Death in Multiple Myeloma Cells by Inhibition of RNA Polymerase II-Dependent Transcription and Down-regulation of Mcl-1
- Roscovitine in cancer and other diseases (a review)
应用
Roscovitine: A Cyclin-Dependent Kinase (CDK) Inhibitor
Cyclins and cyclin-dependent kinases (CDKs) are a key component of the regulatory proteins that control the cell cycle. CDK plays a critical role in regulating the cell cycle transition and is primarily involved in the pathogenesis of cancer. Roscovitine (CYC202) is a CDK inhibitor that competes for ATP binding sites on these kinases, thereby reducing tumor growth and inducing cell death. There are reports that roscovitine inhibits CDK1, CDK2, CDK5 and CDK7 and leads to growth arrest and apoptosis of tumor cell lines. Roscovitine does not significantly affect the activity of other protein kinases. Therefore, roscovitine has been used as an anti-mitotic reagent for cell cycle research. (The product is for research purpose only.)
References
- Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2, and cdk5
- In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine)
- Roscovitine and Other Purines as Kinase Inhibitors. From Starfish Oocytes to Clinical Trials (a review)
- Roscovitine in cancer and other diseases (a review)
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