CAS RN: 186692-46-6 | Product Number: R0207

Roscovitine

Purity: >98.0%(HPLC)(qNMR)

Synonyms:

Seliciclib
CYC 202
(R)-2-[[6-(Benzylamino)-9-isopropyl-9H-purin-2-yl]amino]butan-1-ol

Product Documents:

Size	Unit Price	Belgium	Japan*	Quantity
20MG	€149.00	Contact Us	37

*Stock available in Belgium will be delivered in 1 to 3 days
*Stock available in Japan will be delivered in 1 to 2 weeks (excludes regulated items and dry ice shipments).

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General Information plus

Product Number	R0207
Purity / Analysis Method	>98.0%(HPLC)(qNMR)
Molecular Formula / Molecular Weight	C__1__9H__2__6N__6O = 354.46
Physical State (20 deg.C)	Solid
Storage Temperature	Frozen (-20°C)
Store Under Inert Gas	Store under inert gas
Condition to Avoid	Air Sensitive,Heat Sensitive
CAS RN	186692-46-6
Reaxys Registry Number	7694281
MDL Number	MFCD02266401

Specifications & Properties plus

Specifications

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

Properties (reference)

Melting Point	108 °C
Solubility in water	Insoluble
Solubility (soluble in)	Acetone, Ethanol

Safety & Regulations plus

GHS

Related Laws:

RTECS#

EL5610000

Transport Information:

HS Number

2933998090

Applications & Literature plus

Application

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
- L. Meijer, A. Borgne, O. Mulner, J. P. J. Chong, J. J. Blow, N. Inagaki, M. Inagaki, J.-G. Delcros, J.-P. Moulinoux, Eur. J. Biochem. 1997, 243, 527.
Inhibition of Cyclin-Dependent Kinases by Purine Analogues: Crystal Structure of Human cdk2 Complexed with Roscovitine
- W. F. De Azevedo, S. Leclerc, L. Meijer, L. Havlicek, M. Strnad, S.-H. Kim, Eur. J. Biochem. 1997, 243, 518.
In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine)
- S. J. McClue, D. Blake, R. Clarke, A. Cowan, L. Cummings, P. M. Fischer, M. MacKenzie, J. Melville, K. Stewart, S. Wang, N. Zhelev, D. Zheleva, D. P. Lane, Int. J. Cancer 2002, 102, 463.
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
- D. E. MacCallum, J. Melville, S. Frame, K. Watt, S. Anderson, A. Gianella-Borradori, D. P. Lane, S. R. Green, Cancer Res. 2005, 65, 5399.
Roscovitine in cancer and other diseases (a review)
- J. Cicenas, K. Kalyan, A. Sorokinas, E. Stankunas, J. Levy, I. Meskinyte, V. Stankevicius, A. Kaupinis, M. Valius, Ann. Transl. Med. 2015, 3, 135.

Application

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.)