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557360 Sigma-AldrichRoscovitine - CAS 186692-46-6 - Calbiochem

Roscovitine, CAS 186692-46-6, is a potent, reversible, and selective inhibitor of CDKs. Displays 10 to 20 fold greater potency for p34cdk1, p33cdk2, and p33cdk5 relative to Olomoucine.

Roscovitine - CAS 186692-46-6 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

分析证书
参考
Data Sheet
Citations

同义词: 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine, Cdk7 Inhibitor I

Primary Target: p34^cdk1/cyclin B

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
186692-46-6	C₁₉H₂₆N₆O

价格及供货情况

产品目录编号	库存情况	包装	数量 / 包装	价格	数量
557360-1MGCN	正在查询供货情况...... — 目前缺货有货停产少量现货供货情况有待确认登录查看库存有货目前缺货有货其余：另行通知其余：另行通知另行通知联系客户服务 Contact Customer Service 联系客户服务联系客户服务	塑胶安瓿;塑胶针药瓶	1 mg	正在检索价格...... 无法检索价格。最小订购数量为倍数 Maximum Quantity is 以订单确认为准更多信息您节约了 ()。 — Request Pricing 登录查看价格	查看库存情况 —	添加到收藏夹添加到收藏夹添加到我的收藏夹
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Description
Overview	A potent, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks) that exhibits about ten-fold greater efficacy towards p34^cdk1 and p33^cdk2 and twenty-fold greater efficacy towards p33^cdk5 relative to Olomoucine (Cat. No. 495620). Inhibits p34^cdk1/cyclin B (IC₅₀ = 650 nM), p33^cdk2/cyclin A (IC₅₀ = 700 nM), p33^cdk2/cyclin E (IC₅₀ = 700 nM), and p33^cdk5/p35 (IC₅₀ = 200 nM) by competing for the ATP binding domain of the kinases. Exhibits reduced sensitivity towards related kinases including ERK1 and ERK2 (IC₅₀ = 34 µM and 14 µM, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 µM, including p34^cdk4/cyclin D1 and p40^cdk6/cyclin D2. Compared to olomoucine, roscovitine displays increased anti-mitotic activity at the G₁/S and G₂/M phases of the cell cycle. A 50 mM (5 mg/282 µl) solution of Roscovitine (Cat. No. 557364) in DMSO is also available.
Catalogue Number	557360
Brand Family	Calbiochem®
Synonyms	2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine, Cdk7 Inhibitor I

References
References	De Azevedo, W.F., et al. 1997. Eur. J. Biochem. 243, 518. Meijer, L., et al. 1997. Eur. J. Biochem. 243, 527. Meijer, L., et al. 1996. Trends Cell Biol. 6, 393. Rudolph, B., et al. 1996. EMBO J. 15, 3053.

Product Information
CAS number	186692-46-6
ATP Competitive	N
Declaration	Sold under license of U.S. Patent 6,316,456
Form	White to off-white solid
Hill Formula	C₁₉H₂₆N₆O
Chemical formula	C₁₉H₂₆N₆O
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications
Application	Roscovitine, CAS 186692-46-6, is a potent, reversible, and selective inhibitor of CDKs. Displays 10 to 20 fold greater potency for p34cdk1, p33cdk2, and p33cdk5 relative to Olomoucine.

Biological Information
Primary Target	p34^cdk1/cyclin B
Primary Target IC<sub>50</sub>	650 nM, 700 nM, 700 nM, 200 nM, against p34cdk1/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, p33cdk5/p35, respectively
Purity	≥95% by HPLC

Physicochemical Information
Cell permeable	N

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	-20°C
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for at least 6 months at -20°C.

Packaging Information

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
557360-1MGCN	04055977267983
557360-5MGCN	07790788051495

Documentation

Roscovitine - CAS 186692-46-6 - Calbiochem 分析证书

标题	批号
557360	输入批号

参考

参考信息概述
De Azevedo, W.F., et al. 1997. Eur. J. Biochem. 243, 518. Meijer, L., et al. 1997. Eur. J. Biochem. 243, 527. Meijer, L., et al. 1996. Trends Cell Biol. 6, 393. Rudolph, B., et al. 1996. EMBO J. 15, 3053.

引用

标题

Linsheng Zhang, et al. (2008) Cyclin-dependent kinase phosphorylation of RUNX1/AML1 on 3 sites increases transactivation potency and stimulates cell proliferation. Blood 111, 1193-1200.

Marc Payton, et al. (2006) Discovery and Evaluation of Dual CDK1 and CDK2 Inhibitors. Cancer Research 66, 4299-4308.

Meng Qiao, et al. (2006) Cell cycle-dependent phosphorylation of the RUNX2 transcription factor by cdc2 regulates endothelial cell proliferation. Journal of Biological Chemistry 281, 7118-7128.

Marie Futter, et al. (2005) Phosphorylation of spinophilin by ERK and cyclin-dependent PK 5 (Cdk5). Procedings of the National Academy of Science 102, 3489-3494.

Ping Han, et al. (2005) Suppression of Cyclin-Dependent Kinase 5 Activation by Amyloid Precursor Protein: A Novel Excitoprotective Mechanism Involving Modulation of Tau Phosphorylation. Journal of Neuroscience 25, 11542-11552.

Oscar M. Tirado, Silvia Mateo-Lozano and Vicente Notario. (2005) Roscovitine is an effective inducer of apoptosis of Ewing's sarcoma family of tumor cells in vitro and in vivo. Cancer Research 65, 9320-9327.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	05-October-2010 JSW
Synonyms	2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine, Cdk7 Inhibitor I
Description	A potent, reversible, and selective inhibitor of cyclin-dependent kinases (cdks). Exhibits greater inhibitory potency compared to olomoucine (Cat. No. 495620). Inhibits p34 ^cdc2/cyclin B (IC₅₀ = 0.65 µM), p33 ^cdk2/cyclin A (IC₅₀ = 0.70 µM), p33 ^cdk2/cyclin E (IC₅₀ = 0.70 µM), and p33 ^cdk5/p35 (IC₅₀ = 0.20 µM) by competing for the ATP binding domain of these kinases. Exhibits very low sensitivity towards related kinases, such as erk1 and erk2 (IC₅₀ = 34 µM and 14 µM, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 µM and compared to olomoucine, roscovitine displays increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle.
Form	White to off-white solid
CAS number	186692-46-6
Chemical formula	C₁₉H₂₆N₆O
Structure formula
Purity	≥95% by HPLC
Solubility	DMSO (10 mg/ml)
Storage	-20°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for at least 6 months at -20°C.
Toxicity	Standard Handling
References	De Azevedo, W.F., et al. 1997. Eur. J. Biochem. 243, 518. Meijer, L., et al. 1997. Eur. J. Biochem. 243, 527. Meijer, L., et al. 1996. Trends Cell Biol. 6, 393. Rudolph, B., et al. 1996. EMBO J. 15, 3053.
Citation	Linsheng Zhang, et al. (2008) Cyclin-dependent kinase phosphorylation of RUNX1/AML1 on 3 sites increases transactivation potency and stimulates cell proliferation. Blood 111, 1193-1200. Marc Payton, et al. (2006) Discovery and Evaluation of Dual CDK1 and CDK2 Inhibitors. Cancer Research 66, 4299-4308. Meng Qiao, et al. (2006) Cell cycle-dependent phosphorylation of the RUNX2 transcription factor by cdc2 regulates endothelial cell proliferation. Journal of Biological Chemistry 281, 7118-7128. Marie Futter, et al. (2005) Phosphorylation of spinophilin by ERK and cyclin-dependent PK 5 (Cdk5). Procedings of the National Academy of Science 102, 3489-3494. Ping Han, et al. (2005) Suppression of Cyclin-Dependent Kinase 5 Activation by Amyloid Precursor Protein: A Novel Excitoprotective Mechanism Involving Modulation of Tau Phosphorylation. Journal of Neuroscience 25, 11542-11552. Oscar M. Tirado, Silvia Mateo-Lozano and Vicente Notario. (2005) Roscovitine is an effective inducer of apoptosis of Ewing's sarcoma family of tumor cells in vitro and in vivo. Cancer Research 65, 9320-9327.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Cell Cycle/Cell Division > Cyclin-Dependent Kinase (Cdk) Inhibitors

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