164640

Aminopurvalanol A

A cell-permeable 2,6,9-trisubstituted purine analog that displays anti-mitotic as well as anti-tumor properties.

• 别名: Aminopurvalanol A, (2R)-2-((6-((3-Amino-5-chlorophenyl)amino)-9-(1-methylethyl)-9H-purin-2-yl)amino)-3-methyl-1-butanol, NG-97
• 经验公式（希尔记法）: C₁₉H₂₆ClN₇O
• CAS号: 220792-57-4
• 分子量: 403.91
• UNSPSC代码: 12352200

属性

• 质量水平: 100
• 方案: ≥98% (HPLC)
• 表单: solid
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; protect from light
• 颜色: pale yellow
• 溶解性: DMSO: 40 mg/mL
• 运输: ambient
• 储存温度: 2-8°C
• InChI: 1S/C19H26ClN7O/c1-10(2)15(8-28)24-19-25-17(23-14-6-12(20)5-13(21)7-14)16-18(26-19)27(9-22-16)11(3)4/h5-7,9-11,15,28H,8,21H2,1-4H3,(H2,23,24,25,26)/t15-/m0/s1
• InChI key: RAMROQQYRRQPDL-HNNXBMFYSA-N

说明

一般描述

A cell-permeable 2,6,9-trisubstituted purine analog that displays anti-mitotic as well as anti-tumor properties (GI₅₀ = ~ 1.8 µM in the NCI 60-cell panel in vitro activity screen; potently inhibits the growth of KM12 colon cancer cells with a GI₅₀ of 30 nM). Acts as a reversible and ATP-competitive inhibitor of Cdks (IC₅₀ = 33 nM for Cdk1/cyclin B and Cdk2/cyclin A, 28 nM for Cdk2/cyclin E, and 20 nM for Cdk5/p35), and displays ~ 100-fold greater selectivity over a panel of kinases tested (IC₅₀ ≥ 2.4 µM). Shown to induce cell differentiation by preferentially targeting the G₂/M-phase and act intracellularly by inhibiting both Cdks and MAPKs.

生化/生理作用

Cell permeable: yes

Primary Target
Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p35

Product competes with ATP.

Reversible: yes

Target IC₅₀: 33 nM for Cdk1/cyclin B and Cdk2/cyclin A, 28 nM for Cdk2/cyclin E, and 20 nM for Cdk5/p35

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Breton, M.L., et al. 2003. Biochem. Biophys. Res. Commun.306, 880.
Knockaert, M., et al. 2002.Oncogene21, 6413.
Adachi, S., et al. 2001. Mol. Cell. Biol.21, 4929.
Knockaert, M., et al. 2000. Chem. Biol.7, 411.
Rosiana, G.R., et al. 1999. Proc. Natl. Acad. Sci. USA96, 4797.
Chang, Y.T., et al. 1999. Chem. Biol.6, 361.

法律信息

Sold under license of U.S. Patent 6,255,485 and 6,617,331.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 1