164640

Aminopurvalanol A

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

• 同義詞: Aminopurvalanol A, (2R)-2-((6-((3-Amino-5-chlorophenyl)amino)-9-(1-methylethyl)-9H-purin-2-yl)amino)-3-methyl-1-butanol, NG-97
• 經驗公式（希爾表示法）: C₁₉H₂₆ClN₇O
• CAS號碼: 220792-57-4
• 分子量：: 403.91
• 分類程式碼代碼: 12352200

屬性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: pale yellow
• 溶解度: DMSO: 40 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 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 密鑰: RAMROQQYRRQPDL-HNNXBMFYSA-N

描述

一般說明

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

包裝

Packaged under inert gas

警告

Toxicity: Irritant (B)

重構

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

其他說明

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.

法律資訊

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

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 1