554723-M

ATRA-BA Hybrid

The differentiation-inducer all-trans-Retinoic Acid and the histone deacetylase inhibitor (HDI) Butyric Acid.

• 別名: ATRA-BA Hybrid, 4-(Butanoyloxymethyl)phenyl-(2E,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohex-1-enyl)nona-2,4,6,8-tetraenoate, VNLG/124, HDAC Inhibitor XV, HDAC Inhibitor XV, 4-(Butanoyloxymethyl)phenyl-(2E,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohex-1-enyl)nona-2,4,6,8-tetraenoate, VNLG/124
• 実験式（ヒル表記法）: C₃₁H₄₀O₄
• 分子量: 476.65
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated; protect from light
• 色: yellow
• 溶解性: DMSO: 5 mg/mL
• 保管温度: −20°C

詳細

詳細

The differentiation-inducer all-trans-Retinoic Acid (ATRA; Cat. No. 554720) and the histone deacetylase inhibitor (HDI) Butyric Acid (BA; Cat. No. 567430) are incorporated chemically via a benzyl ester linkage into a single more permeant mutual prodrug (MP) to facilitate their cellular uptake and to better synergize their cancer killing potency. The growth inhibitions of PC-3 and MDA-MB-231 by the MP (IC₅₀ = 1.02 and 0.01 µM, respectively) are much superior to those achieved by separate (IC₅₀ = 7.6 and 10.85 µM, respectively, with ATRA; IC₅₀ = 72.44 and >1000 µM, respectively, with BA) or combined dosing of ATRA/BA (55% vs. 30% PC-3 growth inhibition by 10 µM MP vs. co-treatment of 10 µM each of ATRA & BA). At 37°C, VNLG/124 is completely converted to ATRA and BA within an hour in fresh murine plasma, but is otherwise stable for more than 24 hours in the absence of esterase activity in 20 mM PBS.

警告

Toxicity: Harmful (C)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

その他情報

Gediya, L.K., et al. 2008. J. Med. Chem.51, 3895.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable