554723-M

ATRA-BA Hybrid

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

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₃₁H₄₀O₄
• Masa cząsteczkowa: 476.65
• Kod UNSPSC: 12352200

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated; protect from light
• kolor: yellow
• rozpuszczalność: DMSO: 5 mg/mL
• temp. przechowywania: −20°C

Opis

Opis ogólny

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.

Ostrzeżenie

Toxicity: Harmful (C)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable