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554723-M

ATRA-BA Hybrid

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

Synonym(e):

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

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PackungsgrößeSKUVerfügbarkeitPreis
25 mg
Warenkorb auf Verfügbarkeit prüfen
€ 176,00

Über diesen Artikel

Empirische Formel (Hill-System):
C31H40O4
Molekulargewicht:
476.65
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, desiccated, protect from light

€ 176,00


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Quality Level

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated, protect from light

color

yellow

solubility

DMSO: 5 mg/mL

storage temp.

−20°C

General description

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.

Preparation Note

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

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Harmful (C)

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Dieser Artikel
PHR2919075581011029
assay

≥95% (HPLC)

assay

-

assay

≥90.0% (HPLC)

assay

-

form

solid

form

-

form

-

form

-

manufacturer/tradename

Calbiochem®

manufacturer/tradename

-

manufacturer/tradename

-

manufacturer/tradename

USP

Quality Level

100

Quality Level

300

Quality Level

100

Quality Level

-

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

-

storage temp.

-

storage condition

OK to freeze, protect from light, desiccated

storage condition

-

storage condition

-

storage condition

-


Lagerklasse

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Verwandter Inhalt

Cancer is a complex disease manifestation. At its core, it remains a disease of abnormal cellular proliferation and inappropriate gene expression. In the early days, carcinogenesis was viewed simply as resulting from a collection of genetic mutations that altered the gene expression of key oncogenic genes or tumor suppressor genes leading to uncontrolled growth and disease (Virani, S et al 2012). Today, however, research is showing that carcinogenesis results from the successive accumulation of heritable genetic and epigenetic changes. Moreover, the success in how we predict, treat and overcome cancer will likely involve not only understanding the consequences of direct genetic changes that can cause cancer, but also how the epigenetic and environmental changes cause cancer (Johnson C et al 2015; Waldmann T et al 2013). Epigenetics is the study of heritable gene expression as it relates to changes in DNA structure that are not tied to changes in DNA sequence but, instead, are tied to how the nucleic acid material is read or processed via the myriad of protein-protein, protein-nucleic acid, and nucleic acid-nucleic acid interactions that ultimately manifest themselves into a specific expression phenotype (Ngai SC et al 2012, Johnson C et al 2015). This review will discuss some of the principal aspects of epigenetic research and how they relate to our current understanding of carcinogenesis. Because epigenetics affects phenotype and changes in epigenetics are thought to be key to environmental adaptability and thus may in fact be reversed or manipulated, understanding the integration of experimental and epidemiologic science surrounding cancer and its many manifestations should lead to more effective cancer prognostics as well as treatments (Virani S et al 2012).





Global Trade Item Number

SKUGTIN
554723-25MG04055977193138

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