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Merck
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Key Documents

554723-M

Millipore

ATRA-BA Hybrid

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

别名:

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

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About This Item

经验公式(希尔记法):
C31H40O4
分子量:
476.65
分類程式碼代碼:
12352200

品質等級

化驗

≥95% (HPLC)

形狀

solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
desiccated
protect from light

顏色

yellow

溶解度

DMSO: 5 mg/mL

儲存溫度

−20°C

一般說明

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)

重構

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

其他說明

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

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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