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Merck
CN

341326

Fatty Acid Synthase Inhibitor, Cpd 10v - CAS 1027354-00-2 - Calbiochem

Synonym(s):

7-chloro-4-hydroxy-3-(2ʹ-methoxybiphenyl-3-yl)-2-oxo-1,2-dihydroquinoline-6-carbonitrile, FAS inhibitor

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assay

≥98% (HPLC)

form

solid

color

white

solubility

DMSO: 50 mg/mL, clear, colorless

General description

A hydroxyquinolinone derivative that acts as a potent reversible inhibitor of type 1 fatty acid synthase (FAS) (IC50 = 19 nM) when enzyme activity is monitored by following the synthesis of free coenzyme A (CoA-SH).
The Fatty Acid Synthase Inhibitor, Cpd 10v, controls the biological activity of Fatty. This small molecule/inhibitor is primarily used for Cancer applications.

Preparation Note

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


Regulatory Information

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Alexey Rivkin et al.
Bioorganic & medicinal chemistry letters, 16(17), 4620-4623 (2006-06-21)
A series of 3-aryl-4-hydroxyquinolin-2(1H)-ones with fatty acid synthase inhibitory activity was prepared. Starting from a derivative with an IC(50) = 1.4 microM, SAR studies led to compounds with more than 70-fold increase in potency (IC(50) < 20 nM).