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2 using time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
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79957817552
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note
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Cell growth inhibitory assay: KARPAS-299 cells were treated with various concentrations of assay compounds for 96 h. Cell growth inhibition was determined by cell counting kit-8 assay.
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16
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79957857008
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note
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Microsomal stability assay: 1 μM of each compound was incubated with human (or mouse) liver microsome (0.5 mg protein/mL) in 50 mM phosphate buffer (pH 7.4) containing 1 mM NADPH (the reduced form of nicotinamide adenine dinucleotide phosphate) at 37 °C for 30 min. After the enzyme reaction was terminated with the addition of a three-fold volume of acetonitrile, the reaction mixture was centrifuged at 1500 rpm for 10 min. The resultant supernatant was used as a test sample to measure the stability in human (or mouse) liver microsome by quantitating the compound in the sample using LC/MS.
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77951095524
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79957857906
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note
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The quantity of enzyme and ATP and the kind of substrate and cation species added in each assay are given in Supplementary Table 1.
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79957820693
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note
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0 x 100, where W and W0 are the body weight on a specific experimental day and on the first day of treatment, respectively.
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