Inhibition of human MCT4 in human MDA-MB-231 cells assessed as inhibition of lactate efflux preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by dialysis based UHPLC-ESI-Q-Orbitrap-MS analysis
Inhibition of human MCT4 in human NCI-H358 cells assessed as inhibition of lactate efflux preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by dialysis based UHPLC-ESI-Q-Orbitrap-MS analysis
Inhibition of human MCT4 in human NCI-H441 cells assessed as inhibition of lactate efflux preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by dialysis based UHPLC-ESI-Q-Orbitrap-MS analysis
Oral bioavailability in C57/BL6 mouse at 30 mg/kg administered as homogeneous suspension in 0.5% methocel/0.25% tween20 in 50 mM phosphate buffer (pH 7.4) and measured after 2 hrs by HPLC-MS/MS analysis
Free drug exposure in C57/BL6 mouse plasma assessed as time to exceeding cellular IC50 at 30 mg/kg,po administered as homogeneous suspension in 0.5% methocel/0.25% tween20 in 50 mM phosphate buffer (pH 7.4) by HPLC-MS/MS analysis
Invivo inhibition of lactate efflux in human NCI-H358 cells expressing high MCT4 and low MCT1 xenografted in C57/BL6 mouse assessed as decrease in intracellular tumor lactate accumulation at 100 mg/kg,po BID and measured after 2 hrs by Dialysis method
Invivo inhibition of lactate efflux in human NCI-H441 cells expressing high MCT4 and low MCT1 xenografted in C57/BL6 mouse assessed as decrease in intracellular tumor lactate accumulation at 100 mg/kg,po BID and measured after 2 hrs by Dialysis method
Antitumor activity in human NCI-H358 cells expressing high MCT4 and low MCT1 xenografted in C57/BL6 mouse assessed as tumor growth inhibition at 100 mg/kg,po BID and measured after 2 hrs
Antitumor activity in human NCI-H441 cells expressing high MCT4 and low MCT1 xenografted in C57/BL6 mouse assessed as tumor growth inhibition at 100 mg/kg,po BID and measured after 2 hrs
Invivo inhibition of lactate efflux in human MDA-MB-231 cells expressing high MCT4 and no MCT1 xenografted in C57/BL6 mouse assessed as decrease in intracellular tumor lactate accumulation at 100 mg/kg,po BID and measured after 2 hrs by Dialysis method
Antitumor activity in human MDA-MB-231 cells expressing high MCT4 and low MCT1 xenografted in C57/BL6 mouse assessed as tumor growth inhibition at 100 mg/kg,po BID and measured after 2 hrs