Displacement of [3H]ZM241385 from human A2AAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]ZM241385 addition and measured after 1.5 hrs by TopCount scintillation counting method
Displacement of [3H]DPCPX from human A1AR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
Antitumor activity against mouse 4T1 cells allografted in BALB/c mouse assessed as tumor growth inhibition at 25 mg/kg, ip administered once daily for 25 days relative to control
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
Displacement of [3H]HEMADO from human A3AR expressed in CHO-K1 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]HEMADO addition and measured after 1.5 hrs by TopCount scintillation counting method
Antitumor activity against mouse 4T1 cells implanted in BALB/c mouse assessed as tumor growth inhibition at 25 mg/kg, po administered once daily for 25 days relative to control