Drug metabolism assessed as recombinant human CYP1A2-mediated 2-[[(R)-3-(2-Amino-pyrimidin-5-yl)-5,6,8a,9-tetrahydro-8H-7-oxa-2,4,4b-triaza-fluoren-1-yl]-(2-hydroxy-ethyl)-amino]-propionaldehyde formation incubated for 60 mins by LC-HRMS analysis
Drug metabolism assessed as recombinant human CYP1A1-mediated 2-[[(R)-3-(2-Amino-pyrimidin-5-yl)-8a,9-dihydro-8H-7-oxa-2,4,4b-triaza-fluoren-1-yl]-(2-hydroxy-ethyl)-amino]-propionaldehyde formation incubated for 60 mins by LC-HRMS analysis
Drug metabolism assessed as recombinant human CYP1A1-mediated 2-[[(R)-3-(2-Amino-pyrimidin-5-yl)-5,6,8a,9-tetrahydro-8H-7-oxa-2,4,4b-triaza-fluoren-1-yl]-(2-hydroxy-ethyl)-amino]-propionaldehyde formation incubated for 60 mins by LC-HRMS analysis
Inhibition of alexa fluor 647-labeled kinase tracer 314 binding to recombinant human N-terminal GST-fused mTOR (1360 to 2549 residues) expressed in baculovirus expression system by TR-FRET assay
Inhibition of mTORC1 in human A2058 cells assessed as reduction in ribosomal protein S6 phosphorylation at Ser235/236 residues incubated for 1 hr by Western blot analysis
Inhibition of alexa fluor 647-labeled kinase tracer 314 binding to recombinant human full-length N-terminal His6-tagged p110alpha/p85alpha expressed in baculovirus expression system by TR-FRET assay
Selectivity ratio of Ki for inhibition of alexa fluor 647-labeled kinase tracer 314 binding to recombinant human full-length N-terminal His6-tagged p110alpha/p85alpha expressed in baculovirus expression system to Ki for inhibition of alexa fluor 647-labeled kinase tracer 314 binding to recombinant human N-terminal GST-fused mTOR (1360 to 2549 residues) expressed in baculovirus expression system
Substrate activity at recombinant human CYP1A1 expressed in baculovirus infected insect cells assessed as parent compound remaining at 1 uM incubated for 60 mins in presence of NADP+-regenerating system by LC-MS analysis
Substrate activity at recombinant human CYP1A2 expressed in baculovirus infected insect cells assessed as parent compound remaining at 1 uM incubated for 60 mins in presence of NADP+-regenerating system by LC-MS analysis
Substrate activity at recombinant human CYP1A1 expressed in baculovirus infected insect cells assessed as parent compound remaining at 1 uM incubated for 60 mins in absence of NADP+-regenerating system by LC-MS analysis
Substrate activity at recombinant human CYP1A2 expressed in baculovirus infected insect cells assessed as parent compound remaining at 1 uM incubated for 60 mins in absence of NADP+-regenerating system by LC-MS analysis