Induction of DNA modifying activity in human Jurkat cells assessed as increase in DNA-protein crosslink at 3 mM under aerobic condition by K-SDS assay (Rvb = 4.5. +/- 1.5%)
Drug level in glycine buffer treated with Sodium (((5bS,6aS,7aR,8R,8aS,9aS,9bS,10aS,10bS)-8a-Isopropyl-10b-methyl-3-oxo-1,2,3,5,5b,6,6a,8,8a,9a,9b,10b-dodecahydrotris-(oxireno)[2',3':4b,5;'',3'':6,7;2''',3''':8a,9]phenanthro[1,2-c]furan-8-yl)oxy)methyl Phosphate at pH 9.8 in presence of bovine intestinal mucosal alkaline phosphatase
Reactivation of cyclosarin inhibited human erythrocyte AChE assessed as residual activity at 10 to 1000 uM using acetylthiocholine iodide as substrate preincubated for 2 to 120 mins followed by substrate addition measured for 3 mins by Ellman's method
Reactivation of tabun inhibited human erythrocyte AChE assessed as residual activity at 10 to 1000 uM using acetylthiocholine iodide as substrate preincubated for 2 to 120 mins followed by substrate addition measured for 3 mins by Ellman's method
Drug level treated with Sodium (S)-2-(4-(4-((((3Z,6Z)-6-benzylidene-3-((5-(tertbutyl)-1H-imidazol-4-yl)methylene)-5-oxo-3,4,5,6-tetrahydropyrazin-2-yl)oxy)methoxy)-4-oxobutyl)-1H-1,2,3-triazol-1-yl)pentanedioate assessed as porcine liver carboxylic-ester hydrolase-mediated metabolite formation after 48 hrs by HPLC method
Drug level in rat hepatocytes treated with 25-Chloro-18-methyl-13,14,17,20,22,23-hexahydro-1H,7H-15,19-methano-8,12-(metheno)-4,6,2,14,15,22-benzodioxatetraazacyclopentacosine-3,7,21,28(1H,16H)-tetrone assessed as esterase-mediated compound formation at 4 uM after 40 mins by ultraperformance liquid chromatographic method
Antimalarial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as reduction in parasite growth incubated for 48 hrs followed by addition of [3H]-hypoxanthine and measured after 24 hrs by Topcount liquid scintillation counting method
Antimalarial activity against chloroquine, pyrimethamine, mefloquine and atovaquone- resistant Plasmodium falciparum TM90-C2B infected in human erythrocytes assessed as reduction in parasite growth incubated for 48 hrs followed by addition of [3H]-hypoxanthine and measured after 24 hrs by Topcount liquid scintillation counting method
Synergistic cytotoxicity against doxorubicin-sensitive human NCI/ADR-RES cells assessed as fold change in IC50 at 150 uM incubated for 90 mins in presence of doxorubicin by crystal violet staining assay