Induction of apoptosis in human MDA-MB-231 cells xenografted in BALB/C nude mouse at 4 umol/kg, iv administered starting on day 5 measured after day 22 by tunnel assay relative to control
Invivo prodrug activation in tumor of BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as FAP-alpha mediated (S)-((3S,5R,8R,9S,10S,11S,13R,14S,17R)-11,14-dihydroxy-10,13-dimethyl-12-oxo-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl) 2-amino-3-(1H-indol-3-yl)propanoate formation at 40 umol/L by LC-MS/MS analysis
Ratio of invivo prodrug activation in tumor of BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as FAP-alpha mediated (S)-((3S,5R,8R,9S,10S,11S,13R,14S,17R)-11,14-dihydroxy-10,13-dimethyl-12-oxo-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl) 2-amino-3-(1H-indol-3-yl)propanoate formation in absence of talabostat to FAP-alpha mediated (S)-((3S,5R,8R,9S,10S,11S,13R,14S,17R)-11,14-dihydroxy-10,13-dimethyl-12-oxo-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl) 2-amino-3-(1H-indol-3-yl)propanoate formation in presence of talabostat at 40 umol/L by LC-MS/MS analysis
Prodrug activation in Sprague Dawley rat serum assessed as FAP-alpha mediated (S)-((3S,5R,8R,9S,10S,11S,13R,14S,17R)-11,14-dihydroxy-10,13-dimethyl-12-oxo-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl) 2-amino-3-(1H-indol-3-yl)propanoate formation at 40 umol/L by LC-MS/MS analysis
Prodrug activation in BMSC (unknown origin) assessed as FAP-alpha mediated (S)-((3S,5R,8R,9S,10S,11S,13R,14S,17R)-11,14-dihydroxy-10,13-dimethyl-12-oxo-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl) 2-amino-3-(1H-indol-3-yl)propanoate formation at 40 umol/L by LC-MS/MS analysis
Prodrug activation in 10% fetal bovine serum assessed as FAP-alpha mediated (S)-((3S,5R,8R,9S,10S,11S,13R,14S,17R)-11,14-dihydroxy-10,13-dimethyl-12-oxo-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl) 2-amino-3-(1H-indol-3-yl)propanoate formation at 40 umol/L by LC-MS/MS analysis
Invivo prodrug activation in heart of of BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as FAP-alpha mediated (S)-((3S,5R,8R,9S,10S,11S,13R,14S,17R)-11,14-dihydroxy-10,13-dimethyl-12-oxo-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl) 2-amino-3-(1H-indol-3-yl)propanoate formation at 40 umol/L by LC-MS/MS analysis
Prodrug activation assessed as recombinant human FAP-alpha mediated (S)-((3S,5R,8R,9S,10S,11S,13R,14S,17R)-11,14-dihydroxy-10,13-dimethyl-12-oxo-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl) 2-amino-3-(1H-indol-3-yl)propanoate formation at 40 umol/L after 6 hrs by UPLC-MS/MS analysis
Prodrug activation assessed as recombinant human FAP-alpha mediated (S)-((3S,5R,8R,9S,10S,11S,13R,14S,17R)-11,14-dihydroxy-10,13-dimethyl-12-oxo-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl) 2-amino-3-(1H-indol-3-yl)propanoate formation at 40 umol/L after 6 hrs in presence of FAP-alpha inhibitor talabostat by UPLC-MS/MS analysis
Nephrotoxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells at 12 umol/kg, iv administered starting on day 5 measured after day 22 by hematoxylin-eosin staining-based assay
Toxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as histopathologic change in femur at 12 umol/kg, iv administered starting on day 5 measured after day 22 by hematoxylin-eosin staining-based assay
Hepatotoxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells at 12 umol/kg, iv administered starting on day 5 measured after day 22 by hematoxylin-eosin staining-based assay
Toxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as histopathologic change in spleen at 12 umol/kg, iv administered starting on day 5 measured after day 22 by hematoxylin-eosin staining-based assay
Toxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as histopathologic change in lungh at 12 umol/kg, iv administered starting on day 5 measured after day 22 by hematoxylin-eosin staining-based assay
Toxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as body weight change at 12 umol/kg, iv administered starting on day 5 measured after day 22
Toxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as abnormal behavioral at 12 umol/kg, iv administered starting on day 5 measured after day 22
Toxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as abnormal food intake at 12 umol/kg, iv administered starting on day 5 measured after day 22