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Subacute toxicity in SPF Kunming mouse assessed as heart morphological changes at 2000 mg/kg, po administered once a day for 14 days by H and E staining based microscopic analysis
Assay data:1 Tested
SummaryPubMed Citation
Subacute toxicity in SPF Kunming mouse assessed as kidney morphological changes at 2000 mg/kg, po administered once a day for 14 days by H and E staining based microscopic analysis
Subacute toxicity in SPF Kunming mouse assessed as liver morphological changes at 2000 mg/kg, po administered once a day for 14 days by H and E staining based microscopic analysis
Subacute toxicity in SPF Kunming mouse assessed as behavioural abnormalities at 2000 mg/kg, po administered once a day for 14 days
In vivo inhibition of PI3K/Akt/mTOR in human A549 cells xenografted in athymic nude mouse assessed as decrease in phosphorylation of 4EBP1 at 25 to 50 mg/kg, ip administered once daily for 21 days by immunocytochemistry
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
In vivo inhibition of eIF4E in human A549 cells xenografted in athymic nude mouse assessed as decrease in phosphorylation of eIF4E at 25 to 50 mg/kg, ip administered once daily for 21 days by immunocytochemistry
Induction of ROS generation in human A549 cells at 1 to 5 uM incubated for 48 hrs by DCFH-DA staining based FACS analysis
Inhibition of PI3K/Akt/mTOR in human A549 cells assessed as increase in eIF4E/4EBP1 interaction incubated for 48 hrs by m7GTP pull down assay
Oral bioavailability in female Sprague-Dawley rat at 10 mg/kg measured up to 24 hrs by LC/MS-MS analysis
MRT in female Sprague-Dawley rat at 10 mg/kg, po measured up to 24 hrs by LC/MS-MS analysis
Half life in female Sprague-Dawley rat at 10 mg/kg, po measured up to 24 hrs by LC/MS-MS analysis
AUC (0 to 24 hrs) in female Sprague-Dawley rat at 10 mg/kg, po measured up to 24 hrs by LC/MS-MS analysis
Oral bioavailability in male Sprague-Dawley rat at 10 mg/kg measured up to 24 hrs by LC/MS-MS analysis
Cmax in female Sprague-Dawley rat at 10 mg/kg, po measured up to 24 hrs by LC/MS-MS analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
MRT in male Sprague-Dawley rat at 10 mg/kg, po measured up to 24 hrs by LC/MS-MS analysis
Half life in male Sprague-Dawley rat at 10 mg/kg, po measured up to 24 hrs by LC/MS-MS analysis
AUC (0 to 24 hrs) in male Sprague-Dawley rat at 10 mg/kg, po measured up to 24 hrs by LC/MS-MS analysis
Cmax in male Sprague-Dawley rat at 10 mg/kg, po measured up to 24 hrs by LC/MS-MS analysis
Volume of distribution in steady state in female Sprague-Dawley rat at 2 mg/kg, iv measured up to 24 hrs by LC/MS-MS analysis
Total plasma clearance in female Sprague-Dawley rat at 2 mg/kg, iv measured up to 24 hrs by LC/MS-MS analysis
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