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In vivo antitumor activity against human TALL-1 cells xenograft model assessed as tumor growth inhibition treated po qd for 10 days on - 2 days off - 5 days on
Assay data:1 Tested
SummaryPubMed Citation
In vivo antitumor activity against human MDA-MB-157 cells xenograft model assessed as tumor growth inhibition at 30 mg/kg, po qd for 10 days on - 2 days off - 5 days on
In vivo antitumor activity against human MDA-MB-157 cells xenograft model assessed as tumor growth inhibition at 15 mg/kg, po qd for 10 days on - 2 days off - 5 days on
In vivo antitumor activity against human MDA-MB-157 cells xenograft model assessed as tumor growth inhibition at 7.5 mg/kg, po qd for 10 days on - 2 days off - 5 days on
In vivo antitumor activity against human TALL-1 cells xenograft model assessed as tumor growth inhibition at 24 mg/kg, po qd for 10 days on - 2 days off - 5 days on
In vivo antitumor activity against human TALL-1 cells xenograft model assessed as tumor growth inhibition at 6 mg/kg, po qd for 10 days on - 2 days off - 5 days on
Inhibition of Notch4 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of Notch2 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Metabolic stability in mouse liver microsomes assessed as fraction of 0.5 uM parent compound remaining after 10 mins
Assay data:20 Tested
Metabolic stability in human liver microsomes assessed as fraction of 0.5 uM parent compound remaining after 10 mins
Anticancer activity against human TALL-1 cells assessed as cell number by coulter channelyzer
Assay data:11 Active, 11 Activity ≤ 1 µM, 14 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of Notch3 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
Assay data:20 Active, 4 Activity ≤ 1 nM, 19 Activity ≤ 1 µM, 20 Tested
Inhibition of Notch1 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
Assay data:20 Active, 3 Activity ≤ 1 nM, 18 Activity ≤ 1 µM, 20 Tested
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