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Cmax in Beagle dog at 5 mg/kg, po by LC-MS/MS analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Cmax in Beagle dog at 1 mg/kg, iv by LC-MS/MS analysis
Cmax in mouse at 10 mg/kg, po by LC-MS/MS analysis
Cmax in mouse at 1 mg/kg, iv by LC-MS/MS analysis
Cmax in Sprague-Dawley rat at 10 mg/kg, po by LC-MS/MS analysis
Cmax in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in ERK phosphorylation at T204 residue measured after 2 hrs by Western blot analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in ERK phosphorylation at T202 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in pS6 phosphorylation at S236 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in pS6 phosphorylation at S235 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in AKT phosphorylation at S473 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in AKT phosphorylation at T308 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in ERK phosphorylation at T204 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in ERK phosphorylation at T202 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in pS6 phosphorylation at S236 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in pS6 phosphorylation at S235 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in AKT phosphorylation at S473 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in AKT phosphorylation at T308 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in ERK phosphorylation at T204 residue measured after 2 hrs by Western blot analysis
Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in ERK phosphorylation at T202 residue measured after 2 hrs by Western blot analysis
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