Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 deletion mutant assessed as reduction in cell viability by MTS assay
Decrease in c-KIT phosphorylation in NOD-SCID mouse xenografted with human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant at 80 mg/kg, po measured after 8 hrs by immunoblotting analysis relative to control
Decrease in c-KIT phosphorylation in NOD-SCID mouse xenografted with human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant at 20 mg/kg, po measured after 8 hrs by immunoblotting analysis relative to control
Antitumor activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant xenografted in NOD-SCID mouse assessed as reduction in tumor size at 25, po administered for 2 weeks with 2 days rest after day 5 and measured thrice per week up to 14 days during compound dosing relative to control
Antitumor activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant xenografted in NOD-SCID mouse assessed as tumor growth inhibition at 25 mg/kg, po administered for 2 weeks with 2 days rest after day 5 and measured thrice per week up to 21 days during compound dosing
Inhibition of human c-KIT JM domain exon 11 V560G single mutant using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay
Inhibition of recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation measured after 150 mins in presence of ATP by ADP-glo based luminescence assay
Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30 mins followed by ATP addition and measured after 30 mins by Kinase Glo based luminescence assay
Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30 mins followed by ATP addition and measured after 120 mins by Kinase Glo based luminescence assay
Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay
Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control
Inhibition of human c-KIT JM domain exon 11 V560G single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control
Inhibition of human c-KIT JM domain exon 11 V560G single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control
Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control
Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay
Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control
Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control
Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay
Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control
Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control