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Coupled Nucleotide Exchange Assay from US Patent US20240059703: "HETEROCYCLIC SPIRO COMPOUNDS AND METHODS OF USE"
Assay data:506 Active, 473 Activity ≤ 1 µM, 513 Tested
SummaryRelated BioAssays by Target
KRAS::SOS1 AlphaScreen Binding Assay from US Patent US20240051956: "SOS1 INHIBITORS AND USES THEREOF"
Assay data:85 Active, 87 Activity ≤ 1 µM, 87 Tested
Inhibition of SOS1 (unknown origin)
Assay data:7 Active, 7 Activity ≤ 1 µM, 7 Tested
Inhibition of SOS1 (unknown origin) at 500 nM
Assay data:19 Tested
Invivo induction of SOS1 degradation in human SW620 cells harboring KRAS G12V mutant xenografted BALB/c nude mouse assessed as decrease in SOS1 level in tumor at 50 mg/kg, ip administered twice daily for 2 weeks by immunohistochemistry analysis
Assay data:1 Tested
Invivo induction of SOS1 degradation in human SW620 cells harboring KRAS G12V mutant xenografted BALB/c nude mouse assessed as decrease in SOS1 level at 50 mg/kg, ip administered twice daily for 2 weeks by Immunoblot analysis
Invivo PROTAC activity at VHL/SOS1 in human SW620 cells harboring KRAS G12V mutant xenografted BALB/c nude mouse assessed as decrease in phosphorylated ERK expression in tumor at 10 to 20 mg/kg, ip administered once daily for 2 weeks by immunohistochemistry analysis
Assay data:1 Active, 1 Tested
Invivo PROTAC activity at VHL/SOS1 in human SW620 cells harboring KRAS G12V mutant xenografted BALB/c nude mouse assessed as induction of SOS1 degradation in tumor at 10 to 20 mg/kg, ip administered once daily for 2 weeks by immunohistochemistry analysis
Invivo PROTAC activity at VHL/SOS1 in human SW620 cells harboring KRAS G12V mutant xenografted BALB/c nude mouse assessed as decrease in phosphorylated ERK expression at 10 to 20 mg/kg, ip administered once daily for 2 weeks by Immunoblot analysis
Invivo PROTAC activity at VHL/SOS1 in human SW620 cells harboring KRAS G12V mutant xenografted BALB/c nude mouse assessed as induction of SOS1 degradation at 10 to 20 mg/kg, ip administered once daily for 2 weeks by Immunoblot analysis
Invivo induction of SOS1 degradation in human ASPC1 cells harboring KRAS G12D mutant xenografted BALB/c nude mouse assessed as decrease in SOS1 level in tumor at 50 mg/kg, ip administered twice daily for 3 weeks by immunohistochemical analysis
Invivo induction of SOS1 degradation in human ASPC1 cells harboring KRAS G12D mutant xenografted BALB/c nude mouse assessed as decrease in SOS1 level at 50 mg/kg, ip administered twice daily for 3 weeks by Immunoblot analysis
Invivo PROTAC activity at VHL/SOS1 in human ASPC1 cells harboring KRAS G12D mutant xenografted BALB/c nude mouse assessed as decrease in phosphorylated ERK expression at 10 to 20 mg/kg, ip administered once daily for 3 weeks by immunohistochemistry analysis
Invivo PROTAC activity at VHL/SOS1 in human ASPC1 cells harboring KRAS G12D mutant xenografted BALB/c nude mouse assessed as induction of SOS1 degradation administered intraperitoneally once daily for 3 weeks by immunohistochemistry analysis
Invivo PROTAC activity at VHL/SOS1 in human ASPC1 cells harboring KRAS G12D mutant xenografted BALB/c nude mouse assessed as decrease in phosphorylated ERK expression at 10 to 20 mg/kg, ip administered once daily for 3 weeks by Immunoblot analysis
Invivo PROTAC activity at VHL/SOS1 in human ASPC1 cells harboring KRAS G12D mutant xenografted BALB/c nude mouse assessed as induction of SOS1 degradation administered intraperitoneally once daily for 3 weeks by Immunoblot analysis
Induction of SOS1 degradation in human ASPC1 cells at 1 uM incubated for 6 hrs by quantitative proteomics analysis
PROTAC activity at VHL/SOS1 in human SW620 cells harboring KRAS G12V mutant assessed as induction of SOS1 degradation at 1 uM incubated for 8 hrs by Immunoblot analysis
PROTAC activity at VHL/SOS1 in human HCT-116 cells harboring KRAS G13D mutant assessed as induction of SOS1 degradation at 1 uM incubated for 2 to 4 hrs by Immunoblot analysis
PROTAC activity at VHL/SOS1 in human A549 cells harboring KRAS G12S mutant assessed as induction of SOS1 degradation at 1 uM incubated for 2 to 4 hrs by Immunoblot analysis
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