PROTAC SOS1 degrader-10

PROTAC SOS1 degrader-10 (Compound 11o) inhibits SOS1-mediated KRAS activation in cell-free biochemical assays with an IC₅₀ of 40 nM^[1].
PROTAC SOS1 degrader-10 effectively induces the formation of the SOS1-compound-CRBN ternary complex in cell-free biochemical assays, and among the tested epimers, it generates the strongest signal at lower concentrations^[1].
PROTAC SOS1 degrader-10 (0.9-1000 nM; 1-24 h) induces dose- and time-dependent degradation of SOS1 in KRAS^G12V-mutated SW620 cells via a CRBN- and proteasome-dependent mechanism, with a DC₅₀ of 2.23 nM and a maximum degradation rate of 90.6%^[1].
PROTAC SOS1 degrader-10 (24 h) induces potent SOS1 degradation in KRAS^G12S-mutant A549 cells, with a DC₅₀ of 1.85 nM and a maximum degradation rate of 89.6%^[1].
PROTAC SOS1 degrader-10 (24 h) induces SOS1 degradation in KRAS^G13D-mutant DLD-1 cells, with a DC₅₀ of 7.53 nM and a maximum degradation rate of 80.0%^[1].
PROTAC SOS1 degrader-10 inhibits anchorage-independent 3D proliferation of SW620, A549 and DLD-1 cells harboring KRAS mutations, with IC₅₀ values of 36.7 nM, 52.2 nM and 107 nM, respectively^[1].
PROTAC SOS1 degrader-10 (25-200 nM; 6 h) reduces the level of phosphorylated ERK in KRAS^G12V-mutant SW620 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.