PROTAC SOS1 degrader-10

PROTACSOS1 degrader-10 (Compound 11o) is a degrader of son of sevenless 1 (SOS1) that functions through CRBN- and protease-dependent mechanisms. It effectively degrades SOS1 in KRAS-mutated cancer cells SW620, A549, and DLD-1, with DC50 values of 2.23, 1.85, and 7.53 nM, respectively. Additionally, PROTACSOS1 degrader-10 inhibits the proliferation of SW620, A549, and DLD-1 cells, with IC50 values of 36.7, 52.2, and 107 nM, and suppresses ERK phosphorylation.

C(=O)(N1CCC2(CC1)CCC(CN3CCN(C(=O)[C@@H]4CC[C@H](CC4)C5=CC=6C(N(C)C5=O)=NC=NC6N[C@H](C)C7=CC(C(F)(F)F)=CC(N)=C7)CC3)CC2)C8=CC(=C(OC)C=C8)N9C(=O)NC(=O)CC9