YN14-H

YN14-H is a PROTAC degrader targeting KRASG12C. YN14-H inhibits cell growth in NCI-H358 and MIA PaCa-2 cells (IC50 values of 0.042, 0.021 μM, DC50 values of 28.9, 18.1 nM, respectively). YN14-H significantly induces apoptosis and inhibits migration. YN14-H demonstrates favorable pharmacokinetic properties and excellent antitumor activity in vivo. (Structure Note: Pink: target protein ligand ; Blue: E3 ligase ligand (HY-125905) ; Black: linker (HY-Y0840) ; E3 ligase ligand + linker (HY-173253).

C65H78F3N11O8S

1230.44

O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3OCCCN5CCC(COC6=CC=CC(F)=C6C7=C(F)C=C(C(N8[C@@H](C)CN(C(C=C)=O)CC8)=N9)C(N(C%10=C(C)C=CN=C%10C(C)C)C9=O)=N7)CC5

Apoptosis; PROTACs; Ras

Room temperature