YN14

YN14 is a KRASG12C proteolysis targeting chimera (PROTAC) . YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG) . YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.

C62H75F2N11O7S

1156.39

O=C(C=C)N1C[C@H](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=NC(C5=C(OCC6CCN(CCCC(N[C@@H](C(C)(C)C)C(N7[C@H](C(NCC8=CC=C(C9=C(C)N=CS9)C=C8)=O)C[C@@H](O)C7)=O)=O)CC6)C=CC=C5F)=C(F)C=C42)=O)CC1

PROTACs; Ras

99.08

10 mM in DMSO

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature