CW-2

CW-2 is a PARP1 PROTAC degrader. CW-2 has potent antiproliferative effects against MDA-MB-231 cells (IC50 = 0.72 μM) and CDDP-resistant cells (A549/CDDP: IC50 = 3.52 μM). CW-2 has synergistic antitumor activity and enhanced membrane permeability. CW-2 exerts antitumor effects by inducing DNA damage, impairing DNA repair, and activating mitochondria-dependent apoptosis (Pink: PARP1 ligand ; Blue: E3 CRBN ligand (HY-173439) ; Black: linker (HY-173440) ).

C43H42Cl2FN11O10Pt

1157.85

O=C1NN=C(C2=CC=CC=C21)CC3=CC(F)=C(C=C3)C(NCC(NC(CC4=CC=C(C=C4)OCC5=CN(N=N5)C6=C(C7=CC=C6)CN(C7=O)C8CCC(NC8=O)=O)C(O[Pt]([NH3])(Cl)(Cl)(O)[NH3])=O)=O)=O

DNA/RNA Synthesis; PARP; PROTACs

Room temperature