bmn673

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1 2 (Kis: 1.2 0.85 nM).

(8R,9S)-Talazoparib is Talazoparib enantiomer , less active than Talazoparib on the inhibition of PARP1 (IC50: 144 nM).

PARP1 2-IN-3 (Compound 29) is an orally effective inhibitor of PARP1 and PARP2, exhibiting IC50 values of 0.2235 nM and <0.001 nM, respectively. It inhibits the proliferation of Capan-1 wild-type, AZD2281-resistant, and BMN673-resistant cells, with IC50 values ranging from 1.82 to 9.98 nM. Furthermore, PARP1 2-IN-3 demonstrates anti-tumor activity in mice.