Mefuparib (CVL-218) HCl is a novel and potent PARP1/2 inhibitor (IC50 = 3.2/1.9 nM) with anticancer activity. It displays >406-fold over other PARP isoforms such as PARP3, TNKS1, TNKS2 and PARP6; It reduces poly(ADP-ribose) formation, enhances γH2AX levels, induces G2/M arrest and subsequent apoptosis in homologous recombination repair (HR)-deficient cells. Mefuparib shows potent in vitro and in vivo proliferation and growth inhibition against HR-deficient cancer cells and synergistic sensitization of HR-proficient xenografts to the anticancer drug temozolomide.
纯度:≥98%
CAS:1449746-00-2