Table 2.

Selective killing of tumor cells with BRCA1, BRCA2, or PTEN mutations

SF50, ╬╝mol/L
MX-1 (BRCA1 deficient)SUM149 (BRCA1 deficient)Capan-1 (BRCA2 deficient)MB-468 (PTEN deficient)LNCap (PTEN deficient)PC-3 (PTEN deficient)SW620MDA-MB-231MRC-5 (normal)
VeliparibND0.818>10NDNDNDNDND>10
Rucaparib0.00530.00790.6090.2200.7370.293ND5.538.53
Olaparib0.02320.01980.2590.3680.5890.787ND6.415.83
BMN 6730.00038.57E-60.0050.0060.0030.0040.131.850.31

NOTE: Cultured human tumor cell lines were treated with veliparib, rucaparib, olaparib, or BMN 673, and tumor-killing effects were assessed either by colony formation assays (SUM149) or by two-dimensional cytotoxicity assays (all other cell lines). Survival curves were plotted and the IC50 was calculated as the concentration required to kill 50% of the cells. Known deficiency of homologous recombination DNA repair genes is indicated in parenthesis. Cells with BRCA1/BRCA2 mutations or PTEN deficiency were more sensitive to all PARP inhibitors than cells lacking these mutations.

Abbreviation: ND, not determined.