A-620223 is a PARP-1 inhibitor with a K i of 8 nM against PARP-1 and EC 50 of 3 nM in a whole cell assay. A-620223 demonstrates good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with Temozolomide (TMZ) and in an MX-1 breast xenograph model in combination with Cisplatin. A-620223 can be used for the studies of melanoma and breast cancer [1].
In Vivo, A-620223 (1-25 mg/kg, s.c., successive administration for 7-14 days) demonstrates excellent potentiation of two cytotoxic agents, Temozolomide and Cisplatin, in both a mouse melanoma and a breast cancer model[1].
References:
[1]. Penning TD, et al. Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer. Bioorg Med Chem. 2008 Jul 15;16(14):6965-75.
In Vivo, A-620223 (1-25 mg/kg, s.c., successive administration for 7-14 days) demonstrates excellent potentiation of two cytotoxic agents, Temozolomide and Cisplatin, in both a mouse melanoma and a breast cancer model[1].
References:
[1]. Penning TD, et al. Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer. Bioorg Med Chem. 2008 Jul 15;16(14):6965-75.