Biological activity ABT-888
Oct 11,2019
Biological activity
Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.
In vitro
Veliparib (ABT-888) is a potential anti-cancer drug acting as a PARP inhibitor,which inhibits PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays,respectively.ABT-888 reduces clonogenic survival and inhibits DNA repair in H460 cells. ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells.
In vivo
ABT-888 inhibits PARP in B16F10 and 9L xenograft models, thus enhancing the anticancer activity of temozolomide. The Combined with other cytotoxic agents, ABT-888 shows strong antitumor effect in MX-1 xenograft model. ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg according to the the size of tumors in A375 and Colo829 xenograft models.
Features
ABT-888 enhances the effectiveness of common cancer treatments, such as radiation therapy and alkylating agents.
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Oct 11,2019InhibitorsABT-888
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