(rac)-Talazoparib is a potent inhibitor of PARP1 and PARP2, with Ki values of 1.2 nM and 0.87 nM, respectively. This orally active compound effectively inhibits cellular PARylation, demonstrating an EC50 of 2.51 nM. It induces DNA damage accumulation and significantly suppresses the proliferation of BRCA1/2-mutated cell lines, including MX-1 and Capan-1, with IC50 values of 0.3 nM and 5 nM, respectively. Additionally, (rac)-Talazoparib shows antitumor efficacy in various mouse models, making it a valuable tool for cancer research.
(rac)-Talazoparib is a potent inhibitor of PARP1 and PARP2, with Ki values of 1.2 nM and 0.87 nM, respectively. This orally active compound effectively inhibits cellular PARylation, demonstrating an EC50 of 2.51 nM. It induces DNA damage accumulation and significantly suppresses the proliferation of BRCA1/2-mutated cell lines, including MX-1 and Capan-1, with IC50 values of 0.3 nM and 5 nM, respectively. Additionally, (rac)-Talazoparib shows antitumor efficacy in various mouse models, making it a valuable tool for cancer research.
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