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Background Information:
BMN-673 (Talazoparib) (MDV-3800) is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP), potently inhibiting PARP1 and PARP2 enzyme activity with Ki = 1.2 and 0.87 nM, respectively. It inhibits PARP-mediated PARylation in a whole-cell assay with an EC50 of 2.51 nM and prevents proliferation of cancer cells carrying mutant BRCA1/2, with EC50= 0.3 nM (MX-1) and 5 nM (Capan-1), respectively. Displays favorable pharmacokinetic (PK) properties and remarkable antitumor efficacy in the BRCA1 mutant MX-1 breast cancer xenograft model following oral administration as a single-agent or in combination with chemotherapy agents such as temozolomide and cisplatin (ref. 1). It is currently in clinical evaluation.
Reference:
1. B. Wang, et al, J. Med. Chem., 2016, 59 (1), pp 335–357.
APIM050024: BMN-673 (Talazoparib) (MDV-3800)
CAS No.: 1207456-01-6.
Molecular Formula: C19H14F2N6O.
Molecular Weight: 380.4.
Purity: 100% Optically Pure (Chiral HPLC), 99.3%-99.5% chemically Pure by Achiral HPLC at 214 and 254 nm.
QC: Achiral and Chiral HPLCs, NMR and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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