Talazoparib (BMN 673) is a novel and orally active poly(ADP-ribose) polymerase (PARP) 1 and 2 inhibitor. Talazoparib (BMN 673) inhibits PARP1 and PARP2 enzyme activity with Ki = 1.2 and 0.87 nM, respectively. In a cell-based assay, Talazoparib (BMN 673) inhibits PARP-mediated PARylation with an EC50 of 2.51 nM. It also inhibits the proliferation of cancer cells carrying mutant BRCA1/2, such as MX-1 (EC50 = 0.3 nM) and Capan-1 (EC50 = 5 nM). [1] Talazoparib (BMN 673) demonstrates remarkable antitumor efficacy in a BRCA1 mutant MX-1 breast cancer xenograft model. [1]
Talazoparib (BMN 673) is currently being studied in a Phase III clinical trial in breast cancer patients with BRCA mutation. [2]
Technical information:
| Chemical Formula: | C19H14F2N6O | |
| CAS #: | 1207456-01-6 | |
| Molecular Weight: | 380.35 | |
| Purity: | > 98% | |
| Appearance: | Off-white | |
| Chemical Name: | 3H-Pyrido[4,3,2-de]phthalazin-3-one, 5-fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-, (8S,9R)- | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | BMN 673, BMN673?Talazoparib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
| 1. | Wang B, et al. Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent. J Med Chem. 2016. 59(1):335-57 Pubmed ID: 26652717 |
| 2. | A Study Evaluating Talazoparib (BMN 673), a PARP Inhibitor, in Advanced and/or Metastatic Breast Cancer Patients With BRCA Mutation (EMBRACA Study) (EMBRACA) clinicaltrials.gov/NCT01945775 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
