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Talazoparib (BMN 673)
| Product Name | Talazoparib (BMN 673) |
| Price: | Inquiry |
| Catalog No.: | CN00474 |
| CAS No.: | 1207456-01-6 |
| Molecular Formula: | C19H14F2N6O |
| Molecular Weight: | 380.35 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | Fc1ccc(cc1)[C@H]1Nc2cc(F)cc3c2c([C@@H]1c1ncnn1C)n[nH]c3=O |
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| Description | Talazoparib (BMN-673) is a highly potent PARP1/2 inhibitor with Kis of 1.2 nM and 0.87 nM, respectively. |
| Target | PARP2:0.87 nM (Ki) PARP1:1.2 nM (Ki) |
| In Vitro | Talazoparib (BMN 673) demonstrates excellent potency, inhibiting PARP1 and PARP2 enzyme activity with Ki=1.2 and 0.87 nM, respectively[1]. Talazoparib (BMN 673) exhibits selective antitumor cytotoxicity and elicits DNA repair biomarkers at much lower concentrations than earlier generation PARP1/2 inhibitors (such as Olaparib, Rucaparib, and Veliparib)[2]. |
| In Vivo | Talazoparib (BMN 673; 1 mg/kg, p.o.) is orally available, displaying 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[1]. Talazoparib (BMN 673) is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxylmethyl cellulose. Oral administration of Talazoparib elicits remarkable antitumor activity, xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency are profoundly sensitive to oral Talazoparib treatment at well-tolerated doses in mice[2]. |
| Cell Assay | In single-agent assays, Capan-1 cells (BRCA2-deficient), MX-1 (BRCA1-deficient) cells, or other cultured cells are seeded at densities that allow linear growth for 10-12 days in 96-well plates (typically 500-3000 cells/well). Cells are treated in their recommended growth media containing varying concentrations of PARP inhibitors (Veliparib, Rucaparib, Niraparib, Olaparib, and Talazoparib) for 10-12 consecutive days (media are changed with fresh compounds every 5 days). IC50 values are calculated using GraphPad Prism5[1]. |
| Animal Admin | Mice[1] MX-1 tumor xenografts are prepared. When tumors reach an average volume of approximately 150 mm3, Olaparib (100 mg/kg), Talazoparib (1 mg/kg), or vehicle is administered in a single po dose. Tumors are harvested at 2, 8, and 24 h after drug dosing and snap-frozen in liquid nitrogen. Tumor tissue is then homogenized in PBS on ice and extracted with lysis buffer (25 mM Tris, pH 8.0, 150 mM NaCl, 5 mM EDTA, 2 mM EGTA, 25 mM NaF, 2 mM Na3VO4, 1 mM Pefabloc, 1% Triton X-100, and protease inhibitor cocktail) containing 1% SDS. Levels of PAR in the tumor lysates are determined by ELISA using PARP in vivo PD assay II kit. |
| Density | 1.6±0.1 g/cm3 |
| Exact Mass | 380.119720 |
| PSA | 88.75000 |
| LogP | 1.91 |