Network Version
Talazoparib Data Sheet
| Product Name: | Talazoparib |
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| CAS No.: | 1207456-01-6 | |
| Cat. No.: | HY-16106 | |
| MWt: | 380.35 | |
| Formula: | C19H14F2N6O | |
| Purity : | >98% | |
| Solubility: | DMSO : 25 mg/mL (65.73 mM; Need ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity[1].
IC50 & Target:IC50: 0.57 nM (PARP1)[1]
Ki: 1.2/0.87 nM (PARP1/2)[1] In Vitro: Talazoparib shows an EC50 of 2.51 nM in cellular PARylation assay[1]. Talazoparib shows EC50s of 0.3 nM, 5 nM and 0.31 for MX-1 cells (BRCA1 mutant), Capan-1 cells (BRCA2 mutant) and MRC-5 cells (normal)[1]. In Vivo: Talazoparib (0.33 mg/kg; i.g.; once daily; for 28 days) exhibits antitumor activity against BRCA1 mutant breast cancer model in mice[1]. Talazoparib exhibits moderate oral bioavailability (rat 56%) and Cmax (rat 7948 ng/mL) following oral administration (rat 10 mg/kg)[1]. Talazoparib exhibits the terminal elimination half-life (rat 2.25 h) due to plasma clearance (2 mL/min/kg) following intravenous administration (rat 5 mg/kg)[1]. |
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