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Talazoparib

CAS No. : 1207456-01-6

MCE 站：Talazoparib

产品活性：Talazoparib (BMN-673) 是一种高效的，具有口服活性的 PARP 1/2 抑制剂。Talazoparib 抑制 PARP1 和 PARP2 酶活性的 K_i 值分别为 1.2 nM 和 0.87 nM。Talazoparib 具有抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：PARP

In Vitro: Talazoparib shows an EC₅₀ of 2.51 nM in cellular PARylation assay.
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).

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.
Talazoparib exhibits moderate oral bioavailability (rat 56%) and C_max (rat 7948 ng/mL) following oral administration (rat 10 mg/kg).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).

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