产品
编 号：F071048
分子式：C19H14F2N6O
分子量：380.35
分子式：C19H14F2N6O
分子量：380.35
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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5mg
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10mg
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50mg
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100mg
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200mg
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结构图
CAS No: 1207456-01-6
产品详情
生物活性：
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.
体内研究：
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 Cmax (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).Animal Model:Female athymic nu/nu mice (8-10 weeks old), with MX-1 xenograft-bearing mice
Dosage:0.33 mg/kg
Administration:Oral gavage, once daily, for 28 days
Result:Significantly inhibited xenograft MX-1 tumor growth.
Animal Model:Sprague-Dawley rats
Dosage:5mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (56%), Cmax (7948 ng/mL), T1/2 (2.25 h).
体外研究：
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).
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.
体内研究：
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 Cmax (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).Animal Model:Female athymic nu/nu mice (8-10 weeks old), with MX-1 xenograft-bearing mice
Dosage:0.33 mg/kg
Administration:Oral gavage, once daily, for 28 days
Result:Significantly inhibited xenograft MX-1 tumor growth.
Animal Model:Sprague-Dawley rats
Dosage:5mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (56%), Cmax (7948 ng/mL), T1/2 (2.25 h).
体外研究：
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).
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