Talazoparib

Research use only, not for human use.

Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM.

Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.(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 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).

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 (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 miceDosage: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).

BMN 673

Cell Cycle/DNA Damage

PARP

PARP

Cancer

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1207456-01-6

380.35

C19H14F2N6O

>98% (HPLC)

DMSO:38 mg/mL warmed (99.9 mM); Ethanol:<1 mg/mL (<1 mM); Water：<1 mg/mL (<1 mM)

CN1C(=NC=N1)[C@@H]2[C@H](N=C3C=C(C=C4C3=C2NNC4=O)F)C5=CC=C(C=C5)F

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(-20℃)

With Ice Pack

≥ 2 years