Talazoparib

SKU: orb1226795

Description

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).

Key Properties

• CAS Number: 1207456-01-6
• MW: 380.35
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₄F₂N₆O
• SMILES: CN1C(=NC=N1)[C@@H]2[C@H](N=C3C=C(C=C4C3=C2NNC4=O)F)C5=CC=C(C=C5)F
• Target: PARP
• Solubility: DMSO:38 mg/mL warmed (99.9 mM); Ethanol:<1 mg/mL (<1 mM); Water：<1 mg/mL (<1 mM)

Bioactivity

• 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). 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: 5 mg/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).
• 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMN 673

Quick Database Links

Gene Symbol

PARP