Talazoparib tosylate

SKU: orb1706585

Description

Talazoparib tosylate (BMN 673ts) is a potent, orally bioavailable small molecule inhibitor of PARP1 and PARP2. It is widely used in preclinical research, including in vitro cell-based assays and in vivo xenograft models, to investigate targeted therapies for BRCA-mutated breast and ovarian cancers.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1373431-65-2
• MW: 552.55
• Purity: 99.79%
• Formula: C₂₆H₂₂F₂N₆O₄S
• SMILES: S(=O)(=O)(O)C1=CC=C(C)C=C1.CN1C([C@H]2C=3C4=C(N[C@@H]2C5=CC=C(F)C=C5)C=C(F)C=C4C(=O)NN3)=NC=N1
• Target: PARP
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.24 mM);DMSO:100 mg/mL (180.98 mM);H2O:< 0.1 mg/mL (insoluble)

Bioactivity

• Target IC50:
  PARP2:0.85 nM (Ki)|PARP1:1.20 nM (Ki)
• In Vivo:
  Talazoparib tosylate has high oral bioavailability, with absolute bioavailability exceeding 40% when administered orally in rats using carboxymethylcellulose as the vehicle. Talazoparib tosylate has significant antitumor effects when administered orally; Talazoparib tosylate exhibits high potency sensitivity in transplanted tumors with impaired DNA repair due to BRCA mutations or PTEN defects when administered at well-tolerated doses in mice.
• In Vitro:
  Talazoparib tosylate had similar inhibitory effects on PARP1 and PARP2 (Ki values of 1.20 nM and 0.85 nM, respectively). Talazoparib tosylate induced the formation of an intranuclear γ-H2AX focus at concentrations as low as 100 pM. Talazoparib tosylate had no effect on PARG activity at concentrations up to 1 μM. The dissociation constant for binding of Talazoparib tosylate to PARP1 was 0.29 nM. Talazoparib tosylate selectively targets tumor cells with defects in the BRCA1, BRCA2 or PTEN genes with 20- to 200-fold greater potency than existing PARP1/2 inhibitors. Talazoparib tosylate specifically targets tumor cells with defects in homologous recombination genes, and tumor models with defects in BRCA1 or BRCA2 defective tumor models are extremely sensitive to Talazoparib tosylate.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PARP2, PARP1, BMN 673ts, BMN673ts

Compound Identifiers

PubChem CID

135565654