Venadaparib

SKU: orb1298099

Description

Venadaparib (IDX-1197) is a highly potent and selective oral PARP1/2 inhibitor, demonstrating IC50 values of 1.4 nM and 1.0 nM, respectively. It exhibits no activity against PARP-5. By blocking the repair of DNA single-strand breaks, this inhibitor is a valuable tool for investigating synthetic lethality in various solid tumor models, both in vitro and in vivo.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1681017-83-3
• MW: 406.45
• Purity: 99.86% (May vary between batches)
• Formula: C₂₃H₂₃FN₄O₂
• SMILES: Fc1ccc(Cc2n[nH]c(=O)c3ccccc23)cc1C(=O)N1CC(CNC2CC2)C1
• Target: PARP
• Solubility: DMSO:90 mg/mL (221.43 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (12.3 mM)

Bioactivity

• Target IC50:
  PARP1:0.5 nM(EC50)|PARP1/PARP2:1.4 nM/1.0 nM
• In Vivo:
  Oral administration of Venadaparib significantly inhibits PAR(>90%) in tumor tissues until 24 hr post-dose in the germline BRCA1-mutated ovarian cancer PDX model. Venadaparib also dose-dependently inhibits potent tumor growth compared to the Olaparib treatment group.
• In Vitro:
  Venadaparib significantly inhibits PARP1-mediated PAR expression with an EC50 of 0.5 nM In DNA damage-induced Hela cells.

Storage & Handling

• Storage: 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

poly ADP ribose polymerase, solid, Venadaparib, tumors, Inhibitor, IDX 1197, IDX1197, IDX-1197, PARP, PARP2, PARP1, NOV 140101, NOV140101, NOV-140101, inhibit, anticancer

Compound Identifiers

PubChem CID

117955898