E7016

SKU: orb1688849

Description

E7016 (GPI 21016) is an orally bioavailable PARP inhibitor that disrupts DNA repair mechanisms. This action has been shown to potentiate the effects of radiation therapy, enhancing tumor radiosensitivity in both cellular and animal model studies, supporting its investigation in oncology research.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 902128-92-1
• MW: 349.38
• Purity: 98.16% (May vary between batches)
• Formula: C₂₀H₁₉N₃O₃
• SMILES: OC1CCN(Cc2ccc3oc4cccc5c4c(n[nH]c5=O)c3c2)CC1
• Target: PARP
• Solubility: DMSO:22.5 mg/mL (64.4 mM)

Bioactivity

• In Vivo:
  Administration of E7016 (40 mg/kg; oral gavage) to mice bearing U251 xenografts enhances the effectiveness of the Temozolomide/radiation combination. Mice treated with E7016/irradiation/Temozolomide have an additional growth delay of six days compared with the combination of irradiation/Temozolomide in vivo.
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• In Vitro:
  E7016 (3 μM) enhances radiosensitization by an increase in the number of cells undergoing mitotic catastrophe and not an increase in the number of cells undergoing apoptosis. E7016 inhibits PARP by mimicking NAD+.
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Storage & Handling

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

Alternative Names

E7016, E-7016, E 7016, PARP, GPI21016, GPI-21016, GPI 21016

Compound Identifiers

PubChem CID

11660296