E7016

CAS No. 902128-92-1

E7016( —— )

Catalog No. M35524 CAS No. 902128-92-1

E7016 (GPI 21016) is an orally available PARP inhibitor that inhibits DNA repair and enhances tumor cell radiosensitivity both in vitro and in vivo.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 201 Get Quote
5MG 312 Get Quote
10MG 471 Get Quote
25MG 731 Get Quote
50MG 1003 Get Quote
100MG 1404 Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    E7016
  • Note
    Research use only, not for human use.
  • Brief Description
    E7016 (GPI 21016) is an orally available PARP inhibitor that inhibits DNA repair and enhances tumor cell radiosensitivity both in vitro and in vivo.
  • Description
    E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.
  • In Vitro
    E7016 can enhance tumor cell radiosensitivity through the inhibition of DNA repair.E7016 (3 μM)-mediated radiosensitization occurs through 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+.Apoptosis Analysis Cell Line:The U251 human glioblastoma cell line Concentration:3 μM Incubation Time:6 hours prior to irradiation and were stained at 24 and 72 h postirradiation Result:The number of cells in mitotic catastrophe was significantly greater in the E7016-treated irradiated cells than in cells that received radiation only at 24 hours postirradiation.
  • In Vivo
    E7016 has antitumor efficacy in murine xenograft studies.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 Temozolomide and irradiation in vivo.Animal Model:Four- to six-week-old female nude mice Dosage:40 mg/kg Administration:Oral gavage Result:E7016 enhanced the radiation/Temozolomide (3 mg/kg orally)-induced tumor growth delay of U251 xenografts.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    PARP
  • Recptor
    PARP
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    902128-92-1
  • Formula Weight
    349.38
  • Molecular Formula
    C20H19N3O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 25 mg/mL (71.56 mM; Ultrasonic (<60°C)
  • SMILES
    OC1CCN(Cc2ccc3oc4cccc5c4c(n[nH]c5=O)c3c2)CC1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Andrea L Russo, et al. In vitro and in vivo radiosensitization of glioblastoma cells by the poly (ADP-ribose) polymerase inhibitor E7016. Clin Cancer Res. 2009 Jan 15;15(2):607-12.?
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