
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)






Size | Price / USD | Stock | Quantity |
2MG | 201 | Get Quote |
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5MG | 312 | Get Quote |
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10MG | 471 | Get Quote |
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25MG | 731 | Get Quote |
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50MG | 1003 | Get Quote |
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100MG | 1404 | Get Quote |
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500MG | Get Quote | Get Quote |
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Biological Information
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Product NameE7016
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NoteResearch use only, not for human use.
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Brief DescriptionE7016 (GPI 21016) is an orally available PARP inhibitor that inhibits DNA repair and enhances tumor cell radiosensitivity both in vitro and in vivo.
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DescriptionE7016 (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.
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In VitroE7016 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.
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In VivoE7016 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.
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Synonyms——
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PathwayCell Cycle/DNA Damage
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TargetPARP
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RecptorPARP
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Research Area——
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Indication——
Chemical Information
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CAS Number902128-92-1
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Formula Weight349.38
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Molecular FormulaC20H19N3O3
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 25 mg/mL (71.56 mM; Ultrasonic (<60°C)
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SMILESOC1CCN(Cc2ccc3oc4cccc5c4c(n[nH]c5=O)c3c2)CC1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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