| Chemical Properties | Back Directory | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 25 mg/mL (71.56 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [pka]
11.01±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [in vivo]
E7016 has antitumor efficacy in murine xenograft studies[1].
Administration of E7016 (40 mg/kg; oral gavage) to mice bearing U251 xenografts enhances the effectiveness of the Temozolomide/radiation combination[1].
Mice treated with E7016/irradiation/Temozolomide have an additional growth delay of six days compared with the combination of Temozolomide and irradiation in vivo[1]. | Animal Model: | Four- to six-week-old female nude mice[3] | | Dosage: | 40 mg/kg | | Administration: | Oral gavage | | Result: | E7016 enhanced the radiation/Temozolomide (3 mg/kg orally)-induced tumor growth delay of U251 xenografts. |
| [IC 50]
PARP | [References]
[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. DOI:10.1158/1078-0432.CCR-08-2079
[2] W George Lai, et al. A Baeyer-Villiger oxidation specifically catalyzed by human flavin-containing monooxygenase 5. Drug Metab Dispos. 2011 Jan;39(1):61-70. DOI:10.1124/dmd.110.035360 |
|
|