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E7016

Cat. No. M30842
E7016 Structure
Synonym:

GPI 21016

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Biological Activity

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.

Chemical Information
Molecular Weight 349.38
Formula C20H19N3O3
CAS Number 902128-92-1
Form Solid
Solubility (25°C) DMSO 25 mg/mL (ultrasonic and warming and heat to 60°C)
Storage 4°C, protect from light
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Akira Kanai, et al. Clin Case Rep. A case of adult patent ductus arteriosus-associated infective endarteritis who was successfully treated with only antibiotics

[2] Faryal Tahir, et al. Cureus. Anthropometric Measurements and Lifestyle Characteristics of Individuals with Non-alcoholic Fatty Liver Disease

[3] Telmo Raul Aveiro Róbalo, et al. Medwave. [Report of clinical cases in medical school]

[4] W George Lai, et al. Drug Metab Dispos. A Baeyer-Villiger oxidation specifically catalyzed by human flavin-containing monooxygenase 5

[5] Andrea L Russo, et al. Clin Cancer Res. In vitro and in vivo radiosensitization of glioblastoma cells by the poly (ADP-ribose) polymerase inhibitor E7016

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Keywords: E7016, GPI 21016 supplier, PARP, inhibitors, activators

 
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