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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $132 | In Stock | In Stock | |
| 5 mg | $328 | In Stock | In Stock | |
| 10 mg | $496 | In Stock | In Stock | |
| 25 mg | $795 | In Stock | In Stock | |
| 50 mg | $1,090 | In Stock | In Stock | |
| 100 mg | $1,560 | In Stock | In Stock |
| 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. |
| 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[1]. E7016 inhibits PARP by mimicking NAD+[2]. |
| 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[1]. |
| Synonyms | GPI 21016 |
| Molecular Weight | 349.38 |
| Formula | C20H19N3O3 |
| Cas No. | 902128-92-1 |
| Smiles | OC1CCN(Cc2ccc3oc4cccc5c4c(n[nH]c5=O)c3c2)CC1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 22.5 mg/mL (64.4 mM), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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