E7016
Based on 1 Customer Validation
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.11%
- No. CAS: 902128-92-1
- Fòrmula: C20H19N3O3
- Peso molecular:349.38
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
PARP |
In Vitro
E7016 can enhance tumor cell radiosensitivity through the inhibition of DNA repair[1].
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[1].
E7016 inhibits PARP by mimicking NAD+[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:The U251 human glioblastoma cell line
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Concentration:3 μM
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Incubation Time:6 hours prior to irradiation and were stained at 24 and 72 h postirradiation
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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
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four- to six-week-old female nude mice[3]
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Dosage:40 mg/kg
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Administration:Oral gavage
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Result:E7016 enhanced the radiation/Temozolomide (3 mg/kg orally)-induced tumor growth delay of U251 xenografts.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 902128-92-1
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Appearance Solid
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Peso molecular 349.38
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Fòrmula C20H19N3O3
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Color White to off-white
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SMILES
O=C1NN=C2C3=C1C=CC=C3OC4=CC=C(CN5CCC(O)CC5)C=C42
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Synonyms
GPI 21016
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (71.56 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.58 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8622 mL | 14.3111 mL | 28.6221 mL | 71.5553 mL |
| 5 mM | 0.5724 mL | 2.8622 mL | 5.7244 mL | 14.3111 mL | |
| 10 mM | 0.2862 mL | 1.4311 mL | 2.8622 mL | 7.1555 mL | |
| 15 mM | 0.1908 mL | 0.9541 mL | 1.9081 mL | 4.7704 mL | |
| 20 mM | 0.1431 mL | 0.7156 mL | 1.4311 mL | 3.5778 mL | |
| 25 mM | 0.1145 mL | 0.5724 mL | 1.1449 mL | 2.8622 mL | |
| 30 mM | 0.0954 mL | 0.4770 mL | 0.9541 mL | 2.3852 mL | |
| 40 mM | 0.0716 mL | 0.3578 mL | 0.7156 mL | 1.7889 mL | |
| 50 mM | 0.0572 mL | 0.2862 mL | 0.5724 mL | 1.4311 mL | |
| 60 mM | 0.0477 mL | 0.2385 mL | 0.4770 mL | 1.1926 mL |
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