Venadaparib
Based on 1 publication(s) in Google Scholar
Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.52%
- CAS. Nr.: 1681017-83-3
- Formel: C23H23FN4O2
- Molecular Weight:406.45
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Venadaparib
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PARP1 1.4 nM (IC50) |
PARP2 1 nM (IC50) |
In Vitro
In DNA damage-induced Hela cells, Venadaparib (IDX-1197) significantly inhibits PARP1-mediated PAR expression (EC50 of 0.5 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1681017-83-3
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Appearance Solid
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Molecular Weight 406.45
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Formel C23H23FN4O2
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Color White to yellow
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SMILES
O=C1NN=C(CC2=CC=C(F)C(C(N3CC(CNC4CC4)C3)=O)=C2)C5=C1C=CC=C5
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Synonyms
IDX-1197
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (246.03 mM; Need ultrasonic; 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (12.30 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (12.30 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
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. 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 | 2.4603 mL | 12.3016 mL | 24.6033 mL | 61.5082 mL |
| 5 mM | 0.4921 mL | 2.4603 mL | 4.9207 mL | 12.3016 mL | |
| 10 mM | 0.2460 mL | 1.2302 mL | 2.4603 mL | 6.1508 mL | |
| 15 mM | 0.1640 mL | 0.8201 mL | 1.6402 mL | 4.1005 mL | |
| 20 mM | 0.1230 mL | 0.6151 mL | 1.2302 mL | 3.0754 mL | |
| 25 mM | 0.0984 mL | 0.4921 mL | 0.9841 mL | 2.4603 mL | |
| 30 mM | 0.0820 mL | 0.4101 mL | 0.8201 mL | 2.0503 mL | |
| 40 mM | 0.0615 mL | 0.3075 mL | 0.6151 mL | 1.5377 mL | |
| 50 mM | 0.0492 mL | 0.2460 mL | 0.4921 mL | 1.2302 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4101 mL | 1.0251 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3075 mL | 0.7689 mL | |
| 100 mM | 0.0246 mL | 0.1230 mL | 0.2460 mL | 0.6151 mL |
Venadaparib Related Classifications
HY-137457 Related Classifications
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