iRucaparib-AP6
Based on 2 publication(s) in Google Scholar
iRucaparib-AP6 is a highly efficient and specific PROTAC PARP1 degrader. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1.
(Pink: PARP-1 ligand (HY-10617A); Blue: Cereblon ligand (HY-10984); Black: linker).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.03%
- CAS 番号: 2410557-00-3
- 分子式: C46H55FN6O11
- 分子量:886.96
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 iRucaparib-AP6
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生物活性
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PARP1 82 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAPAN-1 | IC50 |
0.95 μM
Compound: 3; iRucaparib-AP6
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Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay
Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay
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[PMID: 32924477] |
| MDA-MB-436 | IC50 |
0.71 μM
Compound: 3; iRucaparib-AP6
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Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay
Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay
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[PMID: 32924477] |
iRucaparib-AP6 (0-10 μM; 24 hours) decreases PARP-1 level in a dose dependent manner, exhibits a half-maximal degrading concentration (DC50) of 82 nM (Dmax is 92%)[1]. iRucaparib-AP6 (0-20 μM; 24 hours) induces degradation of PARP1 at low concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary rat neonatal cardiomyocyte cells
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Concentration:0.001 μM; 0.01 μM; 0.1 μM; 1 μM; 10 μM
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Incubation Time:24 hours
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Result:Decreased PARP-1 level in primary rat neonatal cardiomyocyte cells.
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Cell Line:Primary rat neonatal cardiomyocyte cells
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Concentration:0.05 μM; 0.1 μM; 0.2 μM; 0.5 μM; 1 μM; 2 μM; 5 μM;10 μM; 20 μM
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Incubation Time:24 hours
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Result:Induced robust PARP1 degradation at concentrations as low as 50 nM.
化学情報
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CAS 番号 2410557-00-3
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性状 Solid
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分子量 886.96
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分子式 C46H55FN6O11
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Color Light yellow to yellow
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SMILES
O=C(NCC1)C2=CC(F)=CC3=C2C1=C(C4=CC=C(C=C4)CN(CCOCCOCCOCCOCCOCCOCCNC5=CC=CC(C(N6C7CCC(NC7=O)=O)=O)=C5C6=O)C)N3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Med Chem
Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers. [Abstract]2020 Oct 8;63(19):11012-11033. PMID: 32924477 -
bioRxiv
2024 Dec 21:2024.12.19.629292. PMID: 39763743
溶剤 & 溶解度
DMSO : 50 mg/mL (56.37 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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 2.5 mg/mL (2.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (stored under nitrogen)
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.
純度とドキュメンテーション
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データシート (271 KB)
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SDS (252 KB)
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- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 (stored under nitrogen). 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 | 1.1274 mL | 5.6372 mL | 11.2745 mL | 28.1862 mL |
| 5 mM | 0.2255 mL | 1.1274 mL | 2.2549 mL | 5.6372 mL | |
| 10 mM | 0.1127 mL | 0.5637 mL | 1.1274 mL | 2.8186 mL | |
| 15 mM | 0.0752 mL | 0.3758 mL | 0.7516 mL | 1.8791 mL | |
| 20 mM | 0.0564 mL | 0.2819 mL | 0.5637 mL | 1.4093 mL | |
| 25 mM | 0.0451 mL | 0.2255 mL | 0.4510 mL | 1.1274 mL | |
| 30 mM | 0.0376 mL | 0.1879 mL | 0.3758 mL | 0.9395 mL | |
| 40 mM | 0.0282 mL | 0.1409 mL | 0.2819 mL | 0.7047 mL | |
| 50 mM | 0.0225 mL | 0.1127 mL | 0.2255 mL | 0.5637 mL |
iRucaparib-AP6 関連分類
HY-130644 関連分類
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