iVeliparib-AP6
Based on 1 Customer Validation
iVeliparib-AP6 is a proteolysis-targeting chimera (PROTAC) molecule designed based on Veliparib (HY-10129), which targets PARP1/2. The DC50s of iVeliparib-AP6 for inducing the degradation of PARP1 and PARP2 are 36 nM and 63 nM, respectively, and its IC50s are 69 nM and 21 nM, respectively. iVeliparib-AP6 contains a Veliparib-based PARP inhibitor warhead linked to a CRBN E3 ligase binder; it uses Thalidomide (HY-14658) as a ligand to recruit CRBN E3 ubiquitin ligase and exerts the PARP2 degradation mechanism.
(Pink: PARP-2 and PARP-1 ligand (HY-10129); Blue: Cereblon ligand (HY-41547); Black: linker (HY-120918)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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 : 99.84%
- CAS 番号: 2472645-27-3
- 分子式: C40H53N7O11
- 分子量:807.89
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保管条件: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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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
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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PARP1 69 nM (IC50) |
PARP2 21 nM (IC50) |
PARP1 36 nM (ED50) |
PARP2 63 nM (ED50) |
Cereblon |
体外実験
化学情報
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CAS 番号 2472645-27-3
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性状 Solid
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分子量 807.89
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分子式 C40H53N7O11
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Color Light yellow to yellow
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SMILES
O=C1C2=C(NCCOCCOCCOCCOCCOCCOCCN3[C@](CCC3)(C4=NC5=CC=CC(C(N)=O)=C5N4)C)C=CC=C2C(N1C6C(NC(CC6)=O)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (123.78 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (273 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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取扱説明書 (2659 KB)
参考文献
[1]. Wang S, et al. Uncoupling of PARP1 trapping and inhibition using selective PARP1 degradation. Nat Chem Biol. 2019;15(12):1223-1231. [Content Brief]
[2]. Cao C, et al. Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers. J Med Chem. 2020;63(19):11012-11033. [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. 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 | 1.2378 mL | 6.1890 mL | 12.3779 mL | 30.9448 mL |
| 5 mM | 0.2476 mL | 1.2378 mL | 2.4756 mL | 6.1890 mL | |
| 10 mM | 0.1238 mL | 0.6189 mL | 1.2378 mL | 3.0945 mL | |
| 15 mM | 0.0825 mL | 0.4126 mL | 0.8252 mL | 2.0630 mL | |
| 20 mM | 0.0619 mL | 0.3094 mL | 0.6189 mL | 1.5472 mL | |
| 25 mM | 0.0495 mL | 0.2476 mL | 0.4951 mL | 1.2378 mL | |
| 30 mM | 0.0413 mL | 0.2063 mL | 0.4126 mL | 1.0315 mL | |
| 40 mM | 0.0309 mL | 0.1547 mL | 0.3094 mL | 0.7736 mL | |
| 50 mM | 0.0248 mL | 0.1238 mL | 0.2476 mL | 0.6189 mL | |
| 60 mM | 0.0206 mL | 0.1031 mL | 0.2063 mL | 0.5157 mL | |
| 80 mM | 0.0155 mL | 0.0774 mL | 0.1547 mL | 0.3868 mL | |
| 100 mM | 0.0124 mL | 0.0619 mL | 0.1238 mL | 0.3094 mL |
iVeliparib-AP6 関連分類
HY-130646 関連分類
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