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)).
For research use only. We do not sell to patients.
- Purity : 99.84%
- CAS No.: 2472645-27-3
- Formula: C40H53N7O11
- Molecular Weight:807.89
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
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PARP1 69 nM (IC50) |
PARP2 21 nM (IC50) |
PARP1 36 nM (ED50) |
PARP2 63 nM (ED50) |
Cereblon |
In Vitro
Chemical Information
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CAS No. 2472645-27-3
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Appearance Solid
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Molecular Weight 807.89
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 Related Classifications
HY-130646 Related Classifications
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