PROTAC PARP1 degrader-1
Based on 1 Customer Validation
PROTAC PARP1 degrader-1 is a PARP1 PROTAC degrader with a DC50 value of 252.5 nM. PROTAC PARP1 degrader-1, combined with Daunorubicin (HY-13062A), induces the accumulation of cytoplasmic DNA fragments, activates the cGAS/STING innate immune pathway, and remodels the tumor microenvironment. PROTAC PARP1 degrader-1 can be used in research related to breast cancer.
(Pink: PARP-1 ligand (HY-W973851); Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.86%
- CAS No.: 3032324-56-1
- Formula: C32H28N6O5
- Molecular Weight:576.60
-
Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, 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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Epigenetics Compound Library
HY-L005
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
PROTAC Library
HY-L151
-
MCE Bioactive Compound Library
HY-L001V
-
High-Throughput Bioactive Compound Library
HY-L205
-
Molecular Glue-like Compound Library
HY-L918
All PROTACs Isoforms
More
Biological Activity
|
PARP-1 252.5 nM (DC50) |
PROTAC PARP1 degrader-1 (CN0) (10 μM; 24 h) does not induce DNA damage alone, but cotreatment with Daunorubicin inhibits DNA repair in MDA-MB-231 breast cancer cells, leading to significant accumulation of DNA double-strand breaks and cytosolic dsDNA[1].
PROTAC PARP1 degrader-1 (CN0) (10 μM) alone does not significantly inhibit cell growth, but cotreatment with Daunorubicin synergistically inhibits growth of MDA-MB-231 and 4T1 breast cancer cells (CI < 1) without affecting untransformed MCF-10A breast epithelial cells[1].
PROTAC PARP1 degrader-1 (CN0) (10 μM; 24 h) alone does not activate the cGAS/STING pathway, but cotreatment with Daunorubicin significantly activates the cGAS/STING innate immune pathway in MDA-MB-231 breast cancer cells, increasing key phosphoprotein levels and proinflammatory cytokine/chemokine gene expression[1].
PROTAC PARP1 degrader-1 (CN0) (10 μM; 24 h pretreatment) alone enhances T cell-mediated killing of MDA-MB-231 breast cancer cells, and cotreatment with Daunorubicin significantly increases this killing effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Cmax | AUC0-t | MRT |
|---|---|---|---|---|---|---|
| Rat[1] | 8 mg/kg | i.v. | 112.24 min | 5770.34 ng/mL | 417540.48 mg/min/L | 152.92 min |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:immunocompetent (bearing 4T1 allograft tumors)[1]
-
Dosage:25 mg/kg (single-agent); 25 mg/kg (combined with daunorubicin 0.5 mg/kg)
-
Administration:i.p.; daily for 4 days, then daily on days 15-18
-
Result:Reduced PARP1 protein levels in tumor tissue to 0.10 relative to β-actin.
Reduced final tumor weight.
Showed no significant body weight loss.
Increased CD8-positive T cell infiltration in tumor tissue.
Chemical Information
-
CAS No. 3032324-56-1
-
Appearance Solid
-
Molecular Weight 576.60
-
Formula C32H28N6O5
-
Color Light yellow to yellow
-
SMILES
NC(C1=CC=CC2=CN(N=C21)C3=CC=C(C=C3)C4CN(CCC4)C5=C(C6=CC=C5)C(N(C6=O)C7CCC(NC7=O)=O)=O)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 25 mg/mL (43.36 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, 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 (protect from light, 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (277 KB)
-
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)
-
Handling Instructions (2659 KB)
References
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, 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 | 1.7343 mL | 8.6715 mL | 17.3430 mL | 43.3576 mL |
| 5 mM | 0.3469 mL | 1.7343 mL | 3.4686 mL | 8.6715 mL | |
| 10 mM | 0.1734 mL | 0.8672 mL | 1.7343 mL | 4.3358 mL | |
| 15 mM | 0.1156 mL | 0.5781 mL | 1.1562 mL | 2.8905 mL | |
| 20 mM | 0.0867 mL | 0.4336 mL | 0.8672 mL | 2.1679 mL | |
| 25 mM | 0.0694 mL | 0.3469 mL | 0.6937 mL | 1.7343 mL | |
| 30 mM | 0.0578 mL | 0.2891 mL | 0.5781 mL | 1.4453 mL | |
| 40 mM | 0.0434 mL | 0.2168 mL | 0.4336 mL | 1.0839 mL |
PROTAC PARP1 degrader-1 Related Classifications
HY-158045 Related Classifications
Powered by Bioz