CPP-13
CPP-13 is a selective PARP1 PROTAC degrader with a DC50 of 0.48 nM. CPP-13 induces CRBN-dependent ubiquitination and proteasomal degradation of PARP1. CPP-13 induces DNA damage. CPP-13 inhibits the growth of BRCA-deficient breast cancer and pancreatic cancer. CPP-13 can be used in studies related to BRCA-deficient breast cancer and BRCA-deficient pancreatic cancer.
(Pink: PARP1 Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker).
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- Formule: C44H52N10O7
- Masse moléculaire:832.95
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
PARP1 0.48 nM (DC50) |
Cereblon |
In Vitro
CPP-13 (0.01-1000 nM; 24 h) potently degrades PARP1 in breast cancer MDA-MB-231 cells, with a DC50 of 0.48 nM and a Dmax of up to 90% after 24 h of treatment[1].
CPP-13 (100 nM; 1-24 h) exhibits rapid and potent PARP1 degradation kinetics in breast cancer cells MDA-MB-231 and MDA-MB-436, whereas a slower degradation rate is observed in pancreatic cancer cells Capan-1 treated with 100 nM for up to 24 h[1].
CPP-13 (0.01-1000 nM; 12-24 h) is a selective PARP1 degrader that induces concentration-dependent PARP1 degradation in MDA-MB-231, MDA-MB-436 and Capan-1 cancer cells, without affecting PARP2 levels at concentrations up to 1000 nM[1].
CPP-13 (100 nM-1 μM; 24 h) induces dose-dependent γH2AX foci formation in MDA-MB-436 and Capan-1 cancer cells, where γH2AX serves as a marker of DNA double-strand breaks; the effect is more pronounced in MDA-MB-436 cells following treatment with 1 μM for 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-231 human breast cancer cells
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Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
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Incubation Time:24 h
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Result:Induced concentration-dependent reduction of PARP1 levels.
Exhibited a half-maximal degradation concentration (DC50) of 0.48 nM.
Achieved a maximum degradation efficacy (Dₘₐₓ) of 90% relative to vehicle control.
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Cell Line:MDA-MB-231, MDA-MB-436, and Capan-1 human cancer cells
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Concentration:100 nM
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Incubation Time:1, 3, 6, 12, 24 h
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Result:Began PARP1 degradation at 1 h, reached >50% reduction by 3 h, and achieved maximal depletion at 12 h, with slight recovery at 24 h in MDA-MB-231 cells.
Achieved 50% PARP1 degradation within 1 h and maximal depletion at 12 h, with more pronounced depletion than MDA-MB-231 cells and slight recovery at 24 h in MDA-MB-436 cells.
Showed significant PARP1 degradation not evident until 6 h and only 50% depletion achieved by 12 h in Capan-1 cells.
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Cell Line:MDA-MB-436 and Capan-1 human cancer cells
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Concentration:100 nM, 1 μM
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Incubation Time:24 h
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Result:Caused no significant γH2AX induction with 100 nM in either cell line.
Significantly upregulated γH2AX levels at 1 μM in both cell lines, with approximately three-fold higher induction in MDA-MB-436 cells than in Capan-1 cells.
Parmacokinetics
Chemical Information
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Masse moléculaire 832.95
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Formule C44H52N10O7
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SMILES
CCC1=CC2=C(NC1=O)C=C(C=N2)CN3CCN(CC3)C4=CN=C(C=C4)C(NCCCCCCCC(NCCNC5=CC=CC6=C5C(N(C6=O)C7CCC(NC7=O)=O)=O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CPP-13 Related Classifications
HY-187176 Related Classifications
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