CCT367766
CCT367766 is a pirin PROTAC degrader. CCT367766 forms a ternary complex with cereblon and induces pirin depletion via the ubiquitin-proteasome pathway in a concentration- and time-dependent manner. CCT367766 can be used for ovarian cancer research.
(Pink: Pirin ligand (HY-184542); Blue: Cereblon ligand (HY-103596); Black: linker).
At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (CCT367766 formic) usually boasts enhanced water solubility and stability.
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- CAS No.: 2229856-58-8
- Formule: C49H48ClN7O11
- Masse moléculaire:946.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Other In-stock Forms of CCT367766
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
CRBN-DDB1 120 nM (Ki) |
Pirin 55 nM (Kd) |
In Vitro
CCT367766 (0.5-1500 nM; 2-24 h) potently and selectively depletes pirin in SK-OV-3 human ovarian carcinoma cells, with near-complete degradation observed at 50 nM for 2 h, and intracellular target engagement confirmed via competition with pirin-binding ligands[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-OV-3 human ovarian carcinoma cells
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Concentration:50, 150, 250, 500, 1500 nM
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Incubation Time:24 h
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Result:Depleted pirin in SK-OV-3 human ovarian carcinoma cells, with near-complete degradation observed at 50 nM for 2 h, and intracellular target engagement confirmed via competition with pirin-binding ligands
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Cell Line:SK-OV-3 human ovarian carcinoma cells
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Concentration:0.5, 1, 2.5, 5, 7.5, 10, 25, 50 nM
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Incubation Time:2 h
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Result:Degraded pirin in cancer cells.
Chemical Information
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CAS No. 2229856-58-8
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Masse moléculaire 946.40
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Formule C49H48ClN7O11
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SMILES
O=C(C1=CC=C2N=C(CN3CCN(CCOCCOCCOC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)CC3)C=CC2=C1)NC7=CC(NC(C8=CC=C(OCCO9)C9=C8)=O)=CC=C7Cl
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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.
Pureté et documentation
Références
[1]. Chessum NEA, et al. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766). Journal of medicinal chemistry. 2018 Feb 08;61(3):918-933. [Content Brief]
[2]. Sun X, et al. PROTACs: great opportunities for academia and industry. Signal transduction and targeted therapy. 2019;4:64. [Content Brief]
Hot Topics
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Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CCT367766 Related Classifications
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