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).
For research use only. We do not sell to patients.
- CAS No.: 2229856-58-8
- Formula: C49H48ClN7O11
- Molecular Weight:946.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
CRBN-DDB1 120 nM (Ki) |
Pirin 55 nM (Kd) |
In Vitro
CCT367766 (0.5 nM; 2 hr) potently and selectively induces cereblon- and proteasome-dependent degradation of pirin in SKOV3 human ovarian cancer cells, with detectable depletion at 0.5 nM after 2 hours of treatment, and causes a 2.3-fold reduction in pirin abundance with no significant effects on other quantifiable proteins in the proteome[3].
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].
CCT367766 binds recombinant pirin with high affinity (Kd = 55 nM) and recombinant CRBN-DDB1 complex with moderate affinity (Ki = 120 nM), while possessing physicochemical properties including a LogD7.4 of 2.7 and kinetic solubility of 2 μM[1].
CCT367766 (50 nM; 2 h) potently and selectively degrades pirin in cancer cells, achieving nearly complete degradation at 50 nM after 2 h of incubation[2].
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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Molecular Weight 946.40
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)