CCT367766 formic
Based on 1 Customer Validation
CCT367766 formic is a pirin PROTAC degrader. CCT367766 formic forms a ternary complex with cereblon and induces pirin depletion via the ubiquitin-proteasome pathway in a concentration- and time-dependent manner. CCT367766 formic 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.
- Purity: 98.10%
- Formula: C50H50ClN7O13
- Molecular Weight:992.42
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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Biological Activity
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CRBN-DDB1 120 nM (Ki) |
Pirin 55 nM (Kd) |
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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Appearance Solid
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Molecular Weight 992.42
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Formula C50H50ClN7O13
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Color Light yellow to yellow
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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.OC=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 250 mg/mL (251.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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]
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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 1.0076 mL | 5.0382 mL | 10.0764 mL | 25.1909 mL |
| 5 mM | 0.2015 mL | 1.0076 mL | 2.0153 mL | 5.0382 mL | |
| 10 mM | 0.1008 mL | 0.5038 mL | 1.0076 mL | 2.5191 mL | |
| 15 mM | 0.0672 mL | 0.3359 mL | 0.6718 mL | 1.6794 mL | |
| 20 mM | 0.0504 mL | 0.2519 mL | 0.5038 mL | 1.2595 mL | |
| 25 mM | 0.0403 mL | 0.2015 mL | 0.4031 mL | 1.0076 mL | |
| 30 mM | 0.0336 mL | 0.1679 mL | 0.3359 mL | 0.8397 mL | |
| 40 mM | 0.0252 mL | 0.1260 mL | 0.2519 mL | 0.6298 mL | |
| 50 mM | 0.0202 mL | 0.1008 mL | 0.2015 mL | 0.5038 mL | |
| 60 mM | 0.0168 mL | 0.0840 mL | 0.1679 mL | 0.4198 mL | |
| 80 mM | 0.0126 mL | 0.0630 mL | 0.1260 mL | 0.3149 mL | |
| 100 mM | 0.0101 mL | 0.0504 mL | 0.1008 mL | 0.2519 mL |
CCT367766 formic Related Classifications
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