| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
CCT367766 targets the pirin protein for degradation via the CRBN-DDB1 complex. It functions as a PROTAC, recruiting the E3 ubiquitin ligase complex (CRBN-DDB1) to pirin, leading to its ubiquitination and subsequent proteasomal degradation. The compound has an IC50 of 490 nM for the CRBN-DDB1 complex. It shows good affinity for both recombinant pirin and CRBN.
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| ln Vitro |
In SK-OV-3 human ovarian cancer cells, CCT367766 (50-1500 nM; 24 hours) shows the depletion of pirin protein as a time-dependent hook-effect[1]. After two hours of treatment in SK-OV-3 cells, CCT367766 (0.5-50 nM; 2 hours) shows the concentration-dependent reduction of pirin protein[1]. In SK-OV-3 cells, pretreatment with chlorobisamide reduces pirin expression in a dose-dependent manner, as demonstrated by CCT367766 (0.5-50 nM; 2 hours) [1].
CCT367766 demonstrates potent in vitro activity by depleting pirin protein expression in SK-OV-3 human ovarian cancer cells. It causes a concentration-dependent depletion of pirin protein after 2 hours of exposure at concentrations ranging from 0.5 to 50 nM. Complete degradation of pirin is observed at 50 nM treatment. It also shows a time-dependent hook-effect at higher concentrations (50-1500 nM) over 24 hours. |
| ln Vivo |
Specific in vivo activity data for CCT367766 is not extensively detailed in the available literature. As a PROTAC-based protein degradation probe, it is designed to be orally active and to deplete pirin protein expression in vivo. Preclinical studies would typically involve administration to animal models to evaluate its efficacy in degrading pirin and its potential therapeutic effects.
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| Enzyme Assay |
CCT367766's activity as a PROTAC is assessed using in vitro binding assays to measure its affinity for pirin and CRBN. Surface plasmon resonance (SPR) or other biophysical techniques can be used to determine the Kd values, which are 55 nM for pirin and 120 nM for CRBN. The compound's ability to recruit the CRBN-DDB1 complex is evaluated, with an IC50 of 490 nM.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: SK-OV-3 human ovarian cancer cells Tested Concentrations: 50, 150, 250, 500 and 1500 nM Incubation Duration: 2 hrs (hours), 4 hrs (hours), 24 hrs (hours) Experimental Results: diminished pirin protein expression. Western Blot Analysis[1] Cell Types: SK-OV-3 human ovarian cancer cells Tested Concentrations: 0.5, 1, 2.5, 5, 7.5, 10, 25, and 50 nM Incubation Duration: 2 hrs (hours) Experimental Results: Completely degraded pirin just at 50 nM treatment. Cellular assays for CCT367766 involve treating SK-OV-3 human ovarian cancer cells with the compound and measuring pirin protein levels by Western blot analysis. Cells are treated with various concentrations (0.5-1500 nM) for different time periods (2-24 hours). The concentration-dependent and time-dependent depletion of pirin protein is assessed to evaluate the compound's efficacy. |
| Animal Protocol |
In vivo animal model protocols for CCT367766 would involve oral administration to tumor-bearing mice to evaluate its ability to degrade pirin protein in vivo. The compound's efficacy in depleting pirin expression in tumor tissues and its potential antitumor activity would be assessed. Pharmacodynamic studies would measure pirin protein levels in treated tumors to confirm target engagement.
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| ADME/Pharmacokinetics |
CCT367766 is an orally active compound. Specific pharmacokinetic data is not extensively detailed in the available literature. As a PROTAC molecule, it would be expected to have properties suitable for oral administration. The compound has a molecular weight of 946.40 and a molecular formula of C49H48ClN7O11.
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| Toxicity/Toxicokinetics |
CCT367766 is intended for research use only and not for human consumption. As a research compound, its comprehensive toxicological profile may not be fully characterized. It would require standard safety assessments for clinical development. The compound is typically stored at recommended conditions as per the Certificate of Analysis.
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| References | |
| Additional Infomation |
CCT367766 (CAS# 2229856-58-8) is a research compound used to study pirin protein function and validate it as a therapeutic target. It is a third-generation PROTAC that demonstrates potent and selective degradation of pirin. The compound is supplied as a solid powder for research purposes. It serves as a useful chemical tool to investigate the biological role of pirin.
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| Molecular Formula |
C49H48CLN7O11
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|---|---|
| Molecular Weight |
946.398731231689
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| Exact Mass |
945.31
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| CAS # |
2229856-58-8
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| PubChem CID |
135397706
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
68
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| Complexity |
1790
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)OCCOCCOCCN4CCN(CC4)CC5=NC6=C(C=C5)C=C(C=C6)C(=O)NC7=C(C=CC(=C7)NC(=O)C8=CC9=C(C=C8)OCCO9)Cl
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| InChi Key |
MYFXVOSCUJQYET-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C49H48ClN7O11/c50-36-9-8-33(52-45(59)32-6-12-40-42(27-32)68-25-24-66-40)28-38(36)53-46(60)31-5-10-37-30(26-31)4-7-34(51-37)29-56-16-14-55(15-17-56)18-19-64-20-21-65-22-23-67-41-3-1-2-35-44(41)49(63)57(48(35)62)39-11-13-43(58)54-47(39)61/h1-10,12,26-28,39H,11,13-25,29H2,(H,52,59)(H,53,60)(H,54,58,61)
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| Chemical Name |
N-[2-chloro-5-(2,3-dihydro-1,4-benzodioxine-6-carbonylamino)phenyl]-2-[[4-[2-[2-[2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyethoxy]ethoxy]ethyl]piperazin-1-yl]methyl]quinoline-6-carboxamide
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| Synonyms |
CCT367766; CCT 367766; CCT-367766
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0566 mL | 5.2832 mL | 10.5664 mL | |
| 5 mM | 0.2113 mL | 1.0566 mL | 2.1133 mL | |
| 10 mM | 0.1057 mL | 0.5283 mL | 1.0566 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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