| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
The molecular target of CP5V is Cdc20 (cell division cycle protein 20), a key regulator of the cell cycle. CP5V recruits Cdc20 to the VHL/VBC E3 ubiquitin ligase complex, leading to its ubiquitination and proteasomal degradation. This degradation of Cdc20 induces mitotic arrest and inhibits cancer cell proliferation. The compound is a PROTAC that links a VHL ligand and a CDK ligand.
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| ln Vitro |
The VHL-binding moiety and Cdc20 ligand in CP5V are connected by a PEG5 linker, which causes Cdc20 degradation. By degrading Cdc20, CP5V considerably reduces the growth of breast cancer cells and resensitizes paclitaxel-resistant cell lines [1]. With a DC50 of about 1.6 μM, CP5V dramatically degrades Cdc20 in MCF7 and MDA-MB-231 cells[1].
In vitro studies have demonstrated that CP5V induces mitotic inhibition and suppresses cancer cell proliferation. It specifically degrades Cdc20 by linking it to the VHL/VBC complex for ubiquitination and proteasomal degradation. The compound is used as a mechanistic tool to study cell cycle regulation and oncology. |
| ln Vivo |
In vivo activity data for CP5V as a standalone compound are not extensively reported. As a PROTAC molecule, its in vivo efficacy would depend on its pharmacokinetic properties and the specific disease model being studied. It is primarily used as a research tool to study the role of Cdc20 in cell cycle regulation and cancer.
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| Enzyme Assay |
In vitro assays for CP5V typically involve studying its ability to induce Cdc20 degradation. Cells are treated with the compound, and Cdc20 levels are measured by Western blotting. Ternary complex formation assays can be performed to evaluate the ability of the compound to simultaneously engage Cdc20 and the VHL E3 ligase. Cell proliferation assays are used to assess the functional consequences of Cdc20 degradation.
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| Cell Assay |
In vitro cell-based assays for CP5V typically involve treatment of cancer cells with the compound followed by assessment of Cdc20 degradation. Cells are treated with CP5V, and Cdc20 levels are measured by Western blotting or immunofluorescence. Cell cycle analysis by flow cytometry is used to assess mitotic arrest. Cell proliferation assays are used to evaluate the effects on cancer cell growth.
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| Animal Protocol |
In vivo animal studies for CP5V are not extensively reported. As a PROTAC molecule, it could potentially be used in mouse xenograft models to assess its ability to degrade Cdc20 and inhibit tumor growth. Typical protocols would involve administering the compound to tumor-bearing mice, followed by assessment of Cdc20 degradation in tumor tissues and tumor growth inhibition.
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| ADME/Pharmacokinetics |
CP5V has a molecular formula of C46H66Cl3N9O12S and a molecular weight of 1075.49. The CAS number is 2509359-75-3. It has a predicted relative density of 1.326 g/cm3. The compound is a PROTAC molecule composed of a VHL ligand and a CDK ligand. It is intended for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of CP5V is not extensively characterized, as it is a research compound. It is intended for research use only and is not approved for therapeutic use in humans. Standard laboratory safety practices, including the use of personal protective equipment, are recommended.
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| References | |
| Additional Infomation |
CP5V (CAS 2509359-75-3) is a rationally designed PROTAC molecule composed of a von Hippel-Lindau (VHL) ligand and a cyclin-dependent kinase (CDK) ligand. It specifically degrades Cdc20 by linking it to the VHL/VBC complex for ubiquitination and proteasomal degradation. It induces mitotic inhibition and suppresses cancer cell proliferation.
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| Molecular Formula |
C46H66CL3N9O12S
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|---|---|
| Molecular Weight |
1075.49334764481
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| Exact Mass |
1073.361
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| CAS # |
2509359-75-3
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| PubChem CID |
139600343
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
33
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| Heavy Atom Count |
71
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| Complexity |
1590
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)[C@@H]3C[C@H](CN3C(=O)[C@H](C(C)(C)C)NC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCCOC(=O)NC(C(Cl)(Cl)Cl)NC4=NC=CC=N4)O
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| InChi Key |
BQQILUVLGKHSNJ-NWRQRLFSSA-N
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| InChi Code |
InChI=1S/C46H66Cl3N9O12S/c1-31-38(71-30-54-31)33-9-7-32(8-10-33)28-53-40(62)35-27-34(59)29-58(35)41(63)39(45(2,3)4)55-37(61)12-18-66-20-22-68-24-26-69-25-23-67-21-19-65-17-11-36(60)50-15-6-16-70-44(64)57-42(46(47,48)49)56-43-51-13-5-14-52-43/h5,7-10,13-14,30,34-35,39,42,59H,6,11-12,15-29H2,1-4H3,(H,50,60)(H,53,62)(H,55,61)(H,57,64)(H,51,52,56)/t34-,35+,39-,42?/m1/s1
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| Chemical Name |
3-[3-[2-[2-[2-[2-[3-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methylcarbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]propyl N-[2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethyl]carbamate
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
DMSO :~150 mg/mL (~139.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.75 mg/mL (3.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 37.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3.75 mg/mL (3.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 37.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3.75 mg/mL (3.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9298 mL | 4.6490 mL | 9.2981 mL | |
| 5 mM | 0.1860 mL | 0.9298 mL | 1.8596 mL | |
| 10 mM | 0.0930 mL | 0.4649 mL | 0.9298 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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