CP5V
Based on 1 publication(s) in Google Scholar
CP5V is a Cdc20 PROTAC degrader with a DC50 of 1.6 μM and a Kd value of 12.4 μM. CP5V couples Cdc20 with the VHL/VBC complex, triggering its ubiquitination and proteasomal degradation, thereby reducing the protein levels of Cdc20 and securin. CP5V induces mitotic arrest, inhibits cell proliferation, resensitizes Paclitaxel-resistant breast cancer cells, and suppresses breast tumor progression in xenograft models. CP5V inhibits excessive proliferation and induces apoptosis in pulmonary arterial hypertension smooth muscle cells and fibroblasts. CP5V can be used in studies related to breast cancer and pulmonary arterial hypertension.
(Pink: Cdc20 ligand (HY-130841); Blue: VHL ligand (HY-125845); Black: linker (HY-116006)).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.31%
- CAS 番号: 2509359-75-3
- 分子式: C46H66Cl3N9O12S
- 分子量:1075.49
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 CP5V
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生物活性
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Cdc20 1.6 μM (DC50) |
Cdc20 12.4 μM (Kd) |
VHL |
CP5V (0.1-5 μM; 2-24 h) potently degrades Cdc20 in MCF-7 breast cancer cells, with a DC50 of 1.6 μM and a half-life of 4 h for Cdc20[1].
CP5V (0.5-10 μM; 2-24 h) potently degrades Cdc20 in MDA-MB-231 triple-negative breast cancer cells via the VHL-dependent ubiquitin-proteasome pathway, with a DC50 of 1.6 μM and a Cdc20 half-life of 4 h, thereby leading to the accumulation of cyclin B and securin[1].
CP5V (72 h) inhibits the proliferation of triple-negative breast cancer cells MDA-MB-231 and MDA-MB-435, with IC50 values of 2.6 μM and 2.0 μM, respectively[1].
CP5V (0.1-1 μM; 24 h) reduces the clonogenic survival rate of MCF-7 breast cancer cells in a dose-dependent manner[1].
CP5V (1-5 μM; 72 h) restores the sensitivity of Paclitaxel (HY-B0015)- and Tamoxifen (HY-13757A)-resistant MDA-MB-435 eb breast cancer cells to Paclitaxel and Tamoxifen[1].
CP5V (1-5 μM; 24 h) induces G2/M phase mitotic arrest in synchronized MDA-MB-231 and MDA-MB-435 triple-negative breast cancer cells, with 35% and 45% of cells arrested at the concentration of 2 μM, respectively[1].
CP5V reduces the protein levels of CDC20 and securin, inhibits cell proliferation, restores BIM expression, and induces apoptosis in human pulmonary arterial hypertension pulmonary artery smooth muscle cells (PAH PASMCs) and pulmonary artery fibroblasts (PAAFs), while exerting no effect on control human pulmonary artery smooth muscle cells and pulmonary artery fibroblasts[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:0.1, 0.5, 1, 2, 5 μM (10 h incubation); 5 μM (time-course incubation)
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Incubation Time:2, 4, 6, 8, 10, 12, 24 h (5 μM concentration); 10 h (0.1-5 μM concentration)
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Result:Induced dose-dependent degradation of Cdc20, with a DC50 (concentration for 50% maximum degradation) of approximately 1.6 μM.
Reduced the half-life of Cdc20 to approximately 4 h.
Suppressed Cdc20 levels for at least 24 h.
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Cell Line:MDA-MB-231 human triple-negative breast cancer cells
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Concentration:0.5, 1, 2, 5, 10 μM (10 h incubation); 10 μM (time-course incubation); 2 μM (8 h treatment, followed by recovery); 2 μM (6 h co-treatment with MG-132 (HY-13259)); 2-5 μM (10 h co-treatment with MG-132)
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Incubation Time:2, 4, 6, 8, 10, 12, 24 h (10 μM concentration); 10 h (0.5-10 μM concentration); 8 h (2 μM treatment, followed by 0-24 h recovery); 6 h (2 μM + MG-132 co-treatment); 10 h (2-5 μM + MG-132 co-treatment)
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Result:Induced dose-dependent degradation of Cdc20, with a DC50 of approximately 1.6 μM.
Reduced the half-life of Cdc20 to approximately 4 h.
Suppressed Cdc20 levels for at least 24 h.
Caused Cdc20 levels to begin recovering within 24 h after removal.
Significantly enhanced Cdc20 ubiquitination.
Had its induced Cdc20 degradation attenuated by co-treatment with MG-132, confirming proteasome-dependent degradation.
Caused accumulation of cyclin B and securin, downstream substrates of Cdc20-APC/C.
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Cell Line:MDA-MB-231 and MDA-MB-435 human triple-negative breast cancer cells
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Concentration:1, 2, 5 μM
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Incubation Time:24 h
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Result:Induced dramatic mitotic arrest in both cell lines.
Arrested over 35% of MDA-MB-231 cells in the G2/M phase at 2 μM, with corresponding reductions in the G0/G1 phase population.
Arrested over 45% of MDA-MB-435 cells in the G2/M phase at 2 μM, with corresponding reductions in the G0/G1 phase population.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:0.1, 0.2, 0.5, 1 μM
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Incubation Time:24 h
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Result:Reduced colony formation in a dose-dependent manner.
Significantly decreased the number of surviving colonies compared to controls at 1 μM.
Exhibited significant inhibition at concentrations as low as 0.1 μM and maximal efficacy at 1 μM.
CP5V reverses SuHx-induced pulmonary artery remodeling, pulmonary hypertension, and right ventricular hypertrophy in male and female mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice[1]
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Dosage:100 mg/kg
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Administration:i.p.; twice a week; 2 weeks
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Result:Reduced 4T1 xenograft tumor size and weight by approximately 70% compared to placebo treatment.
Reduced Cdc20 expression in tumors compared to placebo treatment.
Lowered Ki67 index in tumors compared to placebo treatment.
Caused no significant effect on mouse body weight or liver toxicity.
化学情報
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CAS 番号 2509359-75-3
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性状 Solid
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分子量 1075.49
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分子式 C46H66Cl3N9O12S
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Color Off-white to light yellow
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SMILES
ClC(Cl)(Cl)C(NC(OCCCNC(CCOCCOCCOCCOCCOCCC(N[C@@H](C(C)(C)C)C(N1C[C@H](O)C[C@H]1C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O)=O)=O)NC4=NC=CC=N4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
CCDC41 Drives Oocyte Meiotic Progression by Promoting Rab11a/Rab7-Positive Vesicle Fusion with Target Membranes. [Abstract]2025 Dec 2:e04665. PMID: 41331237
溶剤 & 溶解度
DMSO : 150 mg/mL (139.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.75 mg/mL (3.49 mM); Clear solution
This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.75 mg/mL (3.49 mM); Clear solution
This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 (stored under nitrogen). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9298 mL | 4.6490 mL | 9.2981 mL | 23.2452 mL |
| 5 mM | 0.1860 mL | 0.9298 mL | 1.8596 mL | 4.6490 mL | |
| 10 mM | 0.0930 mL | 0.4649 mL | 0.9298 mL | 2.3245 mL | |
| 15 mM | 0.0620 mL | 0.3099 mL | 0.6199 mL | 1.5497 mL | |
| 20 mM | 0.0465 mL | 0.2325 mL | 0.4649 mL | 1.1623 mL | |
| 25 mM | 0.0372 mL | 0.1860 mL | 0.3719 mL | 0.9298 mL | |
| 30 mM | 0.0310 mL | 0.1550 mL | 0.3099 mL | 0.7748 mL | |
| 40 mM | 0.0232 mL | 0.1162 mL | 0.2325 mL | 0.5811 mL | |
| 50 mM | 0.0186 mL | 0.0930 mL | 0.1860 mL | 0.4649 mL | |
| 60 mM | 0.0155 mL | 0.0775 mL | 0.1550 mL | 0.3874 mL | |
| 80 mM | 0.0116 mL | 0.0581 mL | 0.1162 mL | 0.2906 mL | |
| 100 mM | 0.0093 mL | 0.0465 mL | 0.0930 mL | 0.2325 mL |
CP5V 関連分類
HY-130257 関連分類
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