Art. -Nr.: HY-130257

CP5V

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CP5V is a Cdc20 PROTAC degrader with a DC₅₀ of 1.6 μM and a K_d 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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Reinheit: 99.31%
CAS. Nr.: 2509359-75-3
Formel: C₄₆H₆₆Cl₃N₉O₁₂S
Molecular Weight:1075.49

Speicherung:

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

CP5V Chemical Structure

CAS. Nr.: 2509359-75-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CP5V is a Cdc20 PROTAC degrader with a DC₅₀ of 1.6 μM and a K_d 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^[1]^[2]. (Pink: Cdc20 ligand (HY-130841); Blue: VHL ligand (HY-125845); Black: linker (HY-116006)).

IC₅₀ & Target^[1]

Cdc20

1.6 μM (DC₅₀)

Cdc20

12.4 μM (Kd)

VHL

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

MCF-7 human breast cancer cells
Concentration:

0.1, 0.5, 1, 2, 5 μM (10 h incubation); 5 μM (time-course incubation)
Incubation Time:

2, 4, 6, 8, 10, 12, 24 h (5 μM concentration); 10 h (0.1-5 μM concentration)
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.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 human triple-negative breast cancer cells
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)
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)
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.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-231 and MDA-MB-435 human triple-negative breast cancer cells
Concentration:

1, 2, 5 μM
Incubation Time:

24 h
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.

Cell Proliferation Assay^[1]

Cell Line:

MCF-7 human breast cancer cells
Concentration:

0.1, 0.2, 0.5, 1 μM
Incubation Time:

24 h
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.

In Vivo

CP5V (100 mg/kg; i.p.; twice weekly; for 2 weeks) inhibits the growth of 4T1 breast cancer xenografts with an inhibition rate of approximately 70%^[1].
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.

Animal Model:

BALB/c mice^[1]
Dosage:

100 mg/kg
Administration:

i.p.; twice a week; 2 weeks
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.

Chemical Information

CAS. Nr. 2509359-75-3
Appearance Solid
Molecular Weight 1075.49
Formel C₄₆H₆₆Cl₃N₉O₁₂S
Color Off-white to light yellow
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (1)

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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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.75 mg/mL (3.49 mM); Clear solution

This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chi JJ, et al. A novel strategy to block mitotic progression for targeted therapy. EBioMedicine. 2019 Nov;49:40-54. [Content Brief]

[2]. T. Dey, et al. Non-canonical CDC20-securin Signaling Drives Pulmonary Vascular Cell Hyper-proliferation, Remodeling, and Pulmonary Hypertension, American Journal of Respiratory and Critical Care Medicine, Volume 211, Issue Supplement_1, May 2025, Page A2176.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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CP5V

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) CP5V

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CP5V

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) CP5V

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CP5V Related Classifications

HY-130257 Related Classifications