PLK1/BRD4-IN-5
Based on 1 Customer Validation
PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3 nM and 60.8 nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research.
For research use only. We do not sell to patients.
- Purity: 98.80%
- CAS No.: 3063893-60-4
- Formula: C31H44N8O3
- Molecular Weight:576.73
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Apoptosis Compound Library
HY-L003
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Epigenetics Compound Library
HY-L005
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Kinase Inhibitor Library
HY-L009
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Reprogramming Compound Library
HY-L039
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Orally Active Compound Library
HY-L061
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Anti-Blood Cancer Compound Library
HY-L079
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Anti-Hematopathy Compound Library
HY-L171
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Biological Activity
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PLK1 0.3 nM (IC50) |
BRD4 60.8 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
17.3 nM
Compound: SC10
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay
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[PMID: 38364599] |
| MDA-MB-361 | IC50 |
8.4 nM
Compound: SC10
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Antiproliferative activity against human MDA-MB-361 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay
Antiproliferative activity against human MDA-MB-361 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay
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[PMID: 38364599] |
| MV4-11 | IC50 |
5.4 nM
Compound: SC10
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay
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[PMID: 38364599] |
PLK1/BRD4-IN-5 (Compound SC10) shows significant anti-proliferation activity against all three tumor cell lines (MDA-MB-231 IC50 = 17.3 nM, MDA-MB-361 IC50 = 8.4 nM, MV4-11 IC50 = 5.4 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 cells
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Concentration:0.675 nM, 1.35 nM, 2.7 nM, 5.4 nM and 10.8 nM
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Incubation Time:72 h
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Result:Exhibited an increasing rate of apoptosis ranging from 6.65 to 58.35 % in a concentration-dependent manner.
Pharmacokinetic parameters of compounds in Sprague-Dawley Rats [1]
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-t (ng•h/mL) | Cl (mL•min/kg) | MRT0-t (h) | Vdss (L/kg) | F (%) |
| i.g. | 10 | 3.75 | 2.00 | 108 | 657 | / | 5.26 | / | 21.4 |
| i.v. | 1 | 4.9 | / | / | 303 | 53.6 | 4.39 | 16.4 | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3063893-60-4
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Appearance Solid
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Molecular Weight 576.73
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Formula C31H44N8O3
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Color Off-white to light yellow
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SMILES
CC[C@@H]1C(N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C5C(CCN5C(CN6C[C@@H](N[C@@H](C6)C)C)=O)=C4)OC)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (173.39 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. 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. 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)
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: ≥ 5 mg/mL (8.67 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
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.
Purity & Documentation
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Data Sheet (275 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
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. 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 | 1.7339 mL | 8.6696 mL | 17.3391 mL | 43.3478 mL |
| 5 mM | 0.3468 mL | 1.7339 mL | 3.4678 mL | 8.6696 mL | |
| 10 mM | 0.1734 mL | 0.8670 mL | 1.7339 mL | 4.3348 mL | |
| 15 mM | 0.1156 mL | 0.5780 mL | 1.1559 mL | 2.8899 mL | |
| 20 mM | 0.0867 mL | 0.4335 mL | 0.8670 mL | 2.1674 mL | |
| 25 mM | 0.0694 mL | 0.3468 mL | 0.6936 mL | 1.7339 mL | |
| 30 mM | 0.0578 mL | 0.2890 mL | 0.5780 mL | 1.4449 mL | |
| 40 mM | 0.0433 mL | 0.2167 mL | 0.4335 mL | 1.0837 mL | |
| 50 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8670 mL | |
| 60 mM | 0.0289 mL | 0.1445 mL | 0.2890 mL | 0.7225 mL | |
| 80 mM | 0.0217 mL | 0.1084 mL | 0.2167 mL | 0.5418 mL | |
| 100 mM | 0.0173 mL | 0.0867 mL | 0.1734 mL | 0.4335 mL |
PLK1/BRD4-IN-5 Related Classifications
HY-158031 Related Classifications
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