PLK1-IN-6
Based on 1 Customer Validation
PLK1-IN-6 is a potent and selective PLK1 inhibitor, with an IC50 of 0.45 nM. PLK1-IN-6 shows significant anti-proliferative activities against cancer cells.
For research use only. We do not sell to patients.
- Purity: 99.60%
- CAS No.: 3038489-04-9
- Formula: C28H37N9O3
- Molecular Weight:547.65
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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
Biological Activity
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PLK1 0.45 nM (IC50) |
PLK2 5.73 nM (IC50) |
PLK3 7.56 nM (IC50) |
BRD4 156.3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
26 nM
Compound: 21g
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Antiproliferative activity against human HCT-116 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human HCT-116 cells incubated for 72 to 96 hrs by microplate reader analysis
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[PMID: 36889251] |
| MCF7 | IC50 |
8.64 nM
Compound: 21g
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Antiproliferative activity against human MCF7 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human MCF7 cells incubated for 72 to 96 hrs by microplate reader analysis
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[PMID: 36889251] |
| MDA-MB-231 | IC50 |
14.8 nM
Compound: 21g
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Antiproliferative activity against human MDA-MB-231 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 to 96 hrs by microplate reader analysis
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[PMID: 36889251] |
| MV4-11 | IC50 |
47.4 nM
Compound: 21g
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Antiproliferative activity against human MV4-11 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human MV4-11 cells incubated for 72 to 96 hrs by microplate reader analysis
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[PMID: 36889251] |
PLK1-IN-6 (compound 21 g) shows significant anti-proliferative activities against four tumor-derived cell lines (MCF-7 IC50=8.64 nM, HCT-116 IC50=26.0 nM, MDA-MB-231 IC50=14.8 nM and MV4-11 IC50=47.4 nM)[1].
PLK1-IN-6 shows moderate metabolism and the half-life in human liver microsome is 25.7 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PLK1-IN-6 (10 mg/kg; i.g.) exhibits low clearance values and high plasma exposure (26800 ng•h/mL), with favorable bioavailability (11.4%) in Sprague Dawley rats[1].
PLK1-IN-6 (10 mg/kg; i.g.) exhibits long half-life (2.73 h), high plasma exposure (11227 ng•h/mL) and excellent bioavailability (77.4%) in Balb/c mice[1].
PLK1-IN-6 (20 mg/kg; i.g.) shows no apparent toxicity in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3038489-04-9
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Appearance Solid
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Molecular Weight 547.65
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Formula C28H37N9O3
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Color White to off-white
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SMILES
CC[C@@H]1C(N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C5=NOC(CN6CCNCC6)=N5)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 (182.60 mM; ultrasonic and warming and heat to 60°C; 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: ≥ 2.5 mg/mL (4.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.56 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (272 KB)
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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)
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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 | 1.8260 mL | 9.1299 mL | 18.2598 mL | 45.6496 mL |
| 5 mM | 0.3652 mL | 1.8260 mL | 3.6520 mL | 9.1299 mL | |
| 10 mM | 0.1826 mL | 0.9130 mL | 1.8260 mL | 4.5650 mL | |
| 15 mM | 0.1217 mL | 0.6087 mL | 1.2173 mL | 3.0433 mL | |
| 20 mM | 0.0913 mL | 0.4565 mL | 0.9130 mL | 2.2825 mL | |
| 25 mM | 0.0730 mL | 0.3652 mL | 0.7304 mL | 1.8260 mL | |
| 30 mM | 0.0609 mL | 0.3043 mL | 0.6087 mL | 1.5217 mL | |
| 40 mM | 0.0456 mL | 0.2282 mL | 0.4565 mL | 1.1412 mL | |
| 50 mM | 0.0365 mL | 0.1826 mL | 0.3652 mL | 0.9130 mL | |
| 60 mM | 0.0304 mL | 0.1522 mL | 0.3043 mL | 0.7608 mL | |
| 80 mM | 0.0228 mL | 0.1141 mL | 0.2282 mL | 0.5706 mL | |
| 100 mM | 0.0183 mL | 0.0913 mL | 0.1826 mL | 0.4565 mL |
PLK1-IN-6 Related Classifications
HY-149100 Related Classifications
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