Plogosertib
Based on 1 publication(s) in Google Scholar
Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers.
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- Pureté: 98.59%
- CAS No.: 1137212-79-3
- Formule: C34H48N8O3
- Masse moléculaire:616.80
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Plogosertib
More
Activité biologique
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PLK1 3 nM (IC50) |
PLK2 149 nM (IC50) |
PLK3 393 nM (IC50) |
Plogosertib (CYC140) selectively inhibits PLK1 (IC50: 3 nM), and is >50 fold more potent against PLK2 and PLK3 (IC50s: 149 nM and 393 nM, respectively)[2].
Plogosertib (0-4 μΜ, 2 h) reduces phosphorylation of the PLK1 substrate, pSer4-nucleophosmin (p-NPM) in KYSE-410 cells[2].
Plogosertib (100 nM, 24 h) increases in the proportion of mitotic cells, with increased monopolar spindles in HeLa cells[2].
Plogosertib (72 h) preferentially inhibits cell proliferation in malignant cell lines (IC50s: 14-21 nM), and is less toxic against none-malignant cell lines (IC50: 82 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KYSE-410 cells
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Concentration:0, 0.07, 0.15, 0.3, 0.6, 1.25 μΜ
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Incubation Time:72 h
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Result:Inhibited cell proliferation in a concentration-dependent manner.
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Cell Line:KYSE-410 cells
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Concentration:0, 0.01, 0.025, 0.05, 0.1, 0.25, 0.5, 1, 2, 4 μΜ
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Incubation Time:2 h (p-NPM), 24 h (p-HH3), 72 h (cPARP)
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Result:Reduced phosphorylation of the PLK1 substrate (p-NPM).
Increased in the mitotic marker pSer10 histone H3 (p-HH3), and the cleavage of PARP (cPARP, an indicator of cell death).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HL60 promyelocytic leukemia xenograft[2]
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Dosage:40, 54, 67 mg/kg, qd 5/2/5
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Administration:Oral administration
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Result:Inhibited tumor growth (>87%) without significant loss in body weight.
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Animal Model:OE19 esophageal xenograft[2]
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Dosage:40 mg/kg, qd 5/2
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Administration:Oral administration
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Result:Inhibited tumor growth (61 % inhibition).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1137212-79-3
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Appearance Solid
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Masse moléculaire 616.80
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Formule C34H48N8O3
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Color White to off-white
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SMILES
O=C1C2(CC2)CN(C3CCCC3)C4=NC(NC5=C(C=C(C=C5)C(N[C@@H]6CC[C@@H](N7CCN(CC7)C)CC6)=O)OC)=NC=C4N1C
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Synonyms
CYC140
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep
Proteomic analysis reveals a PLK1-dependent G2/M degradation program and a role for AKAP2 in coordinating the mitotic cytoskeleton. [Abstract]2024 Jul 16;43(8):114510. PMID: 39018246
Solvant et solubilité
DMSO : 100 mg/mL (162.13 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (4.05 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 (4.05 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 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 (sealed storage, away from moisture and light)
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.
Pureté et documentation
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Fiche technique (278 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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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture and light). 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 | 1.6213 mL | 8.1064 mL | 16.2127 mL | 40.5318 mL |
| 5 mM | 0.3243 mL | 1.6213 mL | 3.2425 mL | 8.1064 mL | |
| 10 mM | 0.1621 mL | 0.8106 mL | 1.6213 mL | 4.0532 mL | |
| 15 mM | 0.1081 mL | 0.5404 mL | 1.0808 mL | 2.7021 mL | |
| 20 mM | 0.0811 mL | 0.4053 mL | 0.8106 mL | 2.0266 mL | |
| 25 mM | 0.0649 mL | 0.3243 mL | 0.6485 mL | 1.6213 mL | |
| 30 mM | 0.0540 mL | 0.2702 mL | 0.5404 mL | 1.3511 mL | |
| 40 mM | 0.0405 mL | 0.2027 mL | 0.4053 mL | 1.0133 mL | |
| 50 mM | 0.0324 mL | 0.1621 mL | 0.3243 mL | 0.8106 mL | |
| 60 mM | 0.0270 mL | 0.1351 mL | 0.2702 mL | 0.6755 mL | |
| 80 mM | 0.0203 mL | 0.1013 mL | 0.2027 mL | 0.5066 mL | |
| 100 mM | 0.0162 mL | 0.0811 mL | 0.1621 mL | 0.4053 mL |
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