PLK1-IN-13
Based on 1 Customer Validation
PLK1-IN-13 is a selective and orally active PLK1 inhibitor (IC50: 0.27 nM). PLK1-IN-13 also inhibits PLK2 (IC50: 12.72 nM) and PLK3 (IC50: 4.12 nM). PLK1-IN-13 arrests cell at G2 phase, induces apoptosis and down-regulates the transcription of the proliferation-related oncogene c-MYC. PLK1-IN-13 inhibits tumor growth, and can be used for research of acute myeloid leukemia (AML).
For research use only. We do not sell to patients.
- Purity: 98.02%
- CAS No.: 3038489-48-1
- Formula: C29H39N9O2S
- Molecular Weight:577.74
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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 0.27 nM (IC50) |
PLK2 12.72 nM (IC50) |
PLK3 4.12 nM (IC50) |
PLK1-IN-13 (Compound WD6) (72 h) has antiproliferative activities against MDA-MB-231 (IC50: 9.5 nM) and MV4-11 cell (IC50: 23.3 nM), and the IC50 for MCF-7 and HCT-116 are 47.1 nM and 59.9 nM respectively[1].
PLK1-IN-13 has weak inhibitory effects on CYP2C9 (IC50: 7.39 μM), CYP2C19 (IC50: 14 μM), CYP2D6 (IC50: 13.8 μM), and CYP3A4 (IC50: 17.3 μM), indicating that PLK1-IN-13 may have lower drug-drug interactions[1].
PLK1-IN-13 (2.92 nM-46.6 nM, 72 h) induces G2/M cell-cycle arrest and induces apoptosis in MV4-11 cells[1].
PLK1-IN-13 (0-1 μM, 24 h) down-regulates the transcription of the proliferation-related oncogene c-MYC in MV4-11 cells[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:2.92 nM, 5.83 nM, 11.6 nM, 23.3 nM, and 46.6 nM
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Incubation Time:72 h
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Result:Increased the cell apoptosis rate, ranging from 3.29% to 67.7% in a concentration-dependent manner.
PLK1-IN-13 (10, 20 mg/kg, i.g.) shows a good half-life, high plasma exposure, and moderate bioavailability in SD rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:subcutaneous xenograft mouse models of MV4-11, Balb/c nude mice [1]
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Dosage:20 mg/kg
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Administration:p.o., once a day for 19 consecutive days.
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Result:Inhibited the tumor growth (TGI=91.2%).
Showed no significant weight loss or death in mice.
Chemical Information
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CAS No. 3038489-48-1
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Appearance Solid
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Molecular Weight 577.74
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Formula C29H39N9O2S
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Color Light yellow to yellow
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SMILES
O=C1N(C)C2=CN=C(NC3=CC=C(C4=NN=C(CN5CCN(C)CC5)S4)C=C3OC)N=C2N(C6CCCC6)[C@@H]1CC
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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 (173.09 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 (8.65 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (8.65 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 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 (274 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 |
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| DMSO | 1 mM | 1.7309 mL | 8.6544 mL | 17.3088 mL | 43.2721 mL |
| 5 mM | 0.3462 mL | 1.7309 mL | 3.4618 mL | 8.6544 mL | |
| 10 mM | 0.1731 mL | 0.8654 mL | 1.7309 mL | 4.3272 mL | |
| 15 mM | 0.1154 mL | 0.5770 mL | 1.1539 mL | 2.8848 mL | |
| 20 mM | 0.0865 mL | 0.4327 mL | 0.8654 mL | 2.1636 mL | |
| 25 mM | 0.0692 mL | 0.3462 mL | 0.6924 mL | 1.7309 mL | |
| 30 mM | 0.0577 mL | 0.2885 mL | 0.5770 mL | 1.4424 mL | |
| 40 mM | 0.0433 mL | 0.2164 mL | 0.4327 mL | 1.0818 mL | |
| 50 mM | 0.0346 mL | 0.1731 mL | 0.3462 mL | 0.8654 mL | |
| 60 mM | 0.0288 mL | 0.1442 mL | 0.2885 mL | 0.7212 mL | |
| 80 mM | 0.0216 mL | 0.1082 mL | 0.2164 mL | 0.5409 mL | |
| 100 mM | 0.0173 mL | 0.0865 mL | 0.1731 mL | 0.4327 mL |
PLK1-IN-13 Related Classifications
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