PMV6-PEG4-BI2536
Based on 1 Customer Validation
PMV6-PEG4-BI2536 is a p53-Y220C-PLK1 dual-functional compound, composed of a high-affinity p53-Y220C mutant binder (Kd ≈ 2.5 nM) and a potent PLK1 kinase inhibitor (IC50 = 0.83 nM). PMV6-PEG4-BI2536 triggers TP53Y220C cell G2/M arrest and apoptosis through PLK1 mislocalization and kinase inhibition, independent of p53 transcriptional reactivation. PMV6-PEG4-BI2536 can be used for the study of TP53 mutant cancers.
For research use only. We do not sell to patients.
- Purity: 98.47%
- Formula: C59H75F3N10O11S
- Molecular Weight:1189.35
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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PLK1 0.83 nM (IC50) |
Chemical Information
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Appearance Solid
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Molecular Weight 1189.35
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Formula C59H75F3N10O11S
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Color Light yellow to light brown
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SMILES
O=C(NCCOCCOCCOCCOCCC(N1CCC(NC2=CC=CC3=C2C=C(C#CCNC4=CC=C(S(=O)(C)=O)C=C4OC)N3CC(F)(F)F)CC1)=O)C5=CC=C(NC(N=C6N(C7CCCC7)[C@@H]8CC)=NC=C6N(C)C8=O)C(OC)=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (84.08 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 (4.20 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 (268 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 | 0.8408 mL | 4.2040 mL | 8.4080 mL | 21.0199 mL |
| 5 mM | 0.1682 mL | 0.8408 mL | 1.6816 mL | 4.2040 mL | |
| 10 mM | 0.0841 mL | 0.4204 mL | 0.8408 mL | 2.1020 mL | |
| 15 mM | 0.0561 mL | 0.2803 mL | 0.5605 mL | 1.4013 mL | |
| 20 mM | 0.0420 mL | 0.2102 mL | 0.4204 mL | 1.0510 mL | |
| 25 mM | 0.0336 mL | 0.1682 mL | 0.3363 mL | 0.8408 mL | |
| 30 mM | 0.0280 mL | 0.1401 mL | 0.2803 mL | 0.7007 mL | |
| 40 mM | 0.0210 mL | 0.1051 mL | 0.2102 mL | 0.5255 mL | |
| 50 mM | 0.0168 mL | 0.0841 mL | 0.1682 mL | 0.4204 mL | |
| 60 mM | 0.0140 mL | 0.0701 mL | 0.1401 mL | 0.3503 mL | |
| 80 mM | 0.0105 mL | 0.0525 mL | 0.1051 mL | 0.2627 mL |