PK11000
Based on 1 Customer Validation
PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.56%
- No. CAS: 38275-34-2
- Fòrmula: C6H5ClN2O4S
- Peso molecular:236.63
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
p53[1]
PK11000 (0-120 μM, 24 h) mildly inhibits mutant p53 cancer cells[1].
PK11000 (0-50 μM, 5 d) shows anti-proliferation effects of breast cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:WI-38, HUH-6, NUGC-4, SJSA-1, HUH-7, NUGC-3, SW480 and MKN1 cells
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Concentration:0-120 μM
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Incubation Time:24 hours
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Result:Inhibited NUGC-3 cells mildly.
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Cell Line:UACC812, BT474, ZR-75-1, SUM 159, MDA-MD-468, MDA-MD-453, T47D, Hs578T(i8), MCF7, HCC1937, JimT1, BT20, HCC1143, BT549, SKBR3, MCF12A, MCF10A cells
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Concentration:0-50 μM
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Incubation Time:5 days
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Result:Inhibited breast cell lines with IC50 values ranging from 2.5 to >50 µM.
Chemical Information
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No. CAS 38275-34-2
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Appearance Solid
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Peso molecular 236.63
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Fòrmula C6H5ClN2O4S
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Color White to off-white
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SMILES
O=C(C1=NC(S(=O)(C)=O)=NC=C1Cl)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 100 mg/mL (422.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (105.65 mM; Need ultrasonic)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (10.57 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 (10.57 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 20 mg/mL (84.52 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bauer MR, et al. 2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells. Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5271-80. [Content Brief]
[2]. Naoise C Synnott, et al. Mutant p53 as a therapeutic target for the treatment of triple-negative breast cancer: Preclinical investigation with the anti-p53 drug, PK11007. Cancer Lett. 2018 Feb 1;414:99-106. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.2260 mL | 21.1300 mL | 42.2601 mL | 105.6502 mL |
| 5 mM | 0.8452 mL | 4.2260 mL | 8.4520 mL | 21.1300 mL | |
| 10 mM | 0.4226 mL | 2.1130 mL | 4.2260 mL | 10.5650 mL | |
| 15 mM | 0.2817 mL | 1.4087 mL | 2.8173 mL | 7.0433 mL | |
| 20 mM | 0.2113 mL | 1.0565 mL | 2.1130 mL | 5.2825 mL | |
| 25 mM | 0.1690 mL | 0.8452 mL | 1.6904 mL | 4.2260 mL | |
| 30 mM | 0.1409 mL | 0.7043 mL | 1.4087 mL | 3.5217 mL | |
| 40 mM | 0.1057 mL | 0.5283 mL | 1.0565 mL | 2.6413 mL | |
| 50 mM | 0.0845 mL | 0.4226 mL | 0.8452 mL | 2.1130 mL | |
| 60 mM | 0.0704 mL | 0.3522 mL | 0.7043 mL | 1.7608 mL | |
| 80 mM | 0.0528 mL | 0.2641 mL | 0.5283 mL | 1.3206 mL | |
| 100 mM | 0.0423 mL | 0.2113 mL | 0.4226 mL | 1.0565 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
PK11000 Related Classifications
HY-U00447 Related Classifications
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