T-1-PMPA
Based on 1 Customer Validation
T-1-PMPA is a potent EGFR inhibitor with apoptotic properties. T-1-PMPA effectively inhibits EGFRWT and EGFR790m, with IC50 values of 86 nM and 561.73 nM, respectively.
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- Pureza: 99.70%
- No. CAS: 1323883-62-0
- Fòrmula: C16H17N5O3
- Peso molecular:327.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Ver todos los productos específicos de isoformas EGFR
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Actividad biológica
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EGFRWT 86 nM (IC50) |
EGFRT790M 561.73 nM (IC50) |
T-1-PMPA (0.312-10 μM; 24 h) shows significant suppression of the proliferation of HepG2 and MCF7 malignant cell lines, with IC50 values of 3.51 μM and 4.13 μM, respectively[1]. In HepG2 cells, T-1-PMPA increases the proportion of cells in the early stage of apoptosis from 0.77 to 29.17%, the late stage of apoptosis from 0.17 to 8.81%, and the overall stage from 3.05 to 42.03%. Additionally, the percentage of necrotic cells increased to 4.05% compared to 2.21% in the control cells. The qRT-PCR analysis further supported the apoptotic effects by revealing significant increases in the levels of caspase-3 and caspase-9. T-1-PMPA controlls the levels of TNFα and IL2 by 74 and 50%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 and MCF7 malignant cell lines
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Concentration:0.312 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Showed significant suppression of the proliferation of HepG2 and MCF7 malignant cell lines.
Chemical Information
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No. CAS 1323883-62-0
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Appearance Solid
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Peso molecular 327.34
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Fòrmula C16H17N5O3
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Color White to off-white
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SMILES
CC1=CC=C(C=C1)NC(CN2C(C3=C(N(C2=O)C)N=CN3C)=O)=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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (305.49 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: ≥ 2.5 mg/mL (7.64 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.
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 3.0549 mL | 15.2746 mL | 30.5493 mL | 76.3732 mL |
| 5 mM | 0.6110 mL | 3.0549 mL | 6.1099 mL | 15.2746 mL | |
| 10 mM | 0.3055 mL | 1.5275 mL | 3.0549 mL | 7.6373 mL | |
| 15 mM | 0.2037 mL | 1.0183 mL | 2.0366 mL | 5.0915 mL | |
| 20 mM | 0.1527 mL | 0.7637 mL | 1.5275 mL | 3.8187 mL | |
| 25 mM | 0.1222 mL | 0.6110 mL | 1.2220 mL | 3.0549 mL | |
| 30 mM | 0.1018 mL | 0.5092 mL | 1.0183 mL | 2.5458 mL | |
| 40 mM | 0.0764 mL | 0.3819 mL | 0.7637 mL | 1.9093 mL | |
| 50 mM | 0.0611 mL | 0.3055 mL | 0.6110 mL | 1.5275 mL | |
| 60 mM | 0.0509 mL | 0.2546 mL | 0.5092 mL | 1.2729 mL | |
| 80 mM | 0.0382 mL | 0.1909 mL | 0.3819 mL | 0.9547 mL | |
| 100 mM | 0.0305 mL | 0.1527 mL | 0.3055 mL | 0.7637 mL |
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