MTX-531
Based on 1 Customer Validation
MTX-531 is an oral drug that inhibits EGFR (with an IC50 of 14.7 nM) and PI3K (with IC50 values of 6.4, 233, 8.3, and 1.1 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively), and it has anti-tumor effects. MTX-531 also acts as a weak agonist of PPARγ, with an IC50 of 2.5 µM, helping to alleviate hyperglycemia induced by PI3K inhibitors.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.87%
- No. CAS: 2791417-66-6
- Fòrmula: C22H20ClN5O2S
- Peso molecular:453.94
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Almacenamiento: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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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
Descripciòn
IC50 & Target
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PI3Kα 6.4 nM (IC50) |
PI3Kβ 233 nM (IC50) |
PI3Kδ 1.1 nM (IC50) |
PI3Kγ 8.3 nM (IC50) |
PPARγ 3.4 μM (EC50) |
In Vitro
MTX-531 (0-10000 nM, 2 h) shows a concentration-dependent inhibitory effect on EGFR, P13K, and mTOR in CAL-33 cells[1].
MTX-531 is 3.4 μM with EC50 in 293H cells[1].
MTX-531 (10 μM, 8-24 h) activates PPARγ in 3T3-L1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CAL-33
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Concentration:0, 10, 30, 100, 300, 1000, 3000, 10000 nM
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Incubation Time:2 h
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Result:Suppressed EGFR, P13K, and mTOR in a concentration-dependent manner.
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Cell Line:3T3-L1
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Concentration:10 μM
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Incubation Time:8 and 24 h
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Result:Increased expression levels of PPARγ1 and PPARγ2.
In Vivo
MTX-531 (25 mg/kg, orally, once daily for 134-145 days) suppresses tumor proliferation in mice[1].
MTX-531 (100 mg/kg, orally, single dose) shows excellent tolerance in mice and uniquely does not cause the hyperglycemia commonly seen with PI3K inhibitors[1].
MTX-531 (100 mg/kg, orally, single dose) inhibits EGFR and PI3K-mTOR signaling and tumor growth in the HNSCC PDX model[1].
MTX-531 enhances MEK inhibition in CRC[1].
MTX-531 (100 mg/kg, orally, 0-35 days) combined with KRAS-G12C inhibitors suppresses tumor growth in mice with KRAS-G12C mutant colorectal cancer or pancreatic tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CAL-33 tumor-bearing mice[1]
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Dosage:100 mg/kg; single dose
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Administration:Oral
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Result:Inhibited the EGFR and PI3K-mTOR signaling pathways with time-dependent.
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Animal Model:CAL-33 tumor-bearing mice; CAL-27 tumor-bearing mice[1]
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Dosage:25mg/kg; daily; 134 days for CAL-33; 145 days for CAL-27
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Administration:Oral
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Result:Was very effective against CAL-33 and CAL-27 xenografts, showing a complete remission rate of 33-100% over a broad dosage range, and worked well for advanced CAL-33 tumors before treatment.
Chemical Information
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No. CAS 2791417-66-6
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Appearance Solid
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Peso molecular 453.94
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Fòrmula C22H20ClN5O2S
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Color White to light yellow
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SMILES
ClC1=C(NS(=O)(C)=O)C=C(C2=CC3=C(N=CN=C3N[C@@H](C4=CC=CC=C4)C)C=C2)C=N1
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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
In Vitro:
DMSO : 100 mg/mL (220.29 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)
In Vivo:
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 (11.01 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.
In Vivo Dissolution Calculator
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 (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (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 |
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| DMSO | 1 mM | 2.2029 mL | 11.0147 mL | 22.0293 mL | 55.0734 mL |
| 5 mM | 0.4406 mL | 2.2029 mL | 4.4059 mL | 11.0147 mL | |
| 10 mM | 0.2203 mL | 1.1015 mL | 2.2029 mL | 5.5073 mL | |
| 15 mM | 0.1469 mL | 0.7343 mL | 1.4686 mL | 3.6716 mL | |
| 20 mM | 0.1101 mL | 0.5507 mL | 1.1015 mL | 2.7537 mL | |
| 25 mM | 0.0881 mL | 0.4406 mL | 0.8812 mL | 2.2029 mL | |
| 30 mM | 0.0734 mL | 0.3672 mL | 0.7343 mL | 1.8358 mL | |
| 40 mM | 0.0551 mL | 0.2754 mL | 0.5507 mL | 1.3768 mL | |
| 50 mM | 0.0441 mL | 0.2203 mL | 0.4406 mL | 1.1015 mL | |
| 60 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9179 mL | |
| 80 mM | 0.0275 mL | 0.1377 mL | 0.2754 mL | 0.6884 mL | |
| 100 mM | 0.0220 mL | 0.1101 mL | 0.2203 mL | 0.5507 mL |
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