MTX-216
MTX-216 is a dual ATP-competitive inhibitor of PI3K and EGFR. MTX-216 cosuppresses Ki-67 and ribosomal S6 phosphorylation and induces apoptosis in NF1LOF cells. MTX-216 suppresses the activity of SYK kinase, with an IC50 of 281 nM. MTX-216 is used in the research of Melanoma.
For research use only. We do not sell to patients.
- CAS No.: 1952236-19-9
- Formula: C22H14Cl2FN5O2S
- Molecular Weight:502.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All EGFR Isoforms
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Biological Activity
MTX-216 is highly effective in blocking NF1LOF melanoma growth in vitro and in vivo[1].
MTX-216 suppresses the expression of a group of genes that regulate the mitochondrial electron transport chain[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1952236-19-9
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Appearance Solid
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Molecular Weight 502.35
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Formula C22H14Cl2FN5O2S
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Color Light yellow to light brown
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SMILES
N#CC1=C(NC2=CC=C(C(Cl)=C2)F)C3=CC(C4=CC(NS(=O)(C)=O)=C(Cl)N=C4)=CC=C3N=C1
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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 (199.06 mM; ultrasonic and warming and heat to 60°C; 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 (4.98 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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 (4.98 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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.
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 (276 KB)
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SDS (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 | 1.9906 mL | 9.9532 mL | 19.9064 mL | 49.7661 mL |
| 5 mM | 0.3981 mL | 1.9906 mL | 3.9813 mL | 9.9532 mL | |
| 10 mM | 0.1991 mL | 0.9953 mL | 1.9906 mL | 4.9766 mL | |
| 15 mM | 0.1327 mL | 0.6635 mL | 1.3271 mL | 3.3177 mL | |
| 20 mM | 0.0995 mL | 0.4977 mL | 0.9953 mL | 2.4883 mL | |
| 25 mM | 0.0796 mL | 0.3981 mL | 0.7963 mL | 1.9906 mL | |
| 30 mM | 0.0664 mL | 0.3318 mL | 0.6635 mL | 1.6589 mL | |
| 40 mM | 0.0498 mL | 0.2488 mL | 0.4977 mL | 1.2442 mL | |
| 50 mM | 0.0398 mL | 0.1991 mL | 0.3981 mL | 0.9953 mL | |
| 60 mM | 0.0332 mL | 0.1659 mL | 0.3318 mL | 0.8294 mL | |
| 80 mM | 0.0249 mL | 0.1244 mL | 0.2488 mL | 0.6221 mL | |
| 100 mM | 0.0199 mL | 0.0995 mL | 0.1991 mL | 0.4977 mL |