Trametiglue
Based on 1 publication(s) in Google Scholar
Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.81%
- CAS No.: 2666940-97-0
- Formule: C25H24FIN6O5S
- Masse moléculaire:666.46
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Trametiglue
MoreVoir tous les produits spécifiques à Isoform MEK
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Activité biologique
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MEK1 |
MEK2 |
Trametiglue retains the strong binding potency and residence time of Trametinib on KSR-bound MEK[1].
Trametiglue, unlike Trametinib but similar to Avutometinib (HY-18652), enhances interactions between endogenous BRAF and MEK1[1].
Trametiglue (1 μM) demonstrates high selectivity towards MEK1 and MEK2 in direct binding assays. Trametiglue also displays high selectivity in a panel of active kinases measured for inhibition of MEK1 and MEK2 substrate phosphorylation or direct MEK1 phosphorylation by the upstream kinases[1].
Trametiglue (5 days) inhibits HCT116, A375, A549 and SK-MEL-239 cells viability with IC50s of 0.07, 0.07, 0.12 and 0.47 nM, respectively[1].
Trametiglue (10 nM; 10 days) inhibits colony formation in KRAS-mutant and BRAF-mutant cancer cell lines with higher potency than Trametinib[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-MEL-239, HCT116, A549 and A375
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Concentration:
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Incubation Time:5 days
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Result:Showed IC50s of 0.47, 0.07, 0.12 and 0.07 nM against SK-MEL-239, HCT116, A549 and A375 cells, respectively.
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Cell Line:A549, HCT-116, A375 and SK-MEL-239
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Concentration:0.4, 0.8, 1.6, 3.1, 6.25, 12.5, 25 and 50 nM
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Incubation Time:1 h
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Result:Inhibited the expression of pERK. And the effect was better than Trametinib.
Chemical Information
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CAS No. 2666940-97-0
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Appearance Solid
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Masse moléculaire 666.46
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Formule C25H24FIN6O5S
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Color White to light yellow
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SMILES
O=C1C2=C(N(C)C(C(C)=C2N(C3=CC(NS(=O)(NC)=O)=CC=C3)C(N1C4CC4)=O)=O)NC5=CC=C(C=C5F)I
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Cancer
The MEK-RAF molecular glue IK-595 has potent antitumor activity across RAS/MAPK pathway-altered cancers. [Abstract]2026 Jan;7(1):116-130. PMID: 41482524
Solvant et solubilité
DMSO : 100 mg/mL (150.05 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 (3.75 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.
Pureté et documentation
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Fiche technique (280 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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Instruction de manipulation (2659 KB)
Références
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 | 1.5005 mL | 7.5023 mL | 15.0047 mL | 37.5116 mL |
| 5 mM | 0.3001 mL | 1.5005 mL | 3.0009 mL | 7.5023 mL | |
| 10 mM | 0.1500 mL | 0.7502 mL | 1.5005 mL | 3.7512 mL | |
| 15 mM | 0.1000 mL | 0.5002 mL | 1.0003 mL | 2.5008 mL | |
| 20 mM | 0.0750 mL | 0.3751 mL | 0.7502 mL | 1.8756 mL | |
| 25 mM | 0.0600 mL | 0.3001 mL | 0.6002 mL | 1.5005 mL | |
| 30 mM | 0.0500 mL | 0.2501 mL | 0.5002 mL | 1.2504 mL | |
| 40 mM | 0.0375 mL | 0.1876 mL | 0.3751 mL | 0.9378 mL | |
| 50 mM | 0.0300 mL | 0.1500 mL | 0.3001 mL | 0.7502 mL | |
| 60 mM | 0.0250 mL | 0.1250 mL | 0.2501 mL | 0.6252 mL | |
| 80 mM | 0.0188 mL | 0.0938 mL | 0.1876 mL | 0.4689 mL | |
| 100 mM | 0.0150 mL | 0.0750 mL | 0.1500 mL | 0.3751 mL |
Trametiglue Related Classifications
HY-153181 Related Classifications
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