2. MAPK/ERK Pathway
  3. MEK
  4. Trametiglue

Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions.

For research use only. We do not sell to patients.

Trametiglue Chemical Structure

Trametiglue Chemical Structure

CAS No. : 2666940-97-0

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5 mg USD 400 In-stock
10 mg USD 680 In-stock
25 mg USD 1350 In-stock
50 mg USD 2200 In-stock
100 mg USD 3400 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Trametiglue Related Antibodies

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MEK1 MEK2 MEK5 MEK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions[1].

IC50 & Target[1]

MEK1

 

MEK2

 

In Vitro

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.

Trametiglue Related Antibodies

Cell Viability Assay[1]

Cell Line: SK-MEL-239, HCT116, A549 and A375
Concentration:
Incubation Time: 5 days
Result: Showed IC50s of 0.47, 0.07, 0.12 and 0.07 nM against SK-MEL-239, HCT116, A549 and A375 cells, respectively.

Western Blot Analysis[1]

Cell Line: A549, HCT-116, A375 and SK-MEL-239
Concentration: 0.4, 0.8, 1.6, 3.1, 6.25, 12.5, 25 and 50 nM
Incubation Time: 1 h
Result: Inhibited the expression of pERK. And the effect was better than Trametinib.
Molecular Weight

666.46

Formula

C25H24FIN6O5S
CAS No.
Appearance

Solid

Color

White to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5005 mL 7.5023 mL 15.0047 mL
5 mM 0.3001 mL 1.5005 mL 3.0009 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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 1.5005 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
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Trametiglue Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trametiglue2666940-97-0MEKMitogen-activated protein kinase kinaseMAPKKMAP2KTrametinibCH5126766AvutometinibSK-MEL-239HCT116A549A375pERKInhibitorinhibitorinhibit

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