| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
MEK1 MEK2
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|---|---|
| ln Vitro |
On KSR-bound MEK, trametiglue preserves trametinib's potent binding ability and residence duration [1]. In contrast to trametinib, but akin to avitometinib, trametiglue improves the relationship between endogenous BRAF and MEK1 [1]. Direct binding tests show that metetipleniglue (1 μM) is very selective for MEK1 and MEK2. Trametiglue exhibits a high degree of selectivity when it comes to a class of active kinases that either directly phosphorylate MEK1 or MEK2 substrates or prevent upstream kinases from doing so [1]. HCT116, A375, A549, and SK-MEL-239 cells' viability is inhibited by metamiglue (5 days) with IC50 values of 0.07, 0.07, 0.12, and 0.47 nM, respectively[1]. More potently than trametinib, trametiglue (10 nM; 10 days) suppresses the development of colonies in cancer cells with mutant BRAF and KRAS [1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: SK-MEL-239, HCT116, A549 and A375 Tested Concentrations: Incubation Duration: 5 days Experimental Results: demonstrated 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 Types: A549, HCT-116, A375 and SK-MEL-239 Tested Concentrations: 0.4, 0.8, 1.6, 3.1, 6.25, 12.5, 25 and 50 nM Incubation Duration: 1 h Experimental Results: Inhibited the expression of pERK. And the effect was better than Trametinib. |
| References |
| Molecular Formula |
C25H24FIN6O5S
|
|---|---|
| Molecular Weight |
666.463139533997
|
| Exact Mass |
666.055
|
| CAS # |
2666940-97-0
|
| PubChem CID |
154700547
|
| Appearance |
White to light yellow solid powder
|
| LogP |
2.9
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
39
|
| Complexity |
1230
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(NC1=CC=CC(N2C3=C(C)C(=O)N(C)C(NC4=CC=C(I)C=C4F)=C3C(=O)N(C3CC3)C2=O)=C1)(NC)(=O)=O
|
| InChi Key |
DNNMBAWCLGMMRJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C25H24FIN6O5S/c1-13-21-20(22(31(3)23(13)34)29-19-10-7-14(27)11-18(19)26)24(35)33(16-8-9-16)25(36)32(21)17-6-4-5-15(12-17)30-39(37,38)28-2/h4-7,10-12,16,28-30H,8-9H2,1-3H3
|
| Chemical Name |
3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-1-[3-(methylsulfamoylamino)phenyl]pyrido[4,3-d]pyrimidine-2,4,7-trione
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (150.05 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1500 mL | 0.7502 mL | 1.5005 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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