Trametiglue, a derivative of Trametinib ( HY-10999 ), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactionsIn VitroTrametiglue retains the strong binding potency and residence time of Trametinib on KSR-bound MEK. Trametiglue, unlike Trametinib but similar to Avutometinib (HY-18652), enhances interactions between endogenous BRAF and MEK1. 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. Trametiglue (5 days) inhibits HCT116, A375, A549 and SK-MEL-239 cells viability with IC 50 s of 0.07, 0.07, 0.12 and 0.47 nM, respectively. Trametiglue (10 nM; 10 days) inhibits colony formation in KRAS-mutant and BRAF-mutant cancer cell lines with higher potency than Trametinib. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: SK-MEL-239, HCT116, A549 and A375 Concentration: Incubation Time: 5 days Result: Showed IC 50 s of 0.47, 0.07, 0.12 and 0.07 nM against SK-MEL-239, HCT116, A549 and A375 cells, respectively. Western Blot AnalysisCell 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.Form:SolidIC50& Target:MEK1 MEK2. Specification: 0.98 Molecular Formula: C25H24FIN6O5S Molecular Weight: 666.46
- UPC:
- 51171983
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- T649478-10mg
- CAS:
- 2666940-97-0
- Product Size:
- 10mg
