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CAS No. : 2666940-97-0
MCE 国际站:Trametiglue
产品活性:Trametiglue 是 Trametinib (HY-10999) 的衍生物,通过独特的界面结合相互作用,以前所未有的效力和选择性靶向 KSR-MEK 和 RAF-MEK。
研究领域:MAPK/ERK Pathway
作用靶点:MEK
In Vitro: Trametiglue 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 IC50s 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.
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