Chemical Name: N-(3-(3-Cyclopropyl-5-((2-fluoro-4-iodophenyl)amino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H-yl)phenyl)methylaminosulfonamide. Alternate Names: APS-9-95-1
MEK inhibitor / molecular glue
Molekulargewicht:
666.47
Reinheit:
>98% by TLC NMR (Conforms)
Formulierung:
Off-white solid
CAS Nummer:
[2666940-97-0]
Formel:
C25H24FIN6O5S
Anwendungsbeschreibung:
Trametiglue is a trametinib analog that inhibits both KSR- and RAF-bound MEK and limits adaptive resistance seen with trametinib via enhanced interfacial binding. Displays significantly enhanced inhibition of RAS/ERK signaling versus trametinib is various cell lines with mutant KRAS and BRAF: IC50s/cell line - SK-MEL-239/0.47 nM, HCT116/0.07 nM, A549/0.12 nM, A375/0.07 nM. A molecular glue that is strongly selective towards MEK with no direct interaction with BRAF or CRAF.
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