Trametiglue | MEK inhibitor/molecular glue

CAS:
 2666940-97-0
Catalog Number:
 10-3961

Available Options

Size:PriceQuantity 
5 mg$100.00
25 mg$375.00

Trametiglue (2666940-97-0) 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: IC50’s/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.

References/Citations:

  1. Khan et al. (2020), Structural basis for the action of the drug trametinib at KSR-bound MEK; Nature 588 509
CAS:
2666940-97-0
Catalog Number:
10-3961
Activity:
MEK inhibitor/molecular glue
Chemical Names:
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 Name:
APS-9-95-1
Molecular Weight:
666.47
Molecular Formula:

C25H24FIN6O5S

Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white solid
Purity:

>98% TLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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