Trametiglue - ≥98% , CAS No.2666940-97-0

CAS: 2666940-97-0 Cat. No.: T649478 Peso molecular: 666.46

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

Trametiglue, a derivative of Trametinib , targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions

In Vitro

Trametiglue retains the strong binding potency and residence time of Trametinib on KSR-bound MEK. Trametiglue, unlike Trametinib but similar to Avutometinib , 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:Solid

IC50& Target:MEK1 MEK2

Specifications

Especificaciones y pureza

≥98%

Mecanismos bioquímicos y fisiológicos

Trametiglue, a derivative of Trametinib ( HY-10999 ), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions.

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Pureza

≥98%

Nombres e identificadores

• Sonrisas canónicas: O=C1C2=C(N(C)C(C(C)=C2N(C3=CC(NS(=O)(NC)=O)=CC=C3)C(N1C4CC4)=O)=O)NC5=CC=C(C=C5F)I
• Peso molecular: 666.46

Propiedades químicas y físicas

• Solubilidad: DMSO : 100 mg/mL (150.05 mM; ultrasonic and warming and heat to 60°C)