MS9427 TFA
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1107.50 |
| Molecular Formula | C50H59ClF4N8O14 |
| SMILES | O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC(NCCOCCOCCOCCOCCOCCC(N4CCN(CCCOC5=CC6=C(NC7=CC=C(F)C(Cl)=C7)N=CN=C6C=C5OC)CC4)=O)=C3)=O.OC(C(F)(F)F)=O |
Summary
MS9427 TFA is a potent PROTAC EGFR degrader with K d s of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer [1] .
In Vitro
MS9427 TFA has antiproliferative activity against HCC-827 cells, with a GI
50
of 0.87 ± 0.27 μM
[1]
.
MS9427 TFA (0-10 μM, 16 h) potently induces EGFR
Del19
degradation (DC
50
=82 ± 73 nM) and inhibits EGFR phosphorylation (p-EGFR) in a concentration-dependent manner in HCC-827 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | HCC-827 cells |
| Concentration: | 1, 10, 50, 100, 200, 500, 100, and 10000 nM |
| Incubation Time: | 16 h |
| Result: | Inhibited EGFR phosphorylation (p-EGFR) in a concentration-dependent manner in HCC-827 cells. |
Western Blot Analysis [1]
| Cell Line: | HCC-827 cells |
| Concentration: | 100 nM |
| Incubation Time: | 1, 2, 4, 6, 12, 24, 48 h |
| Result: | Induced EGFR degradation in a time-dependent manner and through the UPS and autophagy/lysosome system. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
