MS154
MS154 is a first-in-class E3 ligase cereblon-recruited EGFR degrader with Kd values of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutant, respectively. MS154 potently induces degradation of mutant, but not wild-type, EGFR in cancer cell lines in an E3 ligase-dependent manner. MS154 exhibits anticancer effects against lung cancer (blue: E3 ligase ligand (HY-103596) ; black: linker (HY-W096167) ; pink: EGFR ligand (HY-168305) ) [1].
Product Specifications
CAS Number
[2550393-21-8]
UNSPSC
12352005
Target
EGFR; PROTACs
Type
Reference compound
Related Pathways
JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/ms154.html
Purity
99.71
Solubility
DMSO : 90.14 mg/mL (ultrasonic; warming)
Smiles
O=C1NC(C(CC1)N2C(C3=C(C2=O)C(OCCCCCCCCNC(CCN4CCN(CCCOC5=CC6=C(NC7=CC=C(C(Cl)=C7)F)N=CN=C6C=C5OC)CC4)=O)=CC=C3)=O)=O
Molecular Formula
C46H54ClFN8O8
Molecular Weight
901.42
References & Citations
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Cereblon; EGFR/ErbB1/HER1
Available Sizes
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