EGFR-IN-48
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].
Product Specifications
CAS Number
2882851-77-4
UNSPSC
12352005
Target
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/egfr-in-48.html
Solubility
10 mM in DMSO
Smiles
CCC1=CC(NC2=NC=C(C(NC3=CC=C4N=CC=NC4=C3P(C)(C)=O)=N2)Br)=C(C=C1N5CCC(CC5)N6CCN(CC6)CCS(C)(=O)=O)OC
Molecular Formula
C35H47BrN9O4PS
Molecular Weight
800.75
References & Citations
[1]Fang H, et al. Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S) . Bioorg Med Chem Lett. 2022; 9:128729.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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