EAI045
EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.
Product Specifications
CAS Number
[1942114-09-1]
UNSPSC
12352005
Hazard Statement
H302, H312, H332
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/EAI045.html
Purity
99.06
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(C(C1=C(O)C=CC(F)=C1)N2C(C(C=CC=C3)=C3C2)=O)NC4=NC=CS4
Molecular Formula
C19H14FN3O3S
Molecular Weight
383.40
Precautions
H302, H312, H332
References & Citations
[1]Jia Y, et al. Overcoming EGFR (T790M) and EGFR (C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534 (7605) :129-32.|[2]Wang S, et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Lett. 2017 Jan 28;385:51-54.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EGFR/ErbB1/HER1
Available Sizes
Curated Selection
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