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EGFR-IN-178

CAT: 0804-HY-178448Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-178448Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM) . EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC) [1].
UNSPSC
12352005
Target
Apoptosis; Cannabinoid Receptor; Caspase; EGFR; Ferroptosis; Glutathione Peroxidase; JAK; Reactive Oxygen Species (ROS)
Related Pathways
Apoptosis; Epigenetics; GPCR/G Protein; Immunology/Inflammation; JAK/STAT Signaling; Metabolic Enzyme/Protease; Neuronal Signaling; NF-κB; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Field of Research
Cancer; Inflammation/Immunology
Smiles
C=CC(NC1=C(C=C(C(NC2=NC(NC3=CN=CC=N3)=CC=N2)=C1)OC)N(CCN(C)C)C)=O
Molecular Formula
C23H29N9O2
Molecular Weight
463.54
References & Citations
[1]Yao H, et al. The synthesis and evaluation of new N- (pyrazin-2-yl) -4-aminopyrimidine derivatives targeted EGFR and JAK. Eur J Med Chem. 2025 Dec 15;300:118120.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Caspase 3; JAK2; JAK3

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