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EGFR-IN-181

CAT: 0804-HY-178939Size: 1 EachDry Ice: NoHazardous: No
CAT#:0804-HY-178939Size:1 Each
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AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM) . EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK) . EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases[1].
UNSPSC
12352005
Target
Akt; Apoptosis; EGFR; PERK
Related Pathways
Apoptosis; Cell Cycle/DNA Damage; JAK/STAT Signaling; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK
Field of Research
Cancer; Neurological Disease
Smiles
CP(C)(C1=CC=CC=C1NC2=NC(NC3=CC4=C(N(CCN(C)C)C=C4)C=C3)=NC=C2Cl)=O
Molecular Formula
C24H28ClN6OP
Molecular Weight
482.95
References & Citations
[1]Zhao L, et al. Discovery of a brain-penetrant fourth-generation EGFR inhibitor to overcome the human triple (L858R/T790 M/C797S) mutation. Eur J Med Chem. 2025 Oct 14;302 (Pt 1) :118256.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Akt; EGFR/ErbB1/HER1

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