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EGFR-IN-60

CAT: 0804-HY-147826Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-147826Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation (IC50=1.32 μM) over A431 cells overexpressing EGFRWT (IC50=4.96 μM) . EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio[1].
CAS Number
2699877-43-3
UNSPSC
12352005
Target
Apoptosis; EGFR
Type
Reference compound
Related Pathways
Apoptosis; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/egfr-in-60.html
Solubility
10 mM in DMSO
Smiles
O=C1C2=C(NC(N=CN(/N=C/C3=CC=C(N(C)C)C=C3)C4=N)=C4C2C5=CC=CC(Cl)=C5Cl)CC(C)(C)C1
Molecular Formula
C28H28Cl2N6O
Molecular Weight
535.47
References & Citations
[1]Mennatallah A Shaheen, et al. Design, synthesis and biological evaluation of new series of hexahydroquinoline and fused quinoline derivatives as potent inhibitors of wild-type EGFR and mutant EGFR (L858R and T790M) . Bioorg Chem. 2020 Dec;105:104274.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EGFR/ErbB1/HER1; JAK3

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