pan-HER-IN-2

Names

[ CAS No. ]:
1639040-95-1

[ Name ]:
pan-HER-IN-2

Biological Activity

[Description]:

pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFRT790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

EGFR:0.72 nM (IC50)

EGFR (L858R/T790M):8.2 nM (IC50)

HER2:75.1 nM (IC50)

HER4:2.0 nM (IC50)


[References]

[1]. Tang Q, et al. Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. Eur J Med Chem. 2022 Apr 5;233:114249.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H15BrClN5O

[ Molecular Weight ]:
444.71

Related Compounds

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