pan-HER-IN-1

Names

[ CAS No. ]:
1639040-94-0

[ Name ]:
pan-HER-IN-1

Biological Activity

[Description]:

pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC50 values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFRT790M/L858R and HER2, respectively. pan-HER-IN-1 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:0.38 nM (IC50)

HER4:1.6 nM (IC50)

EGFRL858R/T790M/C797S:2.2 nM (IC50)

HER2:3.5 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 ]:
C19H14BrN5O

[ Molecular Weight ]:
408.25

Related Compounds