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EGFR-IN-21

Names

[ CAS No. ]:
2648206-31-7

[ Name ]:
EGFR-IN-21

Biological Activity

[Description]:

EGFR-IN-21 is a potent EGFR inhibtior with an IC50 of 0.38 nM. EGFR-IN-21 has antitumor activity[1].

[Related Catalog]:

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

[Target]

EGFR:0.38 nM (IC50)


[In Vitro]

EGFR-IN-21 inhibits HEK293T cells (IC50=951.51 nM) and PC9 EGFR-Del19/T790M/C797S cells (IC50=135.11 nM)[1].

[In Vivo]

EGFR-IN-21 (1 mg/kg; IV) has a T1/2 of 3.33 hours, and a Vss of 0.374 L/kg for female CD-1 mouse[1]. EGFR-IN-21 (5 mg/kg;po) has a T1/2 of 3.13 hours, a Cmax of 2077 ng/ml and an AUC of 7542 h·ng/ml[1].

[References]

[1]. Lei Liu, et al. Polyaryl compounds as EGFR kinase inhibitors. WO2021104441.

Chemical & Physical Properties

[ Molecular Formula ]:
C36H44BrN10O2P

[ Molecular Weight ]:
759.68


Related Compounds