EGFR-IN-49

Names

[ CAS No. ]:
2459932-81-9

[ Name ]:
EGFR-IN-49

Biological Activity

[Description]:

EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFRT790M and EGFRT790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner[1].

[Related Catalog]:

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

[Target]

EGFRT790M:65.0 nM (IC50)

EGFRL858R/T790M:13.6 nM (IC50)


[In Vitro]

EGFR-IN-49 (compound 13a) (1, 10 µM) shows inhibition activity for H1975 cells with an IC50 of 699.2 nM[1]. EGFR-IN-49 (1 µM) shows an strong inhibitory activity to EGFRT790M, EGFRT790M/L858R, EGFRWT with IC50s of 65.0, 13.6, >1000 nM, respectively[1]. EGFR-IN-49 (0.2, 4, 8 µM; 48 h) induces cell apoptosis in a dose-dependent manner in A431 cells[1]. Cell Proliferation Assay[1] Cell Line: A549, A431, Hela, MCF7, LO2 cells Concentration: 0-50 µM Incubation Time: Result: Showed excellent anti-proliferative activities with IC50s of 4.34, 3.79, 6.39, 18.99, >50 µM for A549, A431, Hela, MCF7, LO2 cells, respectively. Apoptosis Analysis[1] Cell Line: A431 cells Concentration: 0.2, 4, 8 µM Incubation Time: 48 h Result: Induced cell apoptosis in a low concentration (0.33 µM) and exhibited higher percent of 16.41% % in the stage of late apoptotic at concentration of 4 µM.

[References]

[1]. Xiao Z, et al. Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations. Eur J Med Chem. 2020 Oct 1;203:112511.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H15N5O2S

[ Molecular Weight ]:
413.45


Related Compounds

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