2459932-81-9

2459932-81-9 structure
2459932-81-9 structure
  • Name: EGFR-IN-49
  • Chemical Name: EGFR-IN-49
  • CAS Number: 2459932-81-9
  • Molecular Formula: C22H15N5O2S
  • Molecular Weight: 413.45
  • Catalog: Signaling Pathways JAK/STAT Signaling EGFR
  • Create Date: 2022-07-19 22:15:43
  • Modify Date: 2024-01-11 14:04:51
  • 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].

Name EGFR-IN-49
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
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.

Molecular Formula C22H15N5O2S
Molecular Weight 413.45