2044508-48-5

2044508-48-5 structure
2044508-48-5 structure
  • Name: EGFR-IN-50
  • Chemical Name: EGFR-IN-50
  • CAS Number: 2044508-48-5
  • Molecular Formula: C24H26BrN3O4S2
  • Molecular Weight: 564.51
  • Catalog: Signaling Pathways JAK/STAT Signaling EGFR
  • Create Date: 2022-10-23 12:52:06
  • Modify Date: 2024-01-02 10:06:35
  • EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells[1].

Name EGFR-IN-50
Description EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells[1].
Related Catalog
In Vitro EGFR-IN-50 (0-10 μM; 72 h) selectively inhibits NSCLC cell line H3255 (expressing EGFR-L858R) compared to other tumor cells[1]. EGFR-IN-50 (1-10 μM; 72 h) induces cell cycle arrest in G0-G1 phase[1]. EGFR-IN-50 (0.039-10 μM; 4 h) inhibits the phosphorylation of EGFR in H3255 cells[1]. Cell Proliferation Assay[1] Cell Line: A549, H3255, HepG2, MCF-7, HT-29 and A431 cells Concentration: 0-10 μM Incubation Time: 72 hours Result: Showed GI50 values of >10, and 0.7873 μM for A549 and H3255 cells, respectively. Showed IC50 values of >10, 7.309, >10 and 6.703 μM for HepG2, MCF-7, HT-29 and A431 cells, respectively. Cell Cycle Analysis[1] Cell Line: H3255 cells Concentration: 1, 5, and 10 μM Incubation Time: 72 hours Result: Increased the percentage of H3255 cells in G0-G1 phase from 60.32% to 88.61%. Western Blot Analysis[1] Cell Line: H3255 cells Concentration: 0.039, 0.15, 0.62, 2.5, and 10 μM Incubation Time: 4 hours Result: Inhibited the phosphorylation of EGFR in H3255 cells in a dose-dependent manner.
References

[1]. You-Guang Zheng, et al. Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H2S) donors as potent EGFR inhibitors against L858R resistance mutation. Eur J Med Chem. 2020 Sep 15;202:112522.

Molecular Formula C24H26BrN3O4S2
Molecular Weight 564.51