Chemistry:BI-3406

From HandWiki

BI-3406 is a drug that acts as an inhibitor of the guanine nucleotide exchange factor protein SOS1, and prevents it from binding to its target protein KRAS. It has potential applications in the treatment of cancer, and has been widely used in cancer research either in combination with other drugs or as a lead compound for the development of related compounds.[1][2][3][4][5][6][7]

See also

  • BAY-293

References

  1. ↑ "One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS". Journal of Medicinal Chemistry 64 (10): 6569–6580. May 2021. doi:10.1021/acs.jmedchem.0c01949. PMID 33719426. 
  2. ↑ "Targeting Son of Sevenless 1: The pacemaker of KRAS". Current Opinion in Chemical Biology 62: 109–118. June 2021. doi:10.1016/j.cbpa.2021.02.014. PMID 33848766. 
  3. ↑ "Inhibition of KRAS, MEK and PI3K Demonstrate Synergistic Anti-Tumor Effects in Pancreatic Ductal Adenocarcinoma Cell Lines". Cancers 14 (18): 4467. September 2022. doi:10.3390/cancers14184467. PMID 36139627. 
  4. ↑ "SOS1 and KSR1 modulate MEK inhibitor responsiveness to target resistant cell populations based on PI3K and KRAS mutation status". Proceedings of the National Academy of Sciences of the United States of America 120 (47). November 2023. doi:10.1073/pnas.2313137120. PMID 37972068. Bibcode: 2023PNAS..12013137D. 
  5. ↑ "Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras". Current Pharmaceutical Design 29 (22): 1741–1746. 2023. doi:10.2174/1381612829666230418114520. PMID 37073657. 
  6. ↑ "Co-targeting SOS1 enhances the antitumor effects of KRASG12C inhibitors by addressing intrinsic and acquired resistance". Nature Cancer 5 (9): 1352–1370. September 2024. doi:10.1038/s43018-024-00800-6. PMID 39103541. 
  7. ↑ "SOS1 inhibitor BI-3406 shows in vivo antitumor activity akin to genetic ablation and synergizes with a KRASG12D inhibitor in KRAS LUAD". Proceedings of the National Academy of Sciences of the United States of America 122 (11). March 2025. doi:10.1073/pnas.2422943122. PMID 40073053. Bibcode: 2025PNAS..12222943B. 



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