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BAY-293

BAY-293
Clinical data
Drug classSOS1 inhibitor
Identifiers
  • 6,7-dimethoxy-2-methyl-N-[(1R)-1-[4-[2-(methylaminomethyl)phenyl]thiophen-2-yl]ethyl]quinazolin-4-amine
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEBI
ChEMBL
PDB ligand
Chemical and physical data
FormulaC25H28N4O2S
Molar mass448.59 g·mol−1
3D model (JSmol)
  • CC1=NC2=CC(=C(C=C2C(=N1)N[C@H](C)C3=CC(=CS3)C4=CC=CC=C4CNC)OC)OC
  • InChI=1S/C25H28N4O2S/c1-15(24-10-18(14-32-24)19-9-7-6-8-17(19)13-26-3)27-25-20-11-22(30-4)23(31-5)12-21(20)28-16(2)29-25/h6-12,14-15,26H,13H2,1-5H3,(H,27,28,29)/t15-/m1/s1
  • Key:WEGLOYDTDILXDA-OAHLLOKOSA-N

BAY-293 is the first drug reported to act as an inhibitor of the guanine nucleotide exchange factor protein SOS1. It acts by preventing SOS1 from binding to its target protein KRAS. It has potential applications in the treatment of cancer, and has been widely used in cancer research.[1][2][3][4][5]

See also

References

  1. ^ Hillig RC, Sautier B, Schroeder J, Moosmayer D, Hilpmann A, Stegmann CM, et al. (February 2019). "Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction". Proceedings of the National Academy of Sciences of the United States of America. 116 (7): 2551–2560. Bibcode:2019PNAS..116.2551H. doi:10.1073/pnas.1812963116. PMC 6377443. PMID 30683722.
  2. ^ Wang CX, Wang TT, Zhang KD, Li MY, Shen QC, Lu SY, et al. (October 2022). "Pan-KRAS inhibitors suppress proliferation through feedback regulation in pancreatic ductal adenocarcinoma". Acta Pharmacologica Sinica. 43 (10): 2696–2708. doi:10.1038/s41401-022-00897-4. PMC 9525295. PMID 35352018.
  3. ^ Hamilton G, Stickler S, Rath B (2023). "Integration of signaling pathway and bromodomain and extra-terminal domain inhibition for the treatment of mutant Kirsten rat sarcoma viral oncogene homolog cancer". Exploration of Targeted Anti-Tumor Therapy. 4 (5): 1027–1038. doi:10.37349/etat.2023.00178. PMC 10651355. PMID 38023987.
  4. ^ Bruggemann L, Falls Z, Mangione W, Schwartz SA, Battaglia S, Aalinkeel R, et al. (January 2023). "Multiscale Analysis and Validation of Effective Drug Combinations Targeting Driver KRAS Mutations in Non-Small Cell Lung Cancer". International Journal of Molecular Sciences. 24 (2): 997. doi:10.3390/ijms24020997. PMC 9867122. PMID 36674513.
  5. ^ Mannino D, Basilotta R, De Luca F, Casili G, Esposito E, Paterniti I (March 2025). "KRAS-SOS-1 Inhibition as New Pharmacological Target to Counteract Anaplastic Thyroid Carcinoma (ATC)". International Journal of Molecular Sciences. 26 (6): 2579. doi:10.3390/ijms26062579. PMC 11942110. PMID 40141222.

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