2719667-13-5
2719667-13-5
Chemical Structure
GNE-0749
- CAS No.: 2719667-13-5
- Formula:C23H27F2N5O2
- Molecular Weight:443.49
InChIKey: LERFSNRPSMKJCV-UHFFFAOYSA-N
SMILES: CC1=CC(F)=C(C=C1NC2=CC=C3N=CN(C(C3=C2F)=O)C)NC(NCCC(C)(C)C)=O
Biological Activity: GNE-0749 is an orally active pan-RAF inhibitor with a Ki value of 0.061 nM against CRAF. GNE-0749 inhibits RAF dimer signaling via a DFG-out/αC-helix-in binding mode, prevents paradoxical activation of the MAPK pathway, and suppresses downstream MEK/ERK/RSK signal transduction. GNE-0749 can be used in studies related to KRASG12C mutation-driven cancers[1][2][3].
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GNE-0749 | GNE-0749 is an orally active pan-RAF inhibitor with a Ki value of 0.061 nM against CRAF. GNE-0749 inhibits RAF dimer signaling via a DFG-out/αC-helix-in binding mode, prevents paradoxical activation of the MAPK pathway, and suppresses downstream MEK/ERK/RSK signal transduction. GNE-0749 can be used in studies related to KRASG12C mutation-driven cancers. | |||||||||||||||||||||
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References
- [1]. Huestis MP, et al. Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor. J Med Chem. 2021;64(7):3940-3955. [Content Brief]
- [2]. Harwood SJ, et al. Selected Approaches to Disrupting Protein-Protein Interactions within the MAPK/RAS Pathway. International journal of molecular sciences. 2023 Apr 17;24(8):7373. [Content Brief]
- [3]. Huestis MP, et al. Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor. ACS medicinal chemistry letters. 2021 May 13;12(5):791-797. [Content Brief]
