2648450-42-2
Chemical Structure
GNE-7883
- CAS No.: 2648450-42-2
- Formula:C28H29FN6O2
- Molecular Weight:500.57
IUPAC Name: 5-(4-cyclohexylphenyl)-3-(3-(fluoromethyl)azetidine-1-carbonyl)-2-(3-methylpyrazin-2-yl)pyrazolo[1,5-a]pyrimidin-7(4H)-one
InChIKey: UNRTVIQQMJRQLZ-UHFFFAOYSA-N
SMILES: O=C(C=C(C1=CC=C(C2CCCCC2)C=C1)N3)N4C3=C(C(N5CC(CF)C5)=O)C(C6=NC=CN=C6C)=N4
Biological Activity: GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation[1][2][3].
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GNE-7883 | 99.54% | GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation. | ||||||||||||||||||||
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- [1]. Hagenbeek TJ, et al. An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance. Nat Cancer. 2023 Jun;4(6):812-828. [Content Brief]
- [2]. McGee L E. YAP Signaling Promotes Resistance to MEK Inhibition in NF1-Related MPNSTs[M]. Van Andel Research Institute, 2023.
- [3]. Barry E R, et al. Recent therapeutic approaches to modulate the Hippo pathway in oncology and regenerative medicine[J]. Cells, 2021, 10(10): 2715. [Content Brief]
Keywords
