GNE-7883

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].

Product Specifications

CAS Number

[2648450-42-2]

UNSPSC

12352005

Target

YAP

Type

Reference compound

Related Pathways

Stem Cell/Wnt

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gne-7883.html

Purity

99.54

Solubility

DMSO : 50 mg/mL (ultrasonic)

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

Molecular Formula

C28H29FN6O2

Molecular Weight

500.57

References & Citations

[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.|[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.