GNE-7883


CAS No. : 2648450-42-2

2648450-42-2
Price and Availability of CAS No. : 2648450-42-2
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1mg $144 In-stock
5mg $360 In-stock
10mg $580 In-stock
50mg $1250 In-stock
100mg $1750 In-stock
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Cat. No. : HY-147214
M.Wt: 500.57
Formula: C28H29FN6O2
Purity: >98 %
Solubility: DMSO : 50 mg/mL (ultrasonic)
Introduction of 2648450-42-2 :

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]. IC50 & Target:TEAD[1]. In Vitro:GNE-7883 exhibits strong dose-dependent antiproliferative effects in both OVCAR-8 and NCI-H226 cells, with EC50 values ​​of 115 nM and 333 nM, respectively[3].
In Vivo:GNE-7883 (100 and 250 mg/kg; s.c.; once daily for 4 days) induces tumor growth arrest in NCI-H226 xenograft mice and tumor regression in MSTO-211H xenograft mice[1].

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