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Chemical Structure : GNE-7883
CAS No.: 2648450-42-2
Catalog No.: PC-20407Not For Human Use, Lab Use Only.
GNE-7883 (GNE7883) is a potent, reversible, allosteric inhibitor of the YAP1-TEAD interaction.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 1 mg | $188 | In stock | |
| 5 mg | $298 | In stock | |
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| 25 mg | Get quote | ||
| 100 mg | Get quote |
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GNE-7883 (GNE7883) is a potent, reversible, allosteric inhibitor of the YAP1-TEAD interaction.
The potent inhibition of pan-TEAD lipidation with GNE-7883 translated well to the disruption of YAP1 binding to each of the four TEAD isoforms by the YAP1 HTRF assay.
GNE-7883 potently inhibited proliferation of the OVCAR-8 and NCI-H226 cells, with EC50 values of 115 nM and 333 nM, respectively.
GNE-7883 (250 mg/kg, subcutaneous dosing) showed strong in vivo tumor growth inhibition (TGI) of 102% in the mesothelioma NCIH226 xenograft mouse model.
| M.Wt | 500.58 | |
| Formula | C28H29FN6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
5-(4-cyclohexylphenyl)-3-(3-(fluoromethyl)azetidine-1-carbonyl)-2-(3-methylpyrazin-2-yl)pyrazolo[1,5-a]pyrimidin-7(4H)-one |
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1. Jeffrey K Holden, et al. Cell Rep. 2020 Jun 23;31(12):107809.
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