GNE-8025 (GNE8025)

Chemical Structure : GNE-8025

CAS No.: 2933893-27-5

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货号: PC-27128Not For Human Use, Lab Use Only.

GNE-8025 is a potent, selective, covalent pan-TEAD inhibitor, disrupts YAP-TEAD interaction with biochemical IC50s of 5/8/326/37 nM for TEAD1/2/3/4 in TR-FRET assays.

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2 mg	￥3980	In stock
5 mg	￥5980	In stock
10 mg	￥8980	In stock
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100 mg		Get quote

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生物&药学活性

GNE-8025 is a potent, selective, covalent pan-TEAD inhibitor, disrupts YAP-TEAD interaction with biochemical IC50s of 5/8/326/37 nM for TEAD1/2/3/4 in TR-FRET assays.
GNE-8025 bind potently and covalently to the lipid pocket of TEAD proteins, form a covalent linkage with the lipid pocket cysteine (C380) of TEAD2 through the acrylamide warhead.
GNE-8025 exhibits strong activity against all four isoforms of TEAD1/2/4, with the exception of TEAD3.
GNE-8025 potently inhibits cell proliferation of Hippo-driven cell lines NCI-H226 and MSTO-211H with EC50 of 7 nM and 22 nM, but not Hippo-independent VMRC-LCD cells with >2500-fold higher EC50 values.
GNE-8025 shows superior efficacy in both NCI-H226 and MSTO-211H cells versus GNE-6915 and GNE-7883, downregulates YAP/TAZ–TEAD-dependent gene programs to exert anti-proliferative effects.
GNE-8025 potently inhibits the proliferation of Hippo deregulated cells and reinforces mesothelioma as a malignancy where TEAD inhibitors are effective at impeding cancer cell proliferation.
GNE-8025 enhances the efficacy of targeted cancer therapies, particularly when combined with inhibitors of RTKs and the RAS/MAPK pathway.
GNE-8025 (10 mg/kg BID) significantly impacted tumor growth inhibition in NCI-H226 xenograft model.

物理化学性质&存储条件

分子量	422.36
分子式	C19H17F3N4O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-N-((4-(1,2-dihydroxyethyl)-1-(4-(trifluoromethoxy)phenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)methyl)acrylamide

参考文献

1. Hagenbeek TJ, et al. Nat Commun. 2026 Jun 27. doi: 10.1038/s41467-026-74722-5.

GNE-8025 (GNE8025)

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物理化学性质&存储条件

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GNE-8025 (GNE8025)

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物理化学性质&存储条件

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