TEAD PROTAC H122

Chemical Structure : TEAD PROTAC H122

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货号: PC-23735Not For Human Use, Lab Use Only.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

TEAD PROTAC H122 is a potent, selective TEAD PROTAC degrader with DC50 of 3.0 nM in MSTO-211H cells, shows TEAD1 binding affinity with Ki of 0.3 nM, promotes the degradation of TEAD1, TEAD3, and TEAD4 with similar potency.
H122 exhibits antiproliferative activity with IC50 of 21.3 and 0.6 nM for MSTO-211H and NCI-H226 cells respectively.
H122 exhibits high affinity for TEAD2, TEAD3, and TEAD4, as evidenced by Ki values that were all below 5 nM。
H122 significantly downregulated the expression of Myc target genes, as highlighted by GSEA analysis.
H122 exhibits robust antitumor efficacy in the MSTO-211H mouse xenograft model.

物理化学性质&存储条件

分子量	838.33
分子式	C45H45ClFN5O8
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	(2S)-2-((2S)-5-Chloro-2-(((2-(1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperidin-4-yl)ethyl)amino)methyl)-2-phenyl-2,3-dihydrobenzofuran-4-yl)-3-fluoro-4-(2-methoxyethoxy)benzamide

参考文献

1. Lu Y, et al. J Med Chem. 2025 Jan 13. doi: 10.1021/acs.jmedchem.4c02884.

TEAD PROTAC H122

生物&药学活性

物理化学性质&存储条件

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TEAD PROTAC H122

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