XM-U-14

Chemical Structure : XM-U-14

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货号: PC-22785Not For Human Use, Lab Use Only.

XM-U-14 is a highly potent, selective and efficacious USP7 PROTAC degrader with DC50 of 0.7 nM in RS4;11 cell, Dmax of 93.1%.

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生物&药学活性

XM-U-14 is a highly potent, selective and efficacious USP7 PROTAC degrader with DC50 of 0.7 nM in RS4;11 cell, Dmax of 93.1%.
XM-U-14 significantly upregulated the levels of p53 and p21 in a time and dose-dependent manner.
XM-U-14 showed significant cell growth inhibition with IC50 values of 0.5 nM and 8.3 nM in RS4;11 cells and Reh cells, respectively.
XM-U-14 (1, 10, 100, and 1000 nM) induced apoptosis and cycle arrest in RS4;11 cells.
XM-U-14 (5, 10 mg/kg and 20 mg/kg for 18 days) significantly decreased the levels of USP7 protein in the RS4;11 tumor tissue, exhibited effective tumor growth inhibition in the RS4;11 xenograft tumor model.

物理化学性质&存储条件

分子量	1064.32
分子式	C58H69N11O7S
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,4R)-4-Hydroxy-1-((R)-2-(3-(4-(4-(6-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-7-oxo-6,7-dihydro-2H-pyrazolo[4,3-d]pyrimidin-3-yl)benzyl)piperazin-1-yl)isoxazol-5-yl)-3-methylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

参考文献

1. Miaomiao Xu, et al. J Med Chem. 2024 Jul 19. doi: 10.1021/acs.jmedchem.4c01134.

XM-U-14

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XM-U-14

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