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首页-抗体药物偶连体和PROTACs-PROTAC-YB-3-17
YB-3-17

Chemical Structure : YB-3-17

CAS No.: 2940242-88-4

YB-3-17

货号: PC-23566Not For Human Use, Lab Use Only.

YB-3-17 is a potent dual-target, dual-mechanism molecule, robustly inhibits mTOR (IC50=0.22 nM) and selectively degrades GSPT1 (DC50=5 nM, U87 cells).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

YB-3-17 is a potent dual-target, dual-mechanism molecule, robustly inhibits mTOR (IC50=0.22 nM) and selectively degrades GSPT1 (DC50=5 nM, U87 cells).
YB-3-17 significantly inhibited the phosphorylation of S6K and 4EBP1 proteins in U87 cells in concentration- and time-dependent manners, also downregulates phosphorylation of the AKT protein.
YB-3-17 efficiently inhibited the proliferation of various glioblastoma cells, achieving IC50 values as low as 3.3 nM.
YB-3-17 significantly degrades only GSPT1 without affecting other intracellular proteins, does not inhibit off-targets such as FGR, CSF1R (FMS), LCK, and LYNa.
YB-3-17 not only significantly outperforms the inhibitor MLN0128 in tumor suppression activity, demonstrating a more robust anticancer effect, but also exhibits superior safety.

物理化学性质&存储条件

分子量 745.80
分子式 C38H39N11O6
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

5-(((4-(4-(4-amino-3-(2-aminobenzo[d]oxazol-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)cyclohexyl)methyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

参考文献

1. Liu Y, et al. J Am Chem Soc. 2024 Dec 2. doi: 10.1021/jacs.4c11930.

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