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首页-抗体药物偶连体和PROTACs-PROTAC-XYD113
XYD113

Chemical Structure : XYD113

CAS No.: 3032314-99-8

XYD113 (XYD-113)

货号: PC-27137Not For Human Use, Lab Use Only.

XYD113 is a potent and highly selective, orally bioavailable CRBN-dependent GSPT1 molecular glue degrader, exerts potent antiproliferative activity against 22Rv1 cells with IC50 of 69 nM, induces complete degradation of GSPT1 at 111 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

XYD113 is a potent and highly selective, orally bioavailable CRBN-dependent GSPT1 molecular glue degrader, exerts potent antiproliferative activity against 22Rv1 cells with IC50 of 69 nM, induces complete degradation of GSPT1 at 111 nM.
XYD113 exhibits significant antiproliferative activity (IC50 < 100 nM) against multiple MYC-overexpressing cancer cell lines (22Rv1, MV4-11, MOLM-16, Calu-1, HS-SY-II), and induces GSPT1 degradation in a dose- and time-dependent manner.
XYD113 at 1 uM for 6 h led to a complete degradation of GSPT1 in 22Rv1 cells.
XYD113 shows exceptional selectivity over SALL4, IKZF1/2/3, ZFP91, or CK1α.
XYD113 functions as a molecular glue to facilitate the formation of the CRBN-GSPT1 ternary complex, a rate-limiting step in targeted protein degradation via the UPS.
XYD113 (5 mg/kg, oral) suppresses tumor growth in a 22Rv1 xenograft model with a favorable safety profile.

物理化学性质&存储条件

分子量 428.87
分子式 C21H21ClN4O4
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

3-((3-(3-chloro-4-methylphenyl)ureido)methyl)-N-(2,6-dioxopiperidin-3-yl)benzamide

参考文献

1. Hui Shen, et al. Acta Pharmacol Sin. 2026 Jun 23. doi: 10.1038/s41401-026-01856-z.

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