XYD049 | GSPT1 degrader | Probechem Biochemicals

Chemical Structure : XYD049

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XYD049 (XYD-049)

货号: PC-23795Not For Human Use, Lab Use Only.

XYD049 is a potent, selective CRBN-interacting molecular glue degrader of G1 to S phase transition 1 (GSPT1) with DC50 of 19 nM in 22Rv1 cells.

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生物&药学活性

XYD049 is a potent, selective CRBN-interacting molecular glue degrader of G1 to S phase transition 1 (GSPT1) with DC50 of 19 nM in 22Rv1 cells.
XYD049 selectively induced GSPT1 degradation among the well-known neo-substrates.
XYD049 effectively suppresses the growth of 22Rv1 cells with an IC50 value of 7 nM.
XYD049 downregulates GSPT1 by triggering its degradation through a CRBN- and proteasome-dependent pathway,
significantly suppressed the expression of AR-FL, AR-V7, PSA (also known as KLK3), and c-Myc at the mRNA level.
XYD049 (10-20 mg/kg dose, i.p.) demonstrates efficacy in inhibiting 22Rv1 tumor growth in mice.

物理化学性质&存储条件

分子量	811.66
分子式	C35H35BrN6O10S
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	2-((5-((5-Bromo-2-methoxyphenyl)sulfonamido)-3-methylbenzo[d]isoxazol-6-yl)oxy)-N-(5-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)pentyl)acetamide

参考文献

1. Shen H, et al. J Med Chem. 2025 Jan 2. doi: 10.1021/acs.jmedchem.4c02205.

XYD049 (XYD-049)

生物&药学活性

物理化学性质&存储条件

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XYD049 (XYD-049)

生物&药学活性

物理化学性质&存储条件

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