Chemical Structure : XYD049
CAS No.:
3006788-11-7
XYD049
(XYD-049)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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811.66
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Formula
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C35H35BrN6O10S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Shen H, et al. J Med Chem. 2025 Jan 2. doi: 10.1021/acs.jmedchem.4c02205.
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