Chemical Structure : XYD129
CAS No.:
XYD129
(XYD 129, XYD-129)
Catalog No.: PC-22486Not For Human Use, Lab Use Only.
XYD129 is a highly potent and selective CBP/p300 degrader with IC50 of 21/30 nM, effectively degrades CBP/p300 proteins and exhibits potent inhibition of growth in acute leukemia cell lines (MOLM-16, IC50=7.4 nM).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
XYD129 is a highly potent and selective CBP/p300 degrader with IC50 of 21/30 nM, effectively degrades CBP/p300 proteins and exhibits potent inhibition of growth in acute leukemia cell lines (MOLM-16, IC50=7.4 nM).
XYD129 can effectively induce the formation of CBP/p300-PROTAC-CRBN.
XYD129 at 1000 nM for 24 h is almost completely depletion of CBP and p300 proteins in MOLM-16 cells.
XYD129 is dependent on the ubiquitin-proteasome system (UPS) and involves the binding of the degraders to CBP/p300 and CRBN.
XYD129 (30 mg/kg) once daily via intraperitoneal injection for 2 weeks suppresses the tumor growth in vivo in MOLM-16 xenograft NOD-SCID mouse model.
Physicochemical Properties
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M.Wt
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806.81
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Formula
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C41H39FN8O9
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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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3-Acetyl-7-(2-((4-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)butyl)amino)-2-oxoethoxy)-N-(2-fluoro-5-(hydroxymethyl)-3-(1-methyl-1H-pyrazol-4-yl)phenyl)indolizine-1-carboxamide
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References
1. Tianbang Wu, et al. J Med Chem. 2024 Jun 13;67(11):9194-9213.
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