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首页-抗体药物偶连体和PROTACs-PROTAC-XYD129
XYD129

Chemical Structure : XYD129

CAS No.:

XYD129 (XYD 129, XYD-129)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 806.81
分子式 C41H39FN8O9
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-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 

参考文献

1. Tianbang Wu, et al. J Med Chem. 2024 Jun 13;67(11):9194-9213.

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