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首页-抗体药物偶连体和PROTACs-PROTAC-MD-224
MD-224

Chemical Structure : MD-224

CAS No.: 2136247-12-4

MD-224 (MD224)

货号: PC-49045Not For Human Use, Lab Use Only.

MD-224 is a small-molecule MDM2 degrader based on the proteolysis targeting chimera (PROTAC), effectively induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MD-224 is a small-molecule MDM2 degrader based on the proteolysis targeting chimera (PROTAC), effectively induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells.
MD-224 inhibits growth of RS4;11 cells with IC50 of 1.5 nM and low nanomolar IC50 values in a panel of leukemia cell lines.
MD-224 achieves complete and durable tumor regression in vivo in the RS4;11 xenograft tumor model in mice at well-tolerated dose schedules.

物理化学性质&存储条件

分子量 889.806
分子式 C48H43Cl2FN6O6
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'R,4'S,5'R)-6''-chloro-4'-(3-chloro-2-fluorophenyl)-N-(4-((5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pent-4-yn-1-yl)carbamoyl)phenyl)-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-indoline]-5'-carboxamide

参考文献

1. Yangbing Li, et al. J Med Chem. 2019 Jan 24;62(2):448-466.

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