MD-4251 | MDM2 degrader | Probechem Biochemicals

Chemical Structure : MD-4251

加入收藏

MD-4251 (MD4251)

货号: PC-27523Not For Human Use, Lab Use Only.

MD-4251 is a potent, selective and orally efficacious MDM2 PROTAC degrader with DC50 of 0.2 nM in RS4;11 cells (Dmax=96% at 2 h), leading to robust p53 activation.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

MD-4251 is a potent, selective and orally efficacious MDM2 PROTAC degrader with DC50 of 0.2 nM in RS4;11 cells (Dmax=96% at 2 h), leading to robust p53 activation.
MD-4251 is potent in inhibition of cell growth in the RS4;11 cell line with IC50 of 1 nM.
MD-4251 is able to induce an increase of p53 protein by > 6-times at 3 nM or higher concentrations.
MD-4251 has no effect on the levels of GSPT1 and IKZF3 and only had a modest effect on IKZF1 and CK1α.
MD-4251 is ≥60-times more potent than APG-115 in inhibition of cell growth in these three leukemia cell lines.
MD-4251 induced robust upregulation of p53 protein (TP53 gene product), also increased the levels of three other proteins, namely DSC1 (Desmocollin-1), NBEA (neurobeachin), and CASP14 (Caspase-14) in the RS4;11 cells.
MD-4251 (3 and 10 mg/kg weekly oral administration) effectively inhibited tumor growth in RS4;11 xenograft tumor model.

物理化学性质&存储条件

分子量	883.89
分子式	C47H53Cl2FN8O4
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-((1r,4R)-4-((4-(3-(2,6-dioxopiperidin-3-yl)-1-methyl-1H-indazol-6-yl)piperazin-1-yl)methyl)cyclohexyl)-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-indoline]-5'-carboxamide O=C([C@H](N1)[C@H](C2=CC=CC(Cl)=C2F)[C@]3(C(NC4=C3C=CC(Cl)=C4)=O)C51CCCCC5)N[C@@H]6CC[C@@H](CN7CCN(C8=CC=C9C(N(C)N=C9C%10C(NC(CC%10)=O)=O)=C8)CC7)CC6

参考文献

1. Acharyya RK, et al.J Med Chem. 2025 Jul 10;68(13):13249-13267.

MD-4251 (MD4251)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

MD-4251 (MD4251)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.