Chemical Structure : MD-4251
CAS No.:
MD-4251
(MD4251)
Catalog No.: 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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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883.89
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Formula
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C47H53Cl2FN8O4
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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'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
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References
1. Acharyya RK, et al.J Med Chem. 2025 Jul 10;68(13):13249-13267.
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