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MD-265

Chemical Structure : MD-265

CAS No.: 2415160-21-1

MD-265 (MD265)

Catalog No.: PC-23385Not For Human Use, Lab Use Only.

MD-265 is a potent PROTAC MDM2 degrader, potently inhibits RS4;11 cell line with IC50 of 0.7 nM, induces strong p53 activation in cancer cells carrying wild-type p53.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

MD-265 is a potent PROTAC MDM2 degrader, potently inhibits RS4;11 cell line with IC50 of 0.7 nM, induces strong p53 activation in cancer cells carrying wild-type p53.
MD-265 potently inhibited cell growth and achieved IC50 values of 0.9 nM to 212 nM in acute leukemia cell lines carrying a wild-type p53.
MD-265 is a potent MDM2 degrader and is >200 times more potent than MI-1063 in cell growth inhibition in the RS4;11 cell line.
MD-265 demonstrated no activity in cancer cells harboring mutated p53.
MD-265 achieved complete and persistent tumor regression in the RS4;11 xenograft model without causing any signs of toxicity.

Physicochemical Properties

M.Wt 921.89
Formula C50H51Cl2FN6O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)ethynyl)piperidine-1-carbonyl)cyclohexyl)-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-indoline]-5'-carboxamide

References

1. Aguilar A, et al. J Med Chem. 2024 Oct 31. doi: 10.1021/acs.jmedchem.4c01818.

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