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
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M.Wt
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921.89
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Formula
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C50H51Cl2FN6O6
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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-((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
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References
1. Aguilar A, et al. J Med Chem. 2024 Oct 31. doi: 10.1021/acs.jmedchem.4c01818.
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