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AM-7209

Chemical Structure : AM-7209

CAS No.: 1623432-51-8

AM-7209 (AM 7209;AM7209)

Catalog No.: PC-60982Not For Human Use, Lab Use Only.

A potent and selective inhibitor of the MDM2-p53 interaction with Kd of 38 pM, and IC50 of 1.6 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent and selective inhibitor of the MDM2-p53 interaction with Kd of 38 pM, and IC50 of 1.6 nM; potently inhibits cell growth on-target in the tumor cell line with wild-type p53 cell with IC50 of 2 nM, exhibits >12,500-fold selectivity over those with p53-deficient cells; demonstrates remarkable pharmacokinetic properties and in vivo antitumor activity in both the SJSA-1 osteosarcoma xenograft model (ED50=2.6 mg/kg QD) and the HCT-116 colorectal carcinoma xenograft model (ED50=10 mg/kg QD).

Physicochemical Properties

M.Wt 747.7
Formula C37H41Cl2FN2O7S
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

4-(2-((3R,5R,6S)-1-((S)-2-(tert-Butylsulfonyl)-1-cyclopropylethyl)-6-(4-chloro-3-fluorophenyl)-5-(3-chlorophenyl)-3- methyl-2-oxopiperidin-3-yl)acetamido)-2-methoxybenzoic Acid

References

1. Rew Y, et al. J Med Chem. 2014 Dec 26;57(24):10499-511.

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