AM-7209

Names

[ Name ]:
AM-7209

[Synonym ]:
Benzoic acid, 4-[[2-[(3R,5R,6S)-6-(4-chloro-3-fluorophenyl)-5-(3-chlorophenyl)-1-[(1S)-1-cyclopropyl-2-[(1,1-dimethylethyl)sulfonyl]ethyl]-3-methyl-2-oxo-3-piperidinyl]acetyl]amino]-2-methoxy-
4-({[(3r,5r,6s)-1-[(1s)-2-(Tert-Butylsulfonyl)-1-Cyclopropylethyl]-6-(4-Chloro-3-Fluorophenyl)-5-(3-Chlorophenyl)-3-Methyl-2-Oxopiperidin-3-Yl]acetyl}amino)-2-Methoxybenzoic Acid
4-({[(3R,5R,6S)-6-(4-Chloro-3-fluorophenyl)-5-(3-chlorophenyl)-1-{(1S)-1-cyclopropyl-2-[(2-methyl-2-propanyl)sulfonyl]ethyl}-3-methyl-2-oxo-3-piperidinyl]acetyl}amino)-2-methoxybenzoic acid

Biological Activity

[Description]:

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).

[References]

References 1. Rew Y, et al. J Med Chem. 2014 Dec 26;57(24):10499-511. View Related Products by Target MDM2-p53

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
896.2±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₇H₄₁Cl₂FN₂O₇S

[ Molecular Weight ]:
747.700

[ Flash Point ]:
495.8±34.3 °C

[ Exact Mass ]:
746.199585

[ LogP ]:
7.50

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.603

Related Compounds

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