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AM-6761

Names

[ CAS No. ]:
1584732-36-4

[ Name ]:
AM-6761

[Synonym ]:
(2-{[(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]methyl}-1,3-thiazol-5-yl)acetic acid
(2-{[(3r,5r,6s)-1-[(1s)-2-(Tert-Butylsulfonyl)-1-Cyclopropylethyl]-6-(4-Chloro-3-Fluorophenyl)-5-(3-Chlorophenyl)-3-Methyl-2-Oxopiperidin-3-Yl]methyl}-1,3-Thiazol-5-Yl)acetic Acid
5-Thiazoleacetic acid, 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]methyl]-

Biological Activity

[Description]:

A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.1 nM), cellular potency (SJSA-1 EdU IC50=16 nM), and favorable pharmacokinetic properties; shows excellent antitumor activity in the SJSA-1 osteosarcoma xenograft model with ED50 of 11 mg/kg.

[References]

References 1. Gonzalez AZ, et al. J Med Chem. 2014 Apr 10;57(7):2963-88. View Related Products by Target MDM2-p53

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
821.7±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C33H37Cl2FN2O5S2

[ Molecular Weight ]:
695.692

[ Flash Point ]:
450.8±34.3 °C

[ Exact Mass ]:
694.150513

[ LogP ]:
6.72

[ Vapour Pressure ]:
0.0±3.1 mmHg at 25°C

[ Index of Refraction ]:
1.611

Related Compounds