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MI 219

Names

[ CAS No. ]:
908027-55-4

[ Name ]:
MI 219

[Synonym ]:
Spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide, 6-chloro-4'-(3-chlorophenyl)-N-[(3S)-3,4-dihydroxybutyl]-2'-(2,2-dimethylpropyl)-5-fluoro-1,2-dihydro-2-oxo-, (2'R,3S,4'R,5'R)-
(2'R,3S,4'R,5'R)-6-Chloro-4'-(3-chlorophenyl)-N-[(3S)-3,4-dihydroxybutyl]-2'-(2,2-dimethylpropyl)-5-fluoro-2-oxo-1,2-dihydrospiro[indole-3,3'-pyrrolidine]-5'-carboxamide

Biological Activity

[Description]:

MI 219 is a potent, specific MDM2-p53 inhibitor with Ki of 5 nM, >10,000-fold selective for MDM2 over MDMX; disrupts the MDM2-p53 interaction and activates the p53 pathway in cells with wild-type p53, which leads to induction of cell cycle arrest in all cells and selective apoptosis in tumor cells; inhibits tumor growth in mouse xenograft models.

[References]

References 1. Shangary S, et al. Proc Natl Acad Sci U S A. 2008 Mar 11;105(10):3933-8. 2. Peterson LF, et al. Leukemia. 2011 May;25(5):761-9. 3. Feng FY, et al. Neoplasia. 2016 Apr;18(4):213-22. View Related Products by Target MDM2-p53

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
779.9±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C27H32Cl2FN3O4

[ Molecular Weight ]:
552.465

[ Flash Point ]:
425.5±32.9 °C

[ Exact Mass ]:
551.175415

[ LogP ]:
4.48

[ Vapour Pressure ]:
0.0±2.8 mmHg at 25°C

[ Index of Refraction ]:
1.629

Related Compounds