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TDP-665759

Names

[ CAS No. ]:
787632-66-0

[ Name ]:
TDP-665759

[Synonym ]:
(3S)-4-[(1R)-1-(2-amino-4-chlorophenyl)ethyl]-3-(4-chlorophenyl)-7-iodo-1-[3-(4-methylpiperazin-1-yl)propyl]-3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione
(3S)-4-[(1R)-1-(2-Amino-4-chlorophenyl)ethyl]-3-(4-chlorophenyl)-7-iodo-1-[3-(4-methyl-1-piperazinyl)propyl]-3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione
1H-1,4-Benzodiazepine-2,5-dione, 4-[(1R)-1-(2-amino-4-chlorophenyl)ethyl]-3-(4-chlorophenyl)-3,4-dihydro-7-iodo-1-[3-(4-methyl-1-piperazinyl)propyl]-, (3S)-

Biological Activity

[Description]:

A small molecule inhibitor of HDM2-p53 interaction with FP IC50 of 0.7 uM; inhibits the proliferation of wt p53-expressing cell lines with average IC50 of 0.7 uM, stabilizes p53 protein levels, upregulates p53 target genes in a DNA damage-independent manner, and induces apoptosis in HepG2 cells; increases p21(waf1/cip1) levels in mice liver samples, synergizes the effect of doxorubicin both in culture and in an A375 xenograft model.

[References]

References 1. Koblish HK, et al. Mol Cancer Ther. 2006 Jan;5(1):160-9. View Related Products by Target MDM2-p53

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
835.4±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C31H34Cl2IN5O2

[ Molecular Weight ]:
706.444

[ Flash Point ]:
459.1±34.3 °C

[ Exact Mass ]:
705.113403

[ LogP ]:
4.39

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

[ Index of Refraction ]:
1.649

Related Compounds