| Identification | Back Directory | [Name]
TDP-665759 | [CAS]
787632-66-0 | [Synonyms]
TDP 665759
TDP-665759
JNJ27291199
JNJ-27291199
JNJ 27291199
(3S)-4-[(1R)-1-(2-amino-4-chlorophenyl)ethyl]-3-(4-chlorophenyl)-7-iodo-1-[3-(4-methylpiperazin-1-yl)propyl]-3H-1,4-benzodiazepine-2,5-dione | [Molecular Formula]
C31H34Cl2IN5O2 | [MDL Number]
MFCD11840556 | [MOL File]
787632-66-0.mol | [Molecular Weight]
706.44 |
| Hazard Information | Back Directory | [Description]
TDP665759 is an inhibitor of the Hdm2:p53 complex. It acts by suppressing human tumor cell proliferation in vitro and sensitizing tumors to doxorubicin in vivo. | [Uses]
TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC50 of 5.90 μM) and the cell viability of p53 expressing A549R (IC50 of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models[1]. | [References]
[1] Koblish HK, et al. Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo. Mol Cancer Ther. 2006 Jan;5(1):160-9. DOI:10.1158/1535-7163.MCT-05-0199 |
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