787632-66-0
787632-66-0 structure
- Name: TDP-665759
- Chemical Name: (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
- CAS Number: 787632-66-0
- Molecular Formula: C31H34Cl2IN5O2
- Molecular Weight: 706.444
- Create Date: 2020-01-20 09:41:56
- Modify Date: 2024-01-12 10:55:44
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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.
| Name | (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 |
|---|---|
| Synonyms |
(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)- |
| 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. |
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| References | References 1. Koblish HK, et al. Mol Cancer Ther. 2006 Jan;5(1):160-9. View Related Products by Target MDM2-p53 |
| 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 |