Page last updated: 2024-12-11
ro 28-2653
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
Ro 28-2653: a synthetic matrix metalloproteinase inhibitor reduces tumor growth and prolongs survival in a prostate cancer standard rat model [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9832179 |
| CHEMBL ID | 456911 |
| SCHEMBL ID | 726759 |
| SCHEMBL ID | 8471189 |
| MeSH ID | M0423293 |
Synonyms (18)
| Synonym |
|---|
| ro 28-2653 |
| ro-28-2653 |
| 5-[4-(4-nitrophenyl)piperazin-1-yl]-5-(4-phenylphenyl)-1,3-diazinane-2,4,6-trione |
| CHEMBL456911 , |
| bdbm50363130 |
| SCHEMBL726759 |
| SCHEMBL8471189 |
| 5-biphenyl-4-yl-5-[4-(4-nitro-phenyl)-piperazin-1-yl]-pyrimidine-2,4,6-trione |
| 5-(4-biphenylyl)-5-[4-(4-nitrophenyl)piperazin-1-yl]barbituric acid |
| 261956-22-3 |
| 5-([1,1'-biphenyl]-4-yl)-5-(4-(4-nitrophenyl)piperazin-1-yl)pyrimidine-2,4,6(1h,3h,5h)-trione |
| ro28-2653 |
| EX-A2614 |
| ro 28 2653; ro 282653; ro-28-2653; ro282653;ro28-2653 |
| BCP30790 |
| (2,4,6(1h,3h,5h)-pyrimidinetrione, 5-[1,1'-biphenyl]-4-yl-5-[4-(4-nitrophenyl)-1-piperazinyl]-) |
| A902961 |
| AKOS040747405 |
Research Excerpts
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " The area under curve (AUC) and the peak serum concentration (Cmax) were approximately 10 times higher than those obtained with the suspension, while the time (Tmax) to reach Cmax was reduced." | ( Pharmacokinetic study of a new synthetic MMP inhibitor (Ro 28-2653) after IV and oral administration of cyclodextrin solutions. Bertholet, P; Castagne, D; Chiap, P; Delattre, L; Evrard, B; Foidart, JM; Frankenne, F; Piel, G; Piette, M, 2006) | 0.58 |
Compound-Compound Interactions
The proliferation rate was only inhibited by etoposide while that effect was increased in combination with Ro 28-2653 and estramustine.
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "Ro-28-2653, a selective and orally bioavailable MMPI with inhibitory activity against MMPs expressed by tumor and/or stromal cells, is a potent antitumor and antiangiogenic agent." | ( Anti-invasive, antitumoral, and antiangiogenic efficacy of a pyrimidine-2,4,6-trione derivative, an orally active and selective matrix metalloproteinases inhibitor. Devy, L; Foidart, JM; Frankenne, F; Grams, F; Krell, HW; Maquoi, E; Noël, A; Olivier, F; Sounni, NE, 2004) | 0.32 |
| " The aim of this study is to demonstrate that an increase in Ro 28-2653 solubility, via ternary complex formation, can lead to an increase in the oral bioavailability of this drug." | ( Pharmacokinetic study of a new synthetic MMP inhibitor (Ro 28-2653) after IV and oral administration of cyclodextrin solutions. Bertholet, P; Castagne, D; Chiap, P; Delattre, L; Evrard, B; Foidart, JM; Frankenne, F; Piel, G; Piette, M, 2006) | 0.82 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (2)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 72 kDa type IV collagenase | Homo sapiens (human) | IC50 (µMol) | 0.0230 | 0.0000 | 1.2848 | 10.0000 | AID643325 |
| Matrix metalloproteinase-9 | Homo sapiens (human) | IC50 (µMol) | 0.0070 | 0.0000 | 0.7053 | 10.0000 | AID643327 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (64)
Molecular Functions (10)
Ceullar Components (10)
Bioassays (4)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID643327 | Inhibition of MMP9 using (7-methoxycoumarin-4-yl)acetyl-Pro-Leu-Gly-Leu-(3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)Ala-Arg-NH2 as substrate preincubated for 30 mins measured after 10 mins by fluorescence analysis | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography. |
| AID396059 | Antiinvasive activity in human HT1080 cells assessed as number of cells migrated at 1 uM after 24 hrs by Boyden chamber invasion assay | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12 | 6-Substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives in a new approach of the treatment of cancer cell invasion and metastasis. |
| AID643324 | Octanol-water partition coefficient, log D of the compound at pH 7.4 by gamma counter | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography. |
| AID643325 | Inhibition of MMP2 using (7-methoxycoumarin-4-yl)acetyl-Pro-Leu-Gly-Leu-(3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)Ala-Arg-NH2 as substrate preincubated for 30 mins measured after 10 mins by fluorescence analysis | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (24)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 19 (79.17) | 29.6817 |
| 2010's | 5 (20.83) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 11.04
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (11.04) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 24 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||