Compounds > rg7112
Page last updated: 2024-11-13

rg7112

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID57406853
CHEMBL ID2386346
SCHEMBL ID12704861
MeSH IDM0583205

Synonyms (40)

Synonym
HY-10959
rg7112 ,
ro5045337
r 7112
mdm2 antagonist ro5045337
rg-7112
ro-5045337
q8mi0x869m ,
ro 5045337
unii-q8mi0x869m
rg 7112
939981-39-2
bdbm50434287
chembl2386346 ,
CS-0330
r 7112 [who-dd]
methanone, ((4s,5r)-4,5-bis(4-chlorophenyl)-2-(4-(1,1-dimethylethyl)-2-ethoxyphenyl)-4,5-dihydro-4,5-dimethyl-1h-imidazol-1-yl)(4-(3-(methylsulfonyl)propyl)-1-piperazinyl)-
S7030
SCHEMBL12704861
((4s,5r)-2-(4-(tert-butyl)-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethyl-4,5-dihydro-1h-imidazol-1-yl)(4-(3-(methylsulfonyl)propyl)piperazin-1-yl)methanone
AC-32970
DTXSID60240182
AKOS027282701
methanone, [(4s,5r)-4,5-bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1h-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]-
[(4s,5r)-2-(4-t-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethylimidazol-1-yl]-[4-(3-methylsulfonylpropyl)piperazin-1-yl]methanone
[(4s,5r)-2-(4-tert-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethylimidazol-1-yl]-[4-(3-methylsulfonylpropyl)piperazin-1-yl]methanone
gtpl9599
ro5045337; rg7112
BCP07937
rg-7112;rg 7112; ro-5045337; ro 5045337; ro5045337
rg7112 (ro5045337)
EX-A1686
DB14793
SB19057
CCG-270414
Q27287118
nsc809100
nsc-809100
A857519
[(4r,5s)-4,5-bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1h-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone;r7112 rg7112 rg 7112; rg7112; ro5045337; ro 5045337; ro5045337

Research Excerpts

Overview

RG7112 is a small-molecule MDM2 antagonist. It frees p53 from negative control, activating the p53 pathway in cancer cells leading to cell cycle arrest and apoptosis.

ExcerptReferenceRelevance
"RG7112 is a small-molecule MDM2 antagonist. "( Results of the Phase I Trial of RG7112, a Small-Molecule MDM2 Antagonist in Leukemia.
Andreeff, M; Assouline, S; Blotner, S; Bowen, D; Bridge, P; Chen, G; Drummond, MW; González, GM; Graves, B; Huang, X; Iyer, SP; Jukofsky, L; Kelly, KR; Kirschbaum, M; Kojima, K; Martinelli, G; Middleton, S; Nichols, G; Popplewell, L; Reckner, M; Rueger, R; Ruvolo, V; Strair, R; Vyas, P; Yee, K; Zhi, J, 2016)		2.16
"RG7112 is a selective inhibitor of p53-MDM2 binding that frees p53 from negative control, activating the p53 pathway in cancer cells leading to cell cycle arrest and apoptosis. "( Initial testing of the MDM2 inhibitor RG7112 by the Pediatric Preclinical Testing Program.
Billups, CA; Carol, H; Geier, B; Gorlick, R; Houghton, PJ; Kang, MH; Keir, ST; Kolb, EA; Kurmasheva, RT; Lock, RB; Maris, JM; Reynolds, CP; Smith, MA, 2013)		2.1
"RG7112 is a potent and selective member of the nutlin family of MDM2 antagonists currently in phase I clinical studies."( MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models.
Filipovic, Z; Garrido, R; Graves, B; Higgins, B; Kolinsky, K; Lee, E; Linn, M; Packman, K; Podlaski, F; Tardell, C; To, KH; Tovar, C; Vassilev, LT; Vu, B; Wovkulich, P; Xia, M, 2013)		1.4

Bioavailability

The drug was used to target JAK2V617F hematopoietic progenitors and stem cells. A high-fat/high-energy meal and a new formulation under fasting condition, respectively, enhanced overall bioavailability of RG7112.

ExcerptReferenceRelevance
"In this issue of Blood, Lu et al describe the cooperation between an orally bioavailable mouse double minute 2 (MDM2) antagonist (RG7112) and the pegylated interferon α (Peg-IFNα 2a) to target JAK2V617F hematopoietic progenitors and stem cells."( p53 at the crossroads of MPN treatment.
Plo, I, 2014)		0.61
"In part 1, the impact of high-energy/high-fat meal and formulations (crystalline and amorphous) on relative bioavailability was examined in single-dose crossover designs."( Clinical pharmacology characterization of RG7112, an MDM2 antagonist, in patients with advanced solid tumors.
Agrawal, M; Beeram, M; Beryozkina, A; Bhalla, K; Middleton, S; Nemunaitis, J; Nichols, G; Patnaik, A; Peck, R; Sarapa, N; Tolcher, A; Weiss, GJ; Zhi, J, 2015)		0.68
"With a single-dose treatment, a high-fat/high-energy meal and a new formulation under fasting condition, respectively, enhanced overall bioavailability of RG7112 slightly over twofold."( Clinical pharmacology characterization of RG7112, an MDM2 antagonist, in patients with advanced solid tumors.
Agrawal, M; Beeram, M; Beryozkina, A; Bhalla, K; Middleton, S; Nemunaitis, J; Nichols, G; Patnaik, A; Peck, R; Sarapa, N; Tolcher, A; Weiss, GJ; Zhi, J, 2015)		0.88
" Furthermore, bioavailability and efficacy were verified ex vivo in the physiological environment of degenerating intact human discs where a single dose improved disc matrix homeostasis."( Senotherapeutic drugs for human intervertebral disc degeneration and low back pain.
Bisson, DG; Cherif, H; Haglund, L; Mannarino, M; Ouellet, JA; Rabau, O, 2020)		0.56

Dosage Studied

Antitumor clinical activity has been demonstrated for the MDM2 antagonist RG7112, but patient tolerability for the necessary daily dosing was poor. High-dose treatments of consecutive daily doses for 5 and 3 days resulted in higher on-treatment-day exposure to RG 7112 than both weekly and low-dose/long-duration (20-day) daily schedules.

ExcerptRelevanceReference
"Antitumor clinical activity has been demonstrated for the MDM2 antagonist RG7112, but patient tolerability for the necessary daily dosing was poor."( Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach.
Adames, V; Filipovic, Z; Garrido, R; Glenn, K; Heimbrook, D; Higgins, B; Hussain, S; Kolinsky, K; Lee, E; Linn, M; Meille, C; Packman, K; Tannu, S; Tovar, C; Vassilev, L; Walz, A, 2014)		0.63
"A pharmacokinetic-pharmacodynamic (PKPD) model was developed on the basis of preclinical data to determine alternative dosing schedule requirements for optimal RG7388-induced antitumor activity."( Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach.
Adames, V; Filipovic, Z; Garrido, R; Glenn, K; Heimbrook, D; Higgins, B; Hussain, S; Kolinsky, K; Lee, E; Linn, M; Meille, C; Packman, K; Tannu, S; Tovar, C; Vassilev, L; Walz, A, 2014)		0.4
" In initial efficacy testing, daily dosing at 30 mg/kg and twice a week dosing at 50 mg/kg of RG7388 were statistically equivalent in our tumor model."( Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach.
Adames, V; Filipovic, Z; Garrido, R; Glenn, K; Heimbrook, D; Higgins, B; Hussain, S; Kolinsky, K; Lee, E; Linn, M; Meille, C; Packman, K; Tannu, S; Tovar, C; Vassilev, L; Walz, A, 2014)		0.4
" High-dose treatments of consecutive daily dosing for 5 and 3 days resulted in higher on-treatment-day exposure to RG7112 than both weekly and low-dose/long-duration (20-day) daily schedules."( Clinical pharmacology characterization of RG7112, an MDM2 antagonist, in patients with advanced solid tumors.
Agrawal, M; Beeram, M; Beryozkina, A; Bhalla, K; Middleton, S; Nemunaitis, J; Nichols, G; Patnaik, A; Peck, R; Sarapa, N; Tolcher, A; Weiss, GJ; Zhi, J, 2015)		0.89
" Pharmacokinetic analysis indicated that twice-daily dosing enhanced daily exposure."( Results of the Phase I Trial of RG7112, a Small-Molecule MDM2 Antagonist in Leukemia.
Andreeff, M; Assouline, S; Blotner, S; Bowen, D; Bridge, P; Chen, G; Drummond, MW; González, GM; Graves, B; Huang, X; Iyer, SP; Jukofsky, L; Kelly, KR; Kirschbaum, M; Kojima, K; Martinelli, G; Middleton, S; Nichols, G; Popplewell, L; Reckner, M; Rueger, R; Ruvolo, V; Strair, R; Vyas, P; Yee, K; Zhi, J, 2016)		0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)IC50 (µMol)0.01800.00060.358210.0000AID1659344; AID1908063; AID748501; AID759660
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)Kd0.00680.00000.25851.0000AID1075196; AID1807820
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (64)

Processvia Protein(s)Taxonomy
regulation of cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein polyubiquitinationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
blood vessel developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
blood vessel remodelingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
regulation of heart rateE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
atrioventricular valve morphogenesisE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
endocardial cushion morphogenesisE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ventricular septum developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
atrial septum developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
apoptotic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
traversing start control point of mitotic cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of cell population proliferationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to xenobiotic stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to toxic substanceE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to iron ionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of gene expressionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of protein processingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of neuron projection developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein ubiquitinationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein sumoylationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein destabilizationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to magnesium ionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein localization to nucleusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
regulation of protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to cocaineE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of DNA damage response, signal transduction by p53 class mediatorE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
establishment of protein localizationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to etherE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of DNA-templated transcriptionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of mitotic cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to antibioticE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of protein export from nucleusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to steroid hormoneE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of muscle cell differentiationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
proteolysis involved in protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein autoubiquitinationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cardiac septum morphogenesisE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein-containing complex assemblyE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to hydrogen peroxideE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to vitamin B1E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to alkaloidE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to growth factor stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to peptide hormone stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to estrogen stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to hypoxiaE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to gamma radiationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to UV-CE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
fibroblast activationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to actinomycin DE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of signal transduction by p53 class mediatorE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway by p53 class mediatorE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to formaldehydeE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell migrationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
amyloid fibril formationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to water-immersion restraint stressE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of apoptotic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
regulation of gene expressionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
p53 bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin-protein transferase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
5S rRNA bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
zinc ion bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ligase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
SUMO transferase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
enzyme bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein domain specific bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin protein ligase bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
receptor serine/threonine kinase bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
identical protein bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
peroxisome proliferator activated receptor bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ribonucleoprotein complex bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin protein ligase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
NEDD8 ligase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
disordered domain specific bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
nuclear bodyE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
nucleusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
nucleoplasmE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
nucleolusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cytoplasmE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cytosolE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
plasma membraneE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
transcription repressor complexE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
endocytic vesicle membraneE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein-containing complexE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (31)

Assay IDTitleYearJournalArticle
AID748495Cmax in mouse at 50 mg/kg, po2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID759668AUC in nude mouse xenografted with human SJSA1 cells at 100 mg/kg, po2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1659344Inhibition of MDM2 (unknown origin) by HTRF assay2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases.
AID748498Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID1872998Antitumor activity against human SJSA-1 xenografted Balb/c mouse assessed as tumor growth inhibition at 50 mg/kg,po administered daily by caliper method2022European journal of medicinal chemistry, Jun-05, Volume: 236Small-molecule MDM2 inhibitors in clinical trials for cancer therapy.
AID759665Antitumor activity against human SJSA1 cells xenografted in nude mouse assessed as tumor growth inhibition at 100 mg/kg, po after 2 weeks relative to control2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID748501Inhibition of N-terminal human recombinant MDM2 assessed as inhibition of protein interaction with p53 by HTRF assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID1075196Binding affinity to human MDM2 by by Surface Plasmon Resonace (SPR) spectroscopy binding assay2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
AID748497Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as cell viability after 5 days by MTT assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID760062Inhibition of Humanized-Xenopus MDM2 (13-119 amino acids) interaction with p53 by SPR analysis2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Deconstruction of a nutlin: dissecting the binding determinants of a potent protein-protein interaction inhibitor.
AID760060Inhibition of [15N]-labeled humanized-Xenopus MDM2 (13-119 amino acids) interaction with p53 at 0.5 mM by NMR method2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Deconstruction of a nutlin: dissecting the binding determinants of a potent protein-protein interaction inhibitor.
AID748500Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID759664Antitumor activity against human SJSA1 cells xenografted in nude mouse assessed as tumor growth inhibition at 50 mg/kg, po after 2 weeks relative to control2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1908063Inhibition of MDM2 (unknown origin)
AID759669AUC in nude mouse xenografted with human SJSA1 cells at 50 mg/kg, po2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1129365Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.
AID1807820Binding affinity to recombinant human GST-tagged HDM22021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Discovery of
AID759641Half life in nude mouse at 5 mg/kg, iv2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1075195Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
AID759642Cmax in nude mouse at 50 mg/kg, po2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID1872999Antitumor activity against human MHM xenografted Balb/c mouse assessed as tumor growth inhibition at 50 mg/kg,po administered daily by caliper method2022European journal of medicinal chemistry, Jun-05, Volume: 236Small-molecule MDM2 inhibitors in clinical trials for cancer therapy.
AID748493Apparent half life in mouse at 50 mg/kg, po2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID748494AUClast in mouse at 50 mg/kg, po2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID759660Binding affinity to GST-tagged MDM2 (unknown origin) assessed as inhibition of interaction with p53 after 1 hr by HTRF assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759644AUC in nude mouse at 50 mg/kg, po2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID748492Antitumor activity against human SJSA1 cells xenografted in nude mouse assessed as tumor growth inhibition at 50 mg/kg, po relative to control2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID748499Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID748496Cytotoxicity against human SW480 cells expressing p53 mutant assessed as cell viability after 5 days by MTT assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID759640Clearance in nude mouse at 5 mg/kg, iv2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID759656Clearance in human liver microsomes at 1 mM by LC-MS/MS analysis2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
AID748491Antitumor activity against human MHM cells xenografted in po dosed mouse relative to nutlin-3a2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (36)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's29 (80.56)24.3611
2020's7 (19.44)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.32

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.32 (24.57)
Research Supply Index3.71 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index33.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (11.11%)5.53%
Reviews6 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other26 (72.22%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
adenine
[no description available]		2.21106-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
imidazole
imidazole: RN given refers to parent cpd. 1H-imidazole : An imidazole tautomer which has the migrating hydrogen at position 1.		2.0810imidazole
4-aminobenzoic acid
para-Aminobenzoates: Benzoic acids, salts, or esters that contain an amino group attached to carbon number 4 of the benzene ring structure.. 4-aminobenzoate : An aromatic amino-acid anion that is the conjugate base of 4-aminobenzoic acid.		3.930aminobenzoate;
aromatic amino-acid anion		Escherichia coli metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
chlorobenzene
[no description available]		2.0810monochlorobenzenessolvent
2-vanillin
ortho-vanillin : A member of the class of benzaldehydes that is salicylaldehyde substituted by a methoxy group at position 3.		2.2510benzaldehydes;
guaiacols		antimutagen;
plant metabolite
2-piperidone
2-piperidone: structure given in first source. piperidin-2-one : A delta-lactam that is piperidine which is substituted by an oxo group at position 2.		2.1710delta-lactam;
piperidones		EC 1.2.1.88 (L-glutamate gamma-semialdehyde dehydrogenase) inhibitor
phenyl acetate
phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.		2.1710benzenes;
phenyl acetates
ecteinascidin 743
[no description available]		2.1110acetate ester;
azaspiro compound;
bridged compound;
hemiaminal;
isoquinoline alkaloid;
lactone;
organic heteropolycyclic compound;
organic sulfide;
oxaspiro compound;
polyphenol;
tertiary amino compound		alkylating agent;
angiogenesis modulating agent;
anti-inflammatory agent;
antineoplastic agent;
marine metabolite
imatinib mesylate
imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.		2.1310methanesulfonate saltanticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
leptomycin b
[no description available]		3.1910
nutlin-3a
nutlin 3: an MDM2 antagonist; structure in first source		5.0360stilbenoid
rg7388
RG7388: structure in first source		4.670
sar405838
SAR405838: an inhibitor of the interaction of MDM2 and p53; has antineoplastic activity; structure in first source		4.8550
(1S,2R)-2-[[(1S)-1-[(1,3-dioxo-2-isoindolyl)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-oxomethyl]-1-cyclohexanecarboxylic acid
LH601A: inhibits the interaction between KEAP1 and NRF2; structure in first source		3.3510phthalimides
amg 232
[no description available]		3.9330
cpi203
CPI203: a BET protein bromodomain inhibitor		2.1310
onc201
TIC10 compound: a TRAIL-dependent antitumor agent; structure in first source		2.4110
ConditionIndicatedRelationship StrengthStudiesTrials
Bone Cancer
[description not available]		02.520
Osteogenic Sarcoma
[description not available]		02.520
Bone Neoplasms
Tumors or cancer located in bone tissue or specific BONES.		02.520
Osteosarcoma
A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)		02.520
Benign Neoplasms
[description not available]		07.0661
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		19.0661
Agnogenic Myeloid Metaplasia
[description not available]		04.2231
Primary Myelofibrosis
A de novo myeloproliferation arising from an abnormal stem cell. It is characterized by the replacement of bone marrow by fibrous tissue, a process that is mediated by CYTOKINES arising from the abnormal clone.		04.2231
Cancer of Ovary
[description not available]		02.5720
Ovarian Neoplasms
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.		02.5720
Adenocarcinoma, Clear Cell
An adenocarcinoma characterized by the presence of varying combinations of clear and hobnail-shaped tumor cells. There are three predominant patterns described as tubulocystic, solid, and papillary. These tumors, usually located in the female reproductive organs, have been seen more frequently in young women since 1970 as a result of the association with intrauterine exposure to diethylstilbestrol. (From Holland et al., Cancer Medicine, 3d ed)		02.5720
Degenerative Disc Disease
[description not available]		02.2510
Low Back Ache
[description not available]		02.2510
Low Back Pain
Acute or chronic pain in the lumbar or sacral regions, which may be associated with musculo-ligamentous SPRAINS AND STRAINS; INTERVERTEBRAL DISK DISPLACEMENT; and other conditions.		02.2510
Intervertebral Disc Degeneration
Degenerative changes in the INTERVERTEBRAL DISC due to aging or structural damage, especially to the vertebral end-plates.		02.2510
Mesothelioma
A tumor derived from mesothelial tissue (peritoneum, pleura, pericardium). It appears as broad sheets of cells, with some regions containing spindle-shaped, sarcoma-like cells and other regions showing adenomatous patterns. Pleural mesotheliomas have been linked to exposure to asbestos. (Dorland, 27th ed)		02.3110
Hematologic Malignancies
[description not available]		03.0610
Hematologic Neoplasms
Neoplasms located in the blood and blood-forming tissue (the bone marrow and lymphatic tissue). The commonest forms are the various types of LEUKEMIA, of LYMPHOMA, and of the progressive, life-threatening forms of the MYELODYSPLASTIC SYNDROMES.		15.0610
T-Cell Lymphoma
[description not available]		02.1710
Extranodal NK-T-Cell Lymphoma
[description not available]		02.1710
Lymphoma, T-Cell
A group of heterogeneous lymphoid tumors representing malignant transformations of T-lymphocytes.		02.1710
Astrocytoma, Grade IV
[description not available]		02.5520
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		07.5520
Sarcoma, Epithelioid
[description not available]		03.4220
Sarcoma
A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant.		110.4220
Cancer of Lung
[description not available]		02.110
Lung Neoplasms
Tumors or cancer of the LUNG.		02.110
Erythremia
[description not available]		03.8921
Polycythemia Vera
A myeloproliferative disorder of unknown etiology, characterized by abnormal proliferation of all hematopoietic bone marrow elements and an absolute increase in red cell mass and total blood volume, associated frequently with splenomegaly, leukocytosis, and thrombocythemia. Hematopoiesis is also reactive in extramedullary sites (liver and spleen). In time myelofibrosis occurs.		03.8921
Leucocythaemia
[description not available]		03.0110
Leukemia
A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)		03.0110
Acute Lymphoid Leukemia
[description not available]		02.1110
Acute Biphenotypic Leukemia
[description not available]		02.1110
Leukemia, Biphenotypic, Acute
An acute leukemia exhibiting cell features characteristic of both the myeloid and lymphoid lineages and probably arising from MULTIPOTENT STEM CELLS.		02.1110
Precursor Cell Lymphoblastic Leukemia-Lymphoma
A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias.		02.1110
Acute Myelogenous Leukemia
[description not available]		03.511
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		03.511
Leukemia, Lymphocytic
[description not available]		03.5111
Leukemia, Lymphoid
Leukemia associated with HYPERPLASIA of the lymphoid tissues and increased numbers of circulating malignant LYMPHOCYTES and lymphoblasts.		03.5111
Granulocytic Leukemia, Chronic
[description not available]		02.1310
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Clonal hematopoetic disorder caused by an acquired genetic defect in PLURIPOTENT STEM CELLS. It starts in MYELOID CELLS of the bone marrow, invades the blood and then other organs. The condition progresses from a stable, more indolent, chronic phase (LEUKEMIA, MYELOID, CHRONIC PHASE) lasting up to 7 years, to an advanced phase composed of an accelerated phase (LEUKEMIA, MYELOID, ACCELERATED PHASE) and BLAST CRISIS.		02.1310
Anoxemia
[description not available]		02.1310
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.5120
Angiogenesis, Pathologic
[description not available]		02.1310
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		02.1310