Compounds > ap 1903 reagent
Page last updated: 2024-11-12

ap 1903 reagent

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

Description

AP 1903 reagent: a dimerizer drug [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16135625
CHEMBL ID269259
SCHEMBL ID10111062
MeSH IDM0384358

Synonyms (37)

Synonym
ap1903
rimiducid ,
CHEMBL269259
ap-1903
S9726
2-piperidinecarboxylic acid, 1-(1-oxo-2-(3,4,5-trimethoxyphenyl)butyl)-, 1,2-ethanediylbis(imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene(3-(3,4-dimethoxyphenyl)propylidene)) ester, (2s-(1(r*),2r*(s*(s*(1(r*),2r*)))))-
h564l1w5j2 ,
unii-h564l1w5j2
ap 1903
rimiducid [inn]
rimiducid [usan:inn]
ap 1903 reagent
195514-63-7
2-piperidinecarboxylic acid, 1-((2s)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl)-, 2,2'-(1,2-ethanediylbis(imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene((1r)-3-(3,4-dimethoxyphenyl)propylidene))) ester, (2s,2's)-
CS-3162
HY-16046
rimiducid [usan]
rimiducid [who-dd]
SCHEMBL10111062
DTXSID80173226
AKOS030238859
DB04974
EX-A1711
(1r,1'r)-((((ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2s,2's)-bis(1-((s)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
D11195
rimiducid (usan/inn)
Q27279658
A919658
AT37167
MS-32155
[(1r)-3-(3,4-dimethoxyphenyl)-1-[3-[2-[2-[[2-[3-[(1r)-3-(3,4-dimethoxyphenyl)-1-[(2s)-1-[(2s)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carbonyl]oxypropyl]phenoxy]acetyl]amino]ethylamino]-2-oxoethoxy]phenyl]propyl] (2s)-1-[(2s)-2-(3,4,5-trimethoxyph
rimiducid (ap1903)
ap1903ap1903
VHA51463
ap 1903new
(1r,1'r)-((((ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl)(2s,2's)-bis(1-((s)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
AC-35487

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"Cellular therapies could play a role in cancer treatment and regenerative medicine if it were possible to quickly eliminate the infused cells in case of adverse events."( Inducible apoptosis as a safety switch for adoptive cell therapy.
Brenner, MK; Cruz, CR; Di Stasi, A; Dotti, G; Durett, AG; Fujita, Y; Gee, AP; Grilley, B; Heslop, HE; Kennedy-Nasser, A; Krance, RA; Liu, E; Liu, H; Martinez, C; Rooney, CM; Savoldo, B; Schindler, J; Spencer, DM; Straathof, K; Tey, SK, 2011)		0.37
" However, after CID treatment, 1% of iC9-T cells remain and can regrow over time; although these resurgent T cells do not cause recurrent GvHD, it remains unclear whether repeat CID treatments are a safe and feasible way to further deplete residual gene-modified T cells should any other adverse effects associated with them occur."( Serial Activation of the Inducible Caspase 9 Safety Switch After Human Stem Cell Transplantation.
Brenner, MK; Dakhova, O; Dotti, G; Heslop, HE; Naik, S; Zhou, X, 2016)		0.43

Dosage Studied

ExcerptRelevanceReference
" Twenty-eight normal healthy male volunteers were randomized into five dosage groups of AP1903 (0."( Intravenous safety and pharmacokinetics of a novel dimerizer drug, AP1903, in healthy volunteers.
Berger, HJ; Clackson, T; Dalgarno, D; Iuliucci, JD; Morley, S; Oliver, SD; Ward, C; Ward, J, 2001)		0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID84259Compound was induced transcription stably transfected with constructs encoding separate DNA-binding domain and activation domain proteins in HT1080 human fibrosarcoma cells2003Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
Regulation of gene expression by synthetic dimerizers with novel specificity.
AID84263Compound was induced transcription stably transfected with constructs encoding separate DNA-binding domain and activation domain proteins in HT1080 human fibrosarcoma cells2003Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
Regulation of gene expression by synthetic dimerizers with novel specificity.
AID84260Compound was induced transcription stably transfected with constructs encoding separate DNA-binding domain and activation domain proteins in HT1080 human fibrosarcoma cells; No induction2003Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
Regulation of gene expression by synthetic dimerizers with novel specificity.
AID84262Compound was induced transcription in transiently transfected with constructs encoding separate DNA-binding domain and activation domain proteins in HT1080 human fibrosarcoma cells2003Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
Regulation of gene expression by synthetic dimerizers with novel specificity.
AID84130Compound was induced transcription in transiently transfected with constructs encoding separate DNA-binding domain and activation domain proteins in HT1080 human fibrosarcoma cells2003Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
Regulation of gene expression by synthetic dimerizers with novel specificity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (29.41)29.6817
2010's11 (64.71)24.3611
2020's1 (5.88)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.60

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.

MetricThis Compound (vs All)
Research Demand Index11.60 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index4.69 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (23.53%)5.53%
Reviews1 (5.88%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (70.59%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		2.110diazine;
pyrazines		Daphnia magna metabolite
azacitidine
Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia.		2.1310N-glycosyl-1,3,5-triazine;
nucleoside analogue		antineoplastic agent
bortezomib
[no description available]		2.110amino acid amide;
L-phenylalanine derivative;
pyrazines		antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
tacrolimus
Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.		3.8330macrolide lactambacterial metabolite;
immunosuppressive agent
calcitriol
dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes		2.3110D3 vitamins;
hydroxycalciol;
triol		antineoplastic agent;
antipsoriatic;
bone density conservation agent;
calcium channel agonist;
calcium channel modulator;
hormone;
human metabolite;
immunomodulator;
metabolite;
mouse metabolite;
nutraceutical
ap20187
AP20187: a nontoxic, cell-permeable analog, a wholly synthesized, cell-permeable dimeric FK506 derivative. AP20187 : A tertiary amino compound that is 2-(aminomethyl)-N,N-dimethylpropane-1,3-diamine in which the primary ammino groups have each been acylated by condensation with the carboxy group of 2-{3-[(1R)-3-(3,4-dimethoxyphenyl)-1-hydroxypropyl]phenoxy}acetic acid, the hydroxy groups of which have been esterified by condensation with the carboxy group of L-pipecolic acid, the nitrogen of which has been acylated by condensation with (2S)-2-(3,4,5-trimethoxyphenyl)butyric acid. It is a synthetic, cell-permeable ligand that can be used to induce homodimerization of fusion proteins containing the DmrB domain.		2.0610aromatic ether;
carboxylic ester;
N-acylpiperidine;
tertiary amino compound		ligand
ConditionIndicatedRelationship StrengthStudiesTrials
Neuroblastoma
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)		02.3110
Anaplastic Large-Cell Lymphoma
[description not available]		04.411
Leukemia, Lymphoblastic, Acute, T Cell
[description not available]		04.411
Aspergillus Infection
[description not available]		04.411
Graft-Versus-Host Disease
[description not available]		09.25116
Dysmyelopoietic Syndromes
[description not available]		04.411
Viral Diseases
[description not available]		04.411
Leukemia, Pre-B-Cell
[description not available]		04.411
Aspergillosis
Infections with fungi of the genus ASPERGILLUS.		04.411
Graft vs Host Disease
The clinical entity characterized by anorexia, diarrhea, loss of hair, leukopenia, thrombocytopenia, growth retardation, and eventual death brought about by the GRAFT VS HOST REACTION.		09.25116
Myelodysplastic Syndromes
Clonal hematopoietic stem cell disorders characterized by dysplasia in one or more hematopoietic cell lineages. They predominantly affect patients over 60, are considered preleukemic conditions, and have high probability of transformation into ACUTE MYELOID LEUKEMIA.		16.411
Virus Diseases
A general term for diseases caused by viruses.		04.411
Precursor B-Cell Lymphoblastic Leukemia-Lymphoma
A leukemia/lymphoma found predominately in children and adolescents and characterized by a high number of lymphoblasts and solid tumor lesions. Frequent sites involve LYMPH NODES, skin, and bones. It most commonly presents as leukemia.		04.411
Lymphoma, Large-Cell, Anaplastic
A systemic, large-cell, non-Hodgkin, malignant lymphoma characterized by cells with pleomorphic appearance and expressing the CD30 ANTIGEN. These so-called hallmark cells have lobulated and indented nuclei. This lymphoma is often mistaken for metastatic carcinoma and MALIGNANT HISTIOCYTOSIS.		04.411
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
A leukemia/lymphoma found predominately in children and young adults and characterized LYMPHADENOPATHY and THYMUS GLAND involvement. It most frequently presents as a lymphoma, but a leukemic progression in the bone marrow is common.		04.411
Carcinoma, Non-Small Cell Lung
[description not available]		02.110
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		02.110
Duncan Disease
[description not available]		04.4111
Lymphoproliferative Disorders
Disorders characterized by proliferation of lymphoid tissue, general or unspecified.		04.4111
Experimental Neoplasms
[description not available]		02.0610
Recrudescence
[description not available]		07.4944
Leucocythaemia
[description not available]		07.4944
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)		07.4944
Benign Neoplasms
[description not available]		02.9610
Anemia
A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.		02.9610
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.		14.9610