Page last updated: 2024-11-13

sf 1126

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

Description

SF 1126: an LY294002 prodrug and pan PI3K inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID66577114
CHEMBL ID2326966
SCHEMBL ID15668089
MeSH IDM0518423

Synonyms (11)

Synonym
sf1126 ,
936487-67-1
sf-1126
sf 1126
CHEMBL2326966
sf-1126 inner salt
SCHEMBL15668089
bdbm50507755
Q27276459
EX-A5997
(8s,14s,17s)-14-(carboxymethyl)-8-(3-guanidinopropyl)-17-(hydroxymethyl)-3,6,9,12,15-pentaoxo-1-(4-(4-oxo-8-phenyl-4h-chromen-2-yl)morpholino-4-ium)-2-oxa-7,10,13,16-tetraazaoctadecan-18-oate

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Exposure measured by peak concentration (C(max)) and area under the time-concentration curve (AUC(0-)(t)) was dose proportional."( Phase I pharmacokinetic and pharmacodynamic study of the pan-PI3K/mTORC vascular targeted pro-drug SF1126 in patients with advanced solid tumours and B-cell malignancies.
Anthony, SP; Becker, MD; Chiorean, EG; Cordova, F; Durden, DL; Garlich, JR; Harris, WB; Mahadevan, D; Qi, W; Ramanathan, RK; Rensvold, DM; Shelton, CF; Stejskal-Barnett, A; Von Hoff, DD; Younger, AE, 2012
)
0.38
[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)
Bromodomain-containing protein 4Homo sapiens (human)IC50 (µMol)5.30000.00040.40329.0500AID1534669
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (10)

Processvia Protein(s)Taxonomy
regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
chromatin organizationBromodomain-containing protein 4Homo sapiens (human)
DNA damage responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
regulation of inflammatory responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of T-helper 17 cell lineage commitmentBromodomain-containing protein 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingBromodomain-containing protein 4Homo sapiens (human)
p53 bindingBromodomain-containing protein 4Homo sapiens (human)
chromatin bindingBromodomain-containing protein 4Homo sapiens (human)
transcription coregulator activityBromodomain-containing protein 4Homo sapiens (human)
transcription coactivator activityBromodomain-containing protein 4Homo sapiens (human)
protein bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityBromodomain-containing protein 4Homo sapiens (human)
enzyme bindingBromodomain-containing protein 4Homo sapiens (human)
lysine-acetylated histone bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II C-terminal domain bindingBromodomain-containing protein 4Homo sapiens (human)
P-TEFb complex bindingBromodomain-containing protein 4Homo sapiens (human)
histone reader activityBromodomain-containing protein 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
condensed nuclear chromosomeBromodomain-containing protein 4Homo sapiens (human)
nucleusBromodomain-containing protein 4Homo sapiens (human)
nucleoplasmBromodomain-containing protein 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1534669Inhibition of recombinant full length human N-terminal His6-tagged BRD4 (2 to 1362 residues) expressed in baculovirus infected insect cells using histone H4 peptide as substrate by alpha screen assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
AID728989Antiproliferative activity against human MCF7 cells assessed as inhibition of mammosphere formation at 10 uM after 5 to 7 days by microscopic analysis relative to control2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (6.67)29.6817
2010's12 (80.00)24.3611
2020's2 (13.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.21

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 Index25.21 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index5.34 (4.65)
Search Engine Demand Index20.59 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (13.33%)5.53%
Reviews1 (6.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]