Page last updated: 2024-12-08

nsc 100880

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

Cross-References

ID SourceID
PubMed CID23705698
CHEMBL ID164269
MeSH IDM0225924

Synonyms (18)

Synonym
nsc-100880
sodium camptothecin
CHEMBL164269 ,
sodium camptothecin, aldrichcpr
sodium (2s)-2-hydroxy-2-[8-(hydroxymethyl)-9-oxo-9h,11h-indolizino[1,2-b]quinolin-7-yl]butanoate
AKOS030524066
AS-75068
indolizino(1,2-b)quinoline-7-acetic acid, .alpha.-ethyl-9,11-dihydro-.alpha.-hydroxy-8-(hydroxymethyl)-9-oxo-, monosodium salt, (.alpha.s)-
indolizino(1,2-b)quinoline-7-acetic acid, .alpha.-ethyl-9,11-dihydro-.alpha.-hydroxy-8-(hydroxymethyl)-9-oxo-, monosodium salt, (s)-
sodium camptothecinate
indolizino(1,2-b)quinoline-7-acetic acid, .alpha.-ethyl-9,11-dihydro-.alpha.-hydroxy-8-(hydroxymethyl)-9-oxo-, sodium salt (1:1), (.alpha.s)-
J-015975
sodium (s)-2-hydroxy-2-(8-(hydroxymethyl)-9-oxo-9,11-dihydroindolizino[1,2-b]quinolin-7-yl)butanoate
sodium;(2s)-2-hydroxy-2-[8-(hydroxymethyl)-9-oxo-11h-indolizino[1,2-b]quinolin-7-yl]butanoate
C74317
A919299
CS-0145886
HY-N8533
[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)
DNA topoisomerase 1Homo sapiens (human)IC50 (µMol)12.00000.02101.862610.0000AID210946
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA topoisomerase 1Homo sapiens (human)CC500.90000.80001.20293.2000AID56563
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
DNA topological changeDNA topoisomerase 1Homo sapiens (human)
chromatin remodelingDNA topoisomerase 1Homo sapiens (human)
circadian rhythmDNA topoisomerase 1Homo sapiens (human)
response to xenobiotic stimulusDNA topoisomerase 1Homo sapiens (human)
programmed cell deathDNA topoisomerase 1Homo sapiens (human)
phosphorylationDNA topoisomerase 1Homo sapiens (human)
peptidyl-serine phosphorylationDNA topoisomerase 1Homo sapiens (human)
circadian regulation of gene expressionDNA topoisomerase 1Homo sapiens (human)
embryonic cleavageDNA topoisomerase 1Homo sapiens (human)
chromosome segregationDNA topoisomerase 1Homo sapiens (human)
DNA replicationDNA topoisomerase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingDNA topoisomerase 1Homo sapiens (human)
DNA bindingDNA topoisomerase 1Homo sapiens (human)
chromatin bindingDNA topoisomerase 1Homo sapiens (human)
double-stranded DNA bindingDNA topoisomerase 1Homo sapiens (human)
single-stranded DNA bindingDNA topoisomerase 1Homo sapiens (human)
RNA bindingDNA topoisomerase 1Homo sapiens (human)
DNA topoisomerase type I (single strand cut, ATP-independent) activityDNA topoisomerase 1Homo sapiens (human)
protein serine/threonine kinase activityDNA topoisomerase 1Homo sapiens (human)
protein bindingDNA topoisomerase 1Homo sapiens (human)
ATP bindingDNA topoisomerase 1Homo sapiens (human)
DNA binding, bendingDNA topoisomerase 1Homo sapiens (human)
protein domain specific bindingDNA topoisomerase 1Homo sapiens (human)
supercoiled DNA bindingDNA topoisomerase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
nuclear chromosomeDNA topoisomerase 1Homo sapiens (human)
P-bodyDNA topoisomerase 1Homo sapiens (human)
fibrillar centerDNA topoisomerase 1Homo sapiens (human)
male germ cell nucleusDNA topoisomerase 1Homo sapiens (human)
nucleusDNA topoisomerase 1Homo sapiens (human)
nucleoplasmDNA topoisomerase 1Homo sapiens (human)
nucleolusDNA topoisomerase 1Homo sapiens (human)
perikaryonDNA topoisomerase 1Homo sapiens (human)
protein-DNA complexDNA topoisomerase 1Homo sapiens (human)
nucleolusDNA topoisomerase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay IDTitleYearJournalArticle
AID137248L-1210 mouse leukemia life prolongation activity was measured as T/C (mean survival time of treated animals divided by the mean survival time of the controls times 100) at dose 10 mg/kg1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Plant antitumor agents. 28. Resolution of a key tricyclic synthon, 5'(RS)-1,5-dioxo-5'-ethyl-5'-hydroxy-2'H,5'H,6'H-6'-oxopyrano[3' ,4'- f]delta 6,8-tetrahydro-indolizine: total synthesis and antitumor activity of 20(S)- and 20(R)-camptothecin.
AID152253Lowest toxicity was observed at this dose against P-388 leukemia cells1980Journal of medicinal chemistry, May, Volume: 23, Issue:5
Plant antitumor agents. 18. Synthesis and biological activity of camptothecin analogues.
AID94100Compound was tested for active dose in L1210 Leukemia assay; 10-40 mg/kg1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Plant antitumor agents. 22. Isolation of 11-hydroxycamptothecin from Camptotheca acuminata Decne: total synthesis and biological activity.
AID137370L-1210 mouse leukemia life prolongation activity was measured as T/C (mean survival time of treated animals divided by the mean survival time of the controls times 100) at dose 80 mg/kg1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Plant antitumor agents. 28. Resolution of a key tricyclic synthon, 5'(RS)-1,5-dioxo-5'-ethyl-5'-hydroxy-2'H,5'H,6'H-6'-oxopyrano[3' ,4'- f]delta 6,8-tetrahydro-indolizine: total synthesis and antitumor activity of 20(S)- and 20(R)-camptothecin.
AID1123927Antitumor activity against mouse L1210 cells allografted in mouse assessed as increase in mouse survival time at 0.4 mg/kg, iv for 4 to 9 days relative to control1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Prodrug analogues of the antitumor alkaloid camptothecin.
AID235764Therapeutic index was measured on P-388 leukemia cells.1980Journal of medicinal chemistry, May, Volume: 23, Issue:5
Plant antitumor agents. 18. Synthesis and biological activity of camptothecin analogues.
AID1123932Antitumor activity against mouse L1210 cells allografted in mouse assessed as increase in mouse survival time at 3.7 mg/kg, iv for 4 to 9 days relative to control1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Prodrug analogues of the antitumor alkaloid camptothecin.
AID1123928Antitumor activity against mouse P388 cells allografted in mouse assessed as increase in mouse survival time at 11.1 mg/kg, iv for 4 to 9 days relative to control1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Prodrug analogues of the antitumor alkaloid camptothecin.
AID210946Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs.
AID98164Concentration that inhibits the proliferation of L1210 cells by 50%1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Modification of the hydroxy lactone ring of camptothecin: inhibition of mammalian topoisomerase I and biological activity.
AID120239Optimal activity expressed as percentage treated to that of control was measured in vivo against P-388 leukemia cells1980Journal of medicinal chemistry, May, Volume: 23, Issue:5
Plant antitumor agents. 18. Synthesis and biological activity of camptothecin analogues.
AID94103Compound was tested for maximum percentage T/C in L1210 Leukemia assay at 40 mg/kg (no cures out of 6)1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Plant antitumor agents. 22. Isolation of 11-hydroxycamptothecin from Camptotheca acuminata Decne: total synthesis and biological activity.
AID8446In vitro cytotoxicity of compound was tested against 9KB cells.1980Journal of medicinal chemistry, May, Volume: 23, Issue:5
Plant antitumor agents. 18. Synthesis and biological activity of camptothecin analogues.
AID1123929Antitumor activity against mouse P388 cells allografted in mouse assessed as increase in mouse survival time at 3.7 mg/kg, iv for 4 to 9 days relative to control1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Prodrug analogues of the antitumor alkaloid camptothecin.
AID1123933Antitumor activity against mouse L1210 cells allografted in mouse assessed as increase in mouse survival time at 1.2 mg/kg, iv for 4 to 9 days relative to control1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Prodrug analogues of the antitumor alkaloid camptothecin.
AID137250L-1210 mouse leukemia life prolongation activity was measured as T/C (mean survival time of treated animals divided by the mean survival time of the controls times 100) at dose 20 mg/kg1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Plant antitumor agents. 28. Resolution of a key tricyclic synthon, 5'(RS)-1,5-dioxo-5'-ethyl-5'-hydroxy-2'H,5'H,6'H-6'-oxopyrano[3' ,4'- f]delta 6,8-tetrahydro-indolizine: total synthesis and antitumor activity of 20(S)- and 20(R)-camptothecin.
AID152254This is the dose at which optimal activity was observed against P-388 leukemia cells1980Journal of medicinal chemistry, May, Volume: 23, Issue:5
Plant antitumor agents. 18. Synthesis and biological activity of camptothecin analogues.
AID1123971Antitumor activity against human HeLa cells assessed as inhibition of radioactive thymidine incorporation into acid-insoluble material by DNA sedimentation assay1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Prodrug analogues of the antitumor alkaloid camptothecin.
AID56563Concentration that produces 50% DNA cleavage mediated by DNA topoisomerase I1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Modification of the hydroxy lactone ring of camptothecin: inhibition of mammalian topoisomerase I and biological activity.
AID1123930Antitumor activity against mouse P388 cells allografted in mouse assessed as increase in mouse survival time at 1.2 mg/kg, iv for 4 to 9 days relative to control1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Prodrug analogues of the antitumor alkaloid camptothecin.
AID1123931Antitumor activity against mouse L1210 cells allografted in mouse assessed as increase in mouse survival time at 11.1 mg/kg, iv for 4 to 9 days relative to control1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Prodrug analogues of the antitumor alkaloid camptothecin.
AID152255Antileukemic activity against P-388 leukemia cells was measured at given dose range1980Journal of medicinal chemistry, May, Volume: 23, Issue:5
Plant antitumor agents. 18. Synthesis and biological activity of camptothecin analogues.
AID137251L-1210 mouse leukemia life prolongation activity was measured as T/C (mean survival time of treated animals divided by the mean survival time of the controls times 100) at dose 40 mg/kg1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Plant antitumor agents. 28. Resolution of a key tricyclic synthon, 5'(RS)-1,5-dioxo-5'-ethyl-5'-hydroxy-2'H,5'H,6'H-6'-oxopyrano[3' ,4'- f]delta 6,8-tetrahydro-indolizine: total synthesis and antitumor activity of 20(S)- and 20(R)-camptothecin.
AID1123923Antitumor activity against mouse P388 cells allografted in mouse assessed as increase in mouse survival time at 0.4 mg/kg, iv for 4 to 9 days relative to control1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Prodrug analogues of the antitumor alkaloid camptothecin.
AID94106Compound was tested for toxic dose in L1210 Leukemia assay1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Plant antitumor agents. 22. Isolation of 11-hydroxycamptothecin from Camptotheca acuminata Decne: total synthesis and biological activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (83.33)18.7374
1990's1 (16.67)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]