Page last updated: 2024-09-22

fazarabine

Description

fazarabine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-arabinofuranosyl residue via an N-glycosidic linkage. A synthetic analogue of cytosine arabinoside and 5-azacytidine that incorporates structural features of both compounds, it shows good activity against a variety of transplanted tumors. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID47751
CHEMBL ID2106666
CHEBI ID141077
SCHEMBL ID3278
SCHEMBL ID19463649
MeSH IDM0077798

Synonyms (41)

Synonym
ara-ac
aza-5-c
aza-a
nsc-281272
65886-71-7
kymarabine
fazarabine
fazarabine (usan/inn)
D04134
fazarabinum [latin]
1,3,5-triazin-2(1h)-one, 4-amino-1-beta-d-arabinofuranosyl-
s-triazin-2(1h)-one, 4-amino-1-beta-d-arabinofuranosyl-
4-amino-1-beta-d-arabinofuranosyl-s-triazin-2(1h)-one
fazarabina [spanish]
1-beta-d-arabinofuranosyl-5-azacytosine
5-azacytosine arabinoside
ccris 93
nsc 281272
fazarabine [usan:inn]
4-amino-1-[(2r,3s,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,3,5-triazin-2-one
CHEBI:141077
fazarabina
5-azacytarabine
fazarabinum
5v71d8jokk ,
unii-5v71d8jokk
NCGC00090851-09
4-amino-1-.beta.-d-arabinofuranosyl-1,3,5-triazin-2(1h)-one
fazarabine [mart.]
fazarabine [usan]
fazarabine [who-dd]
1,3,5-triazin-2(1h)-one, 4-amino-1-.beta.-d-arabinofuranosyl-
fazarabine [inn]
CHEMBL2106666
SCHEMBL3278
SCHEMBL19463649
SW219133-1
Q27262921
ccris93; nsc 281272; kymarabine
4-amino-1-((2r,3s,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1,3,5-triazin-2(1h)-one
DTXSID401024360

Research Excerpts

Overview

ExcerptReference
"Fazarabine is a novel nucleoside with broad spectrum pre-clinical activity and was chosen for study in patients with incurable non-small cell carcinoma of the lung. "( Crowley, JJ; Goodwin, JW; Livingston, RB; Panella, TJ; Williamson, SK, 1995)
"Fazarabine is a synthetic analog of cytosine arabinoside and 5-azacytidine that incorporates structural features of both compounds. "( Bernstein, ML; Devine, S; Dubowy, R; Grier, H; Kung, F; Land, V; Murphy, S; Whitehead, VM, 1993)

Effects

ExcerptReference
"Fazarabine has no demonstrable activity in patients with metastatic non-small cell carcinoma of the lung. "( Crowley, JJ; Goodwin, JW; Livingston, RB; Panella, TJ; Williamson, SK, 1995)
"Fazarabine has shown activity in the panel of 60 cultured human tumor lines of the National Cancer Institute. "( Ahluwalia, GS; Barchi, JJ; Cooney, DA; Covey, JM; Gharehbaghi, K; Hochman, I; Jayaram, HN; Paull, KD, 1996)
"Fazarabine has demonstrated a broad spectrum of antitumor activity in experimental models including P388 and L1210 cell lines. "( Estey, E; Kantarjian, HM; Keating, MJ; O'Brien, S; Plunkett, W; Rios, MB; Sorenson, M; Wilhelm, M, 1999)

Roles (1)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
N-glycosyl-1,3,5-triazine
nucleoside analogueAn analogue of a nucleoside, being an N-glycosyl compound in which the nitrogen-containing moiety is a modified nucleotide base. They are commonly used as antiviral products to prevent viral replication in infected cells.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency37.22120.00308.794948.0869AID1347053
EWS/FLI fusion proteinHomo sapiens (human)Potency5.72700.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
polyproteinZika virusPotency37.22120.00308.794948.0869AID1347053
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (87)

Assay IDTitleYearJournalArticle
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1134733Toxicity in CDF1 mouse assessed as change in body weight at 50 mg/kg, ip measured on day 5 relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1134727Antitumor activity in mouse L1210 cells allografted in CDF1 mouse assessed as increase in life span at 3.12 mg/kg, ip administered as qd for 9 days relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1134719Antitumor activity in mouse L1210 cells allografted in CDF1 mouse assessed as increase in life span at 50 mg/kg, ip administered as qd for 9 days relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1134716Antitumor activity in mouse L1210 cells allografted in CDF1 mouse assessed as increase in life span at 200 mg/kg, ip administered as qd for 9 days relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1134741Toxicity in CDF1 mouse assessed as change in body weight at 3.12 mg/kg, ip measured on day 5 relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1134723Antitumor activity in mouse L1210 cells allografted in CDF1 mouse assessed as increase in life span at 12.5 mg/kg, ip administered as qd for 9 days relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1134717Antitumor activity in mouse L1210 cells allografted in CDF1 mouse assessed as increase in life span at 100 mg/kg, ip administered as qd for 9 days relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1134735Toxicity in CDF1 mouse assessed as change in body weight at 25 mg/kg, ip measured on day 5 relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1134721Antitumor activity in mouse L1210 cells allografted in CDF1 mouse assessed as increase in life span at 25 mg/kg, ip administered as qd for 9 days relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1134728Antitumor activity in mouse L1210 cells allografted in CDF1 mouse assessed as increase in life span at 1.56 mg/kg, ip administered as qd for 9 days relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1134737Toxicity in CDF1 mouse assessed as change in body weight at 12.5 mg/kg, ip measured on day 5 relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1134743Toxicity in CDF1 mouse assessed as change in body weight at 0.78 mg/kg, ip measured on day 5 relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1134742Toxicity in CDF1 mouse assessed as change in body weight at 1.56 mg/kg, ip measured on day 5 relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1134739Toxicity in CDF1 mouse assessed as change in body weight at 6.25 mg/kg, ip measured on day 5 relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1134731Toxicity in CDF1 mouse assessed as change in body weight at 100 mg/kg, ip measured on day 5 relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1134730Toxicity in CDF1 mouse assessed as change in body weight at 200 mg/kg, ip measured on day 5 relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1134725Antitumor activity in mouse L1210 cells allografted in CDF1 mouse assessed as increase in life span at 6.25 mg/kg, ip administered as qd for 9 days relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1134729Antitumor activity in mouse L1210 cells allografted in CDF1 mouse assessed as increase in life span at 0.78 mg/kg, ip administered as qd for 9 days relative to control1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1134745Drug degradation in water solution at 25 degC after 4 hrs by reverse phase liquid chromatography1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Synthesis and antitumor activity of 5-azacytosine arabinoside.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (53)

TimeframeStudies, This Drug (%)All Drugs %
pre-199021 (39.62)18.7374
1990's24 (45.28)18.2507
2000's1 (1.89)29.6817
2010's2 (3.77)24.3611
2020's5 (9.43)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 (%)
Trials16 (28.57%)5.53%
Reviews4 (7.14%)6.00%
Case Studies1 (1.79%)4.05%
Observational0 (0.00%)0.25%
Other35 (62.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Safety/Toxicity (1)

ArticleYear
Enhancement of the toxicity and DNA incorporation of arabinosyl-5-azacytosine and 1-beta-D-arabinofuranosylcytosine by cyclopentenyl cytosine.
Cancer research, Nov-15, Volume: 50, Issue: 22
1990
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Long-term Use (1)

ArticleYear
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (3)

ArticleYear
Phase I trial and pharmacokinetic evaluation of fazarabine in children.
Cancer research, Sep-15, Volume: 49, Issue: 18
1989
Phase I and pharmacokinetic study of arabinofuranosyl-5-azacytosine (fazarabine, NSC 281272).
Cancer research, Feb-15, Volume: 50, Issue: 4
1990
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (1)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, Volume: 96, Issue: 5
2019
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (3)

ArticleYear
A phase II study of fazarabine (NSC 281272) in patients with advanced squamous cell carcinoma of the cervix. A Gynecologic Oncology Group study.
American journal of clinical oncology, Volume: 18, Issue: 5
1995
A phase I trial of fazarabine in refractory pediatric solid tumors. A Pediatric Oncology Group study.
Investigational new drugs, Volume: 11, Issue: 4
1993
A comparison of the lethal effects in culture of cytosine arabinoside and arabinofuranosyl-5-azacytosine acting on the blast cells fo acute myeloblastic leukemia.
Hematologic pathology, Volume: 6, Issue: 3
1992
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]