Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C9H12N2O5S |
| Molecular Weight | 260.267 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
NC(=O)C1=CSC(=N1)[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O
InChI
InChIKey=FVRDYQYEVDDKCR-DBRKOABJSA-N
InChI=1S/C9H12N2O5S/c10-8(15)3-2-17-9(11-3)7-6(14)5(13)4(1-12)16-7/h2,4-7,12-14H,1H2,(H2,10,15)/t4-,5-,6-,7-/m1/s1
| Molecular Formula | C9H12N2O5S |
| Molecular Weight | 260.267 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/11249583
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/11249583
Tiazofurin (NSC-286193; 2-beta-D-ribofuranosylthiazole-4-carboxamide) an approved chronic myeloid leukemia (CML) drug, is converted by cellular enzymes into tiazofurin adenine dinucleotide, TAD, which inhibits the enzyme as a cofactor mimic. Resistance to tiazofurin is quickly developed due to diminished ability of resistant cells to synthesize TAD and increased enzymatic degradation of TAD. It is a nucleoside analog with oncolytic activity being developed by Ribapharm (formerly ICN Pharmaceuticals) as a potential treatment for leukemia. Ribapharm, through a Russian subsidiary of ICN, is planned to conduct phase II studies of tiazofurine involving patients suffering from advanced ovarian cancer or multiple myeloma which is resistant to conventional therapy.
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
244.6 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
1100 mg/m² single, intravenous dose: 1100 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
441.4 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
2200 mg/m² single, intravenous dose: 2200 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
735.5 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
3300 mg/m² single, intravenous dose: 3300 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
903.6 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
4400 mg/m² single, intravenous dose: 4400 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1330 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
5500 mg/m² single, intravenous dose: 5500 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1586 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
6600 mg/m² single, intravenous dose: 6600 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
8.49 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3986812/ |
720 mg/m² 1 times / day steady-state, intravenous dose: 720 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
11.4 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3986812/ |
900 mg/m² 1 times / day steady-state, intravenous dose: 900 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
16 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3986812/ |
1800 mg/m² 1 times / day steady-state, intravenous dose: 1800 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1002 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
1100 mg/m² single, intravenous dose: 1100 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2671 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
2200 mg/m² single, intravenous dose: 2200 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4267 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
3300 mg/m² single, intravenous dose: 3300 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4451 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
4400 mg/m² single, intravenous dose: 4400 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6214 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
5500 mg/m² single, intravenous dose: 5500 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
7013 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
6600 mg/m² single, intravenous dose: 6600 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1044 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3986812/ |
720 mg/m² 1 times / day steady-state, intravenous dose: 720 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1366 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3986812/ |
900 mg/m² 1 times / day steady-state, intravenous dose: 900 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1915 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3986812/ |
1800 mg/m² 1 times / day steady-state, intravenous dose: 1800 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5.23 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
1100 mg/m² single, intravenous dose: 1100 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6.23 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
2200 mg/m² single, intravenous dose: 2200 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
6.57 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
3300 mg/m² single, intravenous dose: 3300 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
5.98 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
4400 mg/m² single, intravenous dose: 4400 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6.07 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
5500 mg/m² single, intravenous dose: 5500 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
5.78 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1568787/ |
6600 mg/m² single, intravenous dose: 6600 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
7.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3986812/ |
720 mg/m² 1 times / day steady-state, intravenous dose: 720 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
11.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3986812/ |
900 mg/m² 1 times / day steady-state, intravenous dose: 900 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3986812/ |
1800 mg/m² 1 times / day steady-state, intravenous dose: 1800 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
TIAZOFURIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
DLT: Malaise, Myalgias... Disc. AE: Neutropenic sepsis... Other AEs: Sleep disorders, Vomiting... Dose limiting toxicities: Malaise (2 patients) AEs leading toMyalgias (2 patients) Headaches (1 pt) discontinuation/dose reduction: Neutropenic sepsis (grade 5, 1 pt) Other AEs:Sleep disorders (4 patients) Sources: Vomiting (2 patients) Stomatitis (2 patients) Diarrhea (1 pt) Bradycardia (2 patients) Skin toxicity (4 patients) Eye disorders (4 patients) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Diarrhea | 1 pt | 2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Headaches | 1 pt DLT |
2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Bradycardia | 2 patients | 2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Stomatitis | 2 patients | 2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Vomiting | 2 patients | 2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Malaise | 2 patients DLT |
2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Myalgias | 2 patients DLT |
2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Eye disorders | 4 patients | 2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Skin toxicity | 4 patients | 2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Sleep disorders | 4 patients | 2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Neutropenic sepsis | grade 5, 1 pt Disc. AE |
2750 mg/m2 1 times / day multiple, oral Highest studied dose Dose: 2750 mg/m2, 1 times / day Route: oral Route: multiple Dose: 2750 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| A comparative profile of methanol extracts of Allium cepa and Allium sativum in diabetic neuropathy in mice. | 2010-11 |
|
| Overexpression of inosine 5'-monophosphate dehydrogenase type II mediates chemoresistance to human osteosarcoma cells. | 2010-08-16 |
|
| New trends in nucleoside biotechnology. | 2010-07 |
|
| Multifactorial anticancer effects of digalloyl-resveratrol encompass apoptosis, cell-cycle arrest, and inhibition of lymphendothelial gap formation in vitro. | 2010-04-27 |
|
| Selective inhibition of nicotinamide adenine dinucleotide kinases by dinucleoside disulfide mimics of nicotinamide adenine dinucleotide analogues. | 2009-08-01 |
|
| Ribavirin targets eIF4E dependent Akt survival signaling. | 2008-10-24 |
|
| A kinetic alignment of orthologous inosine-5'-monophosphate dehydrogenases. | 2008-08-19 |
|
| Therapeutic effects of combined treatment with ribavirin and tiazofurin on experimental autoimmune encephalomyelitis development: clinical and histopathological evaluation. | 2008-04-15 |
|
| Treatment of yellow fever. | 2008-04 |
|
| Probing binding requirements of type I and type II isoforms of inosine monophosphate dehydrogenase with adenine-modified nicotinamide adenine dinucleotide analogues. | 2007-11-15 |
|
| Nicotinamide riboside kinase structures reveal new pathways to NAD+. | 2007-10-02 |
|
| Synthesis and antitumour activity of new tiazofurin analogues bearing a 2,3-anhydro functionality in the furanose ring. | 2007-08-01 |
|
| Crystal structure of human nicotinamide riboside kinase. | 2007-08 |
|
| Recent development of IMP dehydrogenase inhibitors for the treatment of cancer. | 2007-07 |
|
| Antiviral activity of tiazofurin and mycophenolic acid against Grapevine leafroll-associated virus 3 in Vitis vinifera explants. | 2007-03 |
|
| Organosilicon-containing thiazole derivatives as potential lipoxygenase inhibitors and anti-inflammatory agents. | 2007 |
|
| 2-(3-Amino-3-deoxy-beta-D-xylofuranosyl)thiazole-4-carboxamide: a new tiazofurin analogue with potent antitumour activity. | 2006-10-15 |
|
| Synthesis and antiproliferative activity of two new tiazofurin analogues with 2'-amido functionalities. | 2006-05-15 |
|
| Synthesis and biological activity of some new 5'-O-acyl tiazofurin derivatives. | 2006-04 |
|
| Resveratrol, an ingredient of wine, acts synergistically with Ara-C and tiazofurin in HL-60 human promyelocytic leukemia cells. | 2006 |
|
| Modulation of cancer pathways by inhibitors of guanylate metabolism. | 2006 |
|
| Metabolic regulation and chemotherapy. | 2006 |
|
| Zinc(II) triflate-controlled 1,3-dipolar cycloadditions of C-(2-thiazolyl)nitrones: application to the synthesis of a novel isoxazolidinyl analogue of tiazofurin. | 2005-10-28 |
|
| Efficient route to C2 symmetric heterocyclic backbone modified cyclic peptides. | 2005-09-29 |
|
| Combination of nucleoside analogues tiazofurin and ribavirin downregulates experimental autoimmune encephalomyelitis. | 2005-06 |
|
| IMP dehydrogenase from the protozoan parasite Toxoplasma gondii. | 2005-06 |
|
| Synergistic action of resveratrol, an ingredient of wine, with Ara-C and tiazofurin in HL-60 human promyelocytic leukemia cells. | 2005-03 |
|
| Metabolism and antiviral activity of ribavirin. | 2005-02 |
|
| Sensitization of human erythroleukemia K562 cells resistant to methotrexate by inhibiting IMPDH. | 2005-01 |
|
| Role of human nucleoside transporters in the cellular uptake of two inhibitors of IMP dehydrogenase, tiazofurin and benzamide riboside. | 2005-01 |
|
| Synthesis of 3'-deoxy-3'-C-hydroxymethyl analogues of tiazofurin and ribavirin. | 2005 |
|
| Down-regulation of increased signal transduction capacity in human cancer cells. | 2005 |
|
| Differentiation of human prostate cancer PC-3 cells induced by inhibitors of inosine 5'-monophosphate dehydrogenase. | 2004-12-15 |
|
| Inhibition of B16 mouse melanoma cell growth and induction of apoptotic cell death with 8-chloroadenosine-3',5'-monophosphate and tiazofurin. | 2004-12 |
|
| Effects of the IMP-dehydrogenase inhibitor, Tiazofurin, in bcr-abl positive acute myelogenous leukemia. Part II. In vitro studies. | 2004-11 |
|
| Effects of the IMP-dehydrogenase inhibitor, Tiazofurin, in bcr-abl positive acute myelogenous leukemia. Part I. In vivo studies. | 2004-11 |
|
| Cryptosporidium parvum IMP dehydrogenase: identification of functional, structural, and dynamic properties that can be exploited for drug design. | 2004-09-24 |
|
| Discoveries of nicotinamide riboside as a nutrient and conserved NRK genes establish a Preiss-Handler independent route to NAD+ in fungi and humans. | 2004-05-14 |
|
| Substitution of the conserved Arg-Tyr dyad selectively disrupts the hydrolysis phase of the IMP dehydrogenase reaction. | 2004-04-20 |
|
| Cofactor mimics as selective inhibitors of NAD-dependent inosine monophosphate dehydrogenase (IMPDH)--the major therapeutic target. | 2004-04 |
|
| A simple assay for determining antiviral activity against Crimean-Congo hemorrhagic fever virus. | 2004-04 |
|
| Anticancer therapeutic potential of soy isoflavone, genistein. | 2004 |
|
| [Application of tiazofurin in the study of regulation of AMP deaminase in intact malignant cells]. | 2002 |
|
| Tiazofurin: molecular and clinical action. | 1996-11-01 |
|
| Antiviral and immunomodulating inhibitors of experimentally-induced Punta Toro virus infections. | 1994-10 |
|
| Clinical toxicity associated with tiazofurin. | 1990-05 |
|
| Reversible cerebral lesions associated with tiazofurin usage: MR demonstration. | 1988-11-01 |
|
| Phase I trial of tiazofurin administered by i.v. bolus daily for 5 days, with pharmacokinetic evaluation. | 1987-02 |
|
| Synergistic antiviral effects of ribavirin and the C-nucleoside analogs tiazofurin and selenazofurin against togaviruses, bunyaviruses, and arenaviruses. | 1984-10 |
|
| Broad-spectrum antiviral activity of 2-beta-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agent. | 1983-09 |
Sample Use Guides
Tiazofurin was given by IV infusion (2200-2700 mg/m2 per day) for up to 10 days. Leukemia blasts rapidly disappeared from the circulation of patients during treatment, while mature myeloid cells in the marrow increased in number. Although these hematologic responses were transient, persisting less than 3-4 weeks, our findings confirm that Tiazofurin has anti-leukemia activity.
Route of Administration:
Intravenous
Concentration of tiazofurin required to reduce the number of cells in a culture by 50% with respect to control cultures was 0.51 uM for Lewis lung carcinoma cell lines (LLAK), 2.6 uM for in vitro cell line (LLTC), and greater than 10 uM for a range of human cancer cell lines. In cytotoxicity assays involving a 2-hour drug exposure followed by clonogenic assay, tiazofurin was more toxic to LLAK cells than to LLTC cells or L1210 murine leukemia cells, consistent with its high in vivo activity against LL. MM-96 human melanoma cells were highly resistant.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 17:57:50 GMT 2025
by
admin
on
Mon Mar 31 17:57:50 GMT 2025
|
| Record UNII |
ULJ82834RE
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Preferred Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NCI_THESAURUS |
C1556
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
||
|
NCI_THESAURUS |
C2087
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
||
|
WHO-VATC |
QL01XX18
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
||
|
FDA ORPHAN DRUG |
139500
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
||
|
WHO-ATC |
L01XX18
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
m10850
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | Merck Index | ||
|
CHEMBL108358
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
100000082162
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
C033706
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
3605
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
457954
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
DB13243
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
90239
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
TIAZOFURIN
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
5220
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
SUB11015MIG
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
286193
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
DTXSID00208827
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
ULJ82834RE
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
60084-10-8
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY | |||
|
C1254
Created by
admin on Mon Mar 31 17:57:50 GMT 2025 , Edited by admin on Mon Mar 31 17:57:50 GMT 2025
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
