Thioguanine

Catalog No.S1774

Thioguanine, a purine antimetabolite, inhibits DNMT1 activity through ubiquitin-targeted degradation, used in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohn's disease, rheumatoid arthritis) and organ transplant recipients.

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Thioguanine Chemical Structure

Thioguanine Chemical Structure
Molecular Weight: 167.19

Validation & Quality Control

MSDS

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Product Description

Biological Activity

Description Thioguanine, a purine antimetabolite, inhibits DNMT1 activity through ubiquitin-targeted degradation, used in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohn's disease, rheumatoid arthritis) and organ transplant recipients.
Targets DNMT1 [6]
In vitro Thioguanine incorporation alters the DNA cleavage induced by topoisomerase II in the presence and absence of etoposide. [1] 6-Thioguanine alters the structure and lowers the thermal stability of duplex DNA, but duplex DNA can be formed in the presence of 6SG. [2] 6-Thioguanine induced apopotosis is similarly observed in both mismatch repair-proficient and -deficient HCT116 and HeLa cells. [3] Thioguanine integrates into DNA and unlike the canonical DNA bases, it is a strong UVA chromophore with an absorbance maximum at 342 nm. 6-Thioguanine is a photosensitizer and a source of reactive oxygen species. [4] In canine lymphoma cells, Thioguanine significantly decreases DNMT1 protein and global DNA methylation. [6]
In vivo Thioguanine is as efficient as a PARP inhibitor in selectively killing BRCA2-defective tumors in a xenograft model. 6-Thioguanine efficiently kills such BRCA1-defective PARP inhibitor-resistant tumors. 6-Thioguanine could kill cells and tumors that have gained resistance to PARP inhibitors or cisplatin through genetic reversion of the BRCA2 gene. [5]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Krynetskaia NF, et al. FASEB J,2000, 14(14), 2339-2344.

[2] Marathias VM, et al. Nucleic Acids Res,1999, 27(14), 2860-2867.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-03-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02101853 Suspended Adult B Acute Lymphoblastic Leukemia|Childhood B Acute Lymphoblastic Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Childhood Acut  ...more Adult B Acute Lymphoblastic Leukemia|Childhood B Acute Lymphoblastic Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia National Cancer Institute (NCI) December 2014 Phase 3
NCT02112916 Recruiting Adult T Acute Lymphoblastic Leukemia|Childhood T Acute Lymphoblastic Leukemia|Stage II Childhood Lymphoblastic Lymphoma|Stage II Contiguous Adult L  ...more Adult T Acute Lymphoblastic Leukemia|Childhood T Acute Lymphoblastic Leukemia|Stage II Childhood Lymphoblastic Lymphoma|Stage II Contiguous Adult Lymphoblastic Lymphoma|Stage II Non-Contiguous Adult Lymphoblastic Lymphoma|Stage III Adult Lymphoblastic Lymphoma|Stage III Childhood Lymphoblastic Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Childhood Lymphoblastic Lymphoma|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia National Cancer Institute (NCI) September 2014 Phase 3
NCT02141100 Not yet recruiting Non-Hodgkin Lymphoma Kjeld Schmiegelow|Aalborg Universitetshospital |Aarhus U  ...more Kjeld Schmiegelow|Aalborg Universitetshospital |Aarhus University Hospital Skejby|Odense University Hospital|Rigshospitalet, Denmark July 2014 Phase 1|Phase 2
NCT01451515 Recruiting Lymphoblastic Lymphoma St. Jude Childrens Research Hospital|National University,  ...more St. Jude Childrens Research Hospital|National University, Singapore May 2012 Phase 2
NCT01406756 Recruiting B-cell Adult Acute Lymphoblastic Leukemia|B-cell Childhood Acute Lymphoblastic Leukemia|Cognitive/Functional Effects|Neurotoxicity|Pain|Philadelphi  ...more B-cell Adult Acute Lymphoblastic Leukemia|B-cell Childhood Acute Lymphoblastic Leukemia|Cognitive/Functional Effects|Neurotoxicity|Pain|Philadelphia Chromosome Positive Childhood Precursor Acute Lymphoblastic Leukemia|Therapy-related Toxicity|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia Childrens Oncology Group|National Cancer Institute (NCI) February 2012 Phase 3

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Chemical Information

Download Thioguanine SDF
Molecular Weight (MW) 167.19
Formula

C5H5N5S

CAS No. 154-42-7
Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms
Solubility (25°C) * In vitro Ethanol <1 mg/mL (<1 mM)
DMSO <1 mg/mL (<1 mM)
Water <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-​amino-​1,​9-​dihydro-6H-​purine-​6-​thione

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