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

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)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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,?000, 14(14), 2339-2344.

[2] Marathias VM, et al. Nucleic Acids Res,?999, 27(14), 2860-2867.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02723994 Not yet recruiting B-cell Acute Lymphoblastic Leukemia Incyte Corporation|Childrens Oncology Group August 2016 Phase 2
NCT02419469 Recruiting Leukemia|Precursor-B Acute Lymphoblastic Leukemia|Lymphoblastic Lymphoma|Lymphoma M.D. Anderson Cancer Center|Jazz Pharmaceuticals November 2015 Phase 2
NCT02521493 Recruiting Childhood Acute Myeloid Leukemia|Childhood Myelodysplastic Syndrome|Cytopenia|Down Syndrome|Myeloid Leukemia Associated With Down Syndrome|Myelopro  ...more Childhood Acute Myeloid Leukemia|Childhood Myelodysplastic Syndrome|Cytopenia|Down Syndrome|Myeloid Leukemia Associated With Down Syndrome|Myeloproliferative Neoplasm Childrens Oncology Group|National Cancer Institute (NCI) November 2015 Phase 3
NCT02101853 Recruiting 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

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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
Synonyms N/A
Solubility (25°C) * In vitro DMSO <1 mg/mL (<1 mM)
Water <1 mg/mL (<1 mM)
Ethanol <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

Tech Support

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