Dezaguanine
Dezaguanine is a purine analog. Dezaguanine exhibits antitumor activity in leukemia and breast cancer cells. Dezaguanine can be used in cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 41729-52-6
- Formula: C6H6N4O
- Molecular Weight:150.14
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AA6 | MIC |
0.5 mM
Compound: 1
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Ability to inhibit growth of AA-6 cells (a mutant cell line resistant to 8-azaadenine and lacks adenine phosphoryltransferase) was determined
Ability to inhibit growth of AA-6 cells (a mutant cell line resistant to 8-azaadenine and lacks adenine phosphoryltransferase) was determined
|
[PMID: 6438321] |
| CV-1 | CC50 |
250 μM
Compound: 3-deazaguanine
|
Cytotoxicity against African green monkey CV1 cells
Cytotoxicity against African green monkey CV1 cells
|
[PMID: 26260336] |
| CV-1 | IC50 |
4.1 μM
Compound: 3-deazaguanine
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Antiviral activity against Measles virus infected in African green monkey CV1 cells after 3 days by neutral red dye-based plaque reduction assay
Antiviral activity against Measles virus infected in African green monkey CV1 cells after 3 days by neutral red dye-based plaque reduction assay
|
[PMID: 26260336] |
| L1210 | ED50 |
11 μM
Compound: 3-deazaguanine
|
Effective dose that produced 50% inhibition of L1210 Leukemia cell growth in culture
Effective dose that produced 50% inhibition of L1210 Leukemia cell growth in culture
|
[PMID: 6827548] |
| MOLT-4 | IC50 |
3.7 μM
Compound: 1
|
Compound was tested for inhibition of MOLT-4 cell growth using human lymphoblast cytotoxicity assay in the absence of 2''-deoxy guanosine, cytotoxicity determined by monitoring uptake of [3H]thymidine
Compound was tested for inhibition of MOLT-4 cell growth using human lymphoblast cytotoxicity assay in the absence of 2''-deoxy guanosine, cytotoxicity determined by monitoring uptake of [3H]thymidine
|
[PMID: 3093681] |
| MOLT-4 | IC50 |
5.9 μM
Compound: 1
|
Compound was tested for inhibition of MOLT-4 cell growth using human lymphoblast cytotoxicity assay in the presence of 2''-deoxy guanosine, cytotoxicity determined by monitoring uptake of [3H]thymidine
Compound was tested for inhibition of MOLT-4 cell growth using human lymphoblast cytotoxicity assay in the presence of 2''-deoxy guanosine, cytotoxicity determined by monitoring uptake of [3H]thymidine
|
[PMID: 3093681] |
In Vitro
Dezaguanine (0.1-150 μg/mL) inhibits virus-induced cytopathic effects in primary rabbit kidney cells, Vero cells and HeLa cells, with an IC50 range of 0.1 to 150 μg/mL against all tested viruses[1].
Dezaguanine (0.01-1.50 mM; 7 days) inhibits the growth of wild-type CHO cells, APRT-deficient CHO AAR-6a cells, and HGPRT-deficient CHO TGR-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Wild-type CHO cells, APRTase-deficient CHO AAR-6a cells, HGPRTase-deficient CHO TGR-1 cells
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Concentration:0.01 mM; 0.50 mM; 1.50 mM
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Incubation Time:7 days
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Result:Inhibited growth with a minimum inhibitory concentration of 0.01 mM in wild-type CHO cells.
Inhibited growth with a minimum inhibitory concentration of 0.50 mM in APRTase-deficient CHO AAR-6a cells.
Inhibited growth with a minimum inhibitory concentration of 1.50 mM in HGPRTase-deficient CHO TGR-1 cells.
In Vivo
Dezaguanine (17-270 mg/kg; intravenous injection; single dose/5 consecutive days) only causes mild gastrointestinal reactions in Beagle dogs at a single intravenous dose of 270 mg/kg, whereas the 17 mg/kg dose administered intravenously for 5 consecutive days is lethal[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Beagle[2]
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Dosage:270 mg/kg (single i.v. dose); 17 mg/kg/day (5-day daily i.v. dose)
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Administration:i.v. (single dose; daily; 5 consecutive days)
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Result:Caused only mild emesis and anorexia, with no detectable organ toxicities via biochemical or histological evaluation (single i.v. 270 mg/kg dose).
Was lethal, with death secondary to necrotizing enteritis and myelosuppression (5-day daily i.v. 17 mg/kg dose).
Chemical Information
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CAS No. 41729-52-6
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Molecular Weight 150.14
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Formula C6H6N4O
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SMILES
O=C1NC(N)=CC=2NC=NC12
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)