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Dezaguanine

Dezaguanine is a purine analog. Dezaguanine exhibits antitumor activity in leukemia and breast cancer cells. Dezaguanine can be used in cancer-related research.

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CAS No.: 41729-52-6
Formule: C₆H₆N₄O
Masse moléculaire:150.14

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Dezaguanine Chemical Structure

CAS No.: 41729-52-6

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Dezaguanine is a purine analog. Dezaguanine exhibits antitumor activity in leukemia and breast cancer cells. Dezaguanine can be used in cancer-related research^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
AA6	MIC	0.5 mM Compound: 1	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	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.

Cell Proliferation Assay^[1]

Cell Line:

Wild-type CHO cells, APRTase-deficient CHO AAR-6a cells, HGPRTase-deficient CHO TGR-1 cells
Concentration:

0.01 mM; 0.50 mM; 1.50 mM
Incubation Time:

7 days
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 (intravenous injection/intraperitoneal injection; single dose/5 consecutive days) exhibits an LD₁₀ of 98 mg/kg following a single intravenous administration, and an LD₁₀ of 112 mg/kg/day following daily intraperitoneal administration for 5 consecutive days in mice^[2].
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.

Animal Model:

Beagle^[2]
Dosage:

270 mg/kg (single i.v. dose); 17 mg/kg/day (5-day daily i.v. dose)
Administration:

i.v. (single dose; daily; 5 consecutive days)
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

CAS No. 41729-52-6
Masse moléculaire 150.14
Formule C₆H₆N₄O
SMILES

O=C1NC(N)=CC=2NC=NC12
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Schneller S W, et al. Synthesis and biological evaluation of 6-amino-1H-pyrrolo [3, 2-c] pyridin-4 (5H)-one (3, 7-dideazaguanine). Journal of medicinal chemistry, 1984, 27(12): 1737-1739.

[2]. Margolin K, et al. 3-Deazaguanine: report of a phase I trial and drug-related cardiac toxicity. Invest New Drugs. 1990;8(4):369-376. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

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100 mg

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