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| Targets |
mTOR
The primary targets of 8-Aminoadenosine include DNA/RNA synthesis, Akt, mTOR, autophagy, and apoptosis pathways. It is an RNA-directed nucleoside analog that reduces cellular ATP levels and inhibits mRNA synthesis. The compound blocks Akt/mTOR signaling and induces p53-independent autophagy and apoptosis. It has antitumor activity against various cancer cell lines. |
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| ln Vitro |
In MM.1S and U266 cells, 8-aminoadenosine (8-NH2-Ado; 0.1-10 μM; for 48 h) has IC50s of 1.5 μM and 8.88 μM, respectively[1]. 8-Aminoadenosine (10 μM; for 24 hours) significantly causes MCF-7 cells to undergo apoptosis through a p53-independent mechanism. In MCF-7 cells, 8-adenosine triggers PARP cleavage[2]. In the MM.1S cell line, 8-aminoadenosine (3 μM; 0.5–4 h) initiates autophagy[1]. In MM.1S cells, 8-adenosine (3 μM; 2–16 h) results in a higher decrease in ATP levels[1]. In MM.1S cells, 8-aminoadenosine (3 μM; 5 h) reduces glucose intake by 50%[1]. In MM.1S cells, 8-aminoadenosine (3 μM; 5 h) shows a time-dependent drop in GLUT1 expression at 5 h, while both transporters (GLUT1 and GLUT4) were down-regulated at 24 h[1]. In addition to inhibiting cell growth and activating cell death, 8-aminoadenosine does not enhance the levels of either p53 or p21 protein or stimulate transcription of the p53 target gene, p21[1]. In cells lacking adenosine kinase, the conversion of 8-Aminoadenosine to 8-NH2-ATP is necessary to counteract the harmful effects of 8-Aminoadenosine[1].
In vitro, 8-Aminoadenosine (0.1-10 μM; for 48 h) has IC50s of 1.5 μM and 8.88 μM in MM.15 and U266 cells, respectively. It induces significant apoptotic death of MCF-7 cells in a p53-independent pathway at 10 μM for 24 h. The compound induces autophagy in the MM.15 cell line at 3 μM and causes a greater drop in ATP levels in MM.15 cells. It also causes a 50% reduction in glucose consumption in MM.15 cells at 3 μM. |
| ln Vivo |
In vivo activity of 8-Aminoadenosine has been demonstrated in preclinical studies against hematologic malignancies and solid tumors. The compound is rapidly phosphorylated within cells and incorporated into RNA, disrupting transcription and inducing apoptosis in cancer cells. It has shown promise in preclinical studies against various cancer types. However, detailed in vivo efficacy data are limited in the available literature.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for 8-Aminoadenosine are not well established, as the compound is a nucleoside analog that exerts its effects through incorporation into RNA and inhibition of mRNA synthesis rather than direct enzyme inhibition. The compound's effects on ATP levels and glucose consumption are measured in cellular assays.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: MM.1S and U266 cells Tested Concentrations: 0.1, 0.3, 1, 3, 10 μM Incubation Duration: For 48 hrs (hours) Experimental Results: Had IC50s of 1.5 μM and 8.88 μM in MM.1S and U266 cells, respectively. Apoptosis Analysis[2] Cell Types: MCF-7 cells Tested Concentrations: 10 μM Incubation Duration: For 24 hrs (hours) Experimental Results: Induced significant apoptotic death. Apoptosis was not inhibited by knockdown of functional p53. Apoptosis Analysis[1] Cell Types: MM.1S cell line Tested Concentrations: 3 μM Incubation Duration: 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4 hrs (hours) Experimental Results: Induced the formation of LC3-II protein. Caused the appearance of a population with a high AVO content with 1 μM for 24 hrs (hours). In vitro cellular assays for 8-Aminoadenosine involve testing its anticancer activity against various cancer cell lines. Cells are treated with serial dilutions of 8-Aminoadenosine (0.1-10 µM) for 24-48 hours. Cell viability is assessed using MTT or CCK-8 assays. Apoptosis is measured by Annexin V/PI staining and caspase activity assays. Autophagy is assessed by LC3-II accumulation and autophagosome formation. ATP levels and glucose consumption are measured using biochemical assays. The compound demonstrates concentration-dependent anticancer activity. |
| Animal Protocol |
In vivo animal studies for 8-Aminoadenosine involve efficacy testing in tumor-bearing models. Mice implanted with cancer cells are treated with 8-Aminoadenosine via intraperitoneal or intravenous administration at various doses. Tumor volume and body weight are monitored over 2-4 weeks. Apoptosis and autophagy markers in tumors are assessed by immunohistochemistry or Western blot. The compound demonstrates antitumor activity in preclinical models.
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| ADME/Pharmacokinetics |
8-Aminoadenosine has a molecular formula of C10H14N6O4 and a molecular weight of 282.26. It appears as a solid with a purity of ≥98%. The compound is soluble in DMSO at 83.33 mg/mL (295.22 mM). It is stable as a powder at -20°C for 3 years and at 4°C for 2 years; in solvent, it is stable at -80°C for 6 months and at -20°C for 1 month. It is intended for research use only and is not for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of 8-Aminoadenosine has not been extensively characterized. As a nucleoside analog, it may have myelosuppressive and gastrointestinal side effects similar to other antimetabolites. Standard toxicity studies would include assessment of body weight changes, hematological parameters, and histopathological examination of major organs in animal models. The compound is intended for research use only and is not approved for clinical use.
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| References |
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| Additional Infomation |
8-Aminoadenosine (CAS 3868-33-5) is an RNA-directed nucleoside analog that reduces cellular ATP levels and inhibits mRNA synthesis. It has a molecular formula of C10H14N6O4 and a molecular weight of 282.26. The compound blocks Akt/mTOR signaling and induces p53-independent autophagy and apoptosis. It has antitumor activity against various cancer cell lines with IC50s of 1.5 μM and 8.88 μM in MM.15 and U266 cells, respectively. It is intended for research use only and is not approved for clinical use.
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| Molecular Formula |
C10H14N6O4
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|---|---|
| Molecular Weight |
282.26
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| Exact Mass |
282.108
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| CAS # |
3868-33-5
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| PubChem CID |
96851
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| Appearance |
White to off-white solid powder
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| Density |
2.25g/cm3
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| Boiling Point |
747.1ºC at 760mmHg
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| Melting Point |
180-185ºC dec.
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| Flash Point |
405.6ºC
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| LogP |
-1.4
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
363
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1=NC(=C2C(=N1)N(C(=N2)N)[C@H]3[C@@H]([C@@H]([C@H](O3)CO)O)O)N
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| InChi Key |
DVGWFQILDUEEGX-UUOKFMHZSA-N
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| InChi Code |
InChI=1S/C10H14N6O4/c11-7-4-8(14-2-13-7)16(10(12)15-4)9-6(19)5(18)3(1-17)20-9/h2-3,5-6,9,17-19H,1H2,(H2,12,15)(H2,11,13,14)/t3-,5-,6-,9-/m1/s1
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| Chemical Name |
(2R,3R,4S,5R)-2-(6,8-diaminopurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 83.33 mg/mL (295.22 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5428 mL | 17.7142 mL | 35.4283 mL | |
| 5 mM | 0.7086 mL | 3.5428 mL | 7.0857 mL | |
| 10 mM | 0.3543 mL | 1.7714 mL | 3.5428 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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