Size | Price | Stock | Qty |
---|---|---|---|
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
Other Sizes |
|
Azacitidine (Ladakamycin; 5-AzaC):Nature. 2021 Aug 25. doi: 10.1038/s41586-021-03850-3.
Purity: ≥98%
5-Azacytidine (5AzaC; Ladakamycin; U-18496; Vidaza; Mylosar; 5-AzaC) is an FDA approved anticancer drug bearing a pyrimidine nucleoside core and belongs to cytosine class of antimetabolites. It acts as a DNA methyl transferase (DNMT) inhibitor.
ln Vitro |
Unmethylated CpG islands associated with a number of genes are partially or fully methylated in malignancies and can be reactivated by 5-Azacytidine [1]. 5-Azacytidine works as a mild inducer of erythroid differentiation of Friend erythroleukemia cells within the same dose range that influences DNA methyltransferase activity [2]. 5-Azacytidine inhibits L1210 cells with ID50 and ID90 values of 0.019 and ~0.15 μg/mL, respectively [3].
|
||
---|---|---|---|
ln Vivo |
TdR-3H incorporation was markedly decreased when rats were treated to 5-Azacytidine (100 mg/kg, i.p.) for two hours or longer [3].
|
||
Animal Protocol |
|
||
References |
[1]. Christman JK. 5-Azacytidine and 5-aza-2'-deoxycytidine as inhibitors of DNA methylation: mechanistic studies and their implications for cancer therapy. Oncogene. 2002 Aug 12;21(35):5483-95.
[2]. Creusot F, et al. Inhibition of DNA methyltransferase and induction of Friend erythroleukemia cell differentiation by 5-azacytidineand 5-aza-2'-deoxycytidine. J Biol Chem. 1982 Feb 25;257(4):2041-8. [3]. Li LH,et al. Cytotoxicity and mode of action of 5-azacytidine on L1210 leukemia. Cancer Res. 1970 Nov;30(11):2760-9. [4]. Marycz K, et al. 5-Azacytidine and Resveratrol Enhance Chondrogenic Differentiation of Metabolic Syndrome-Derived Mesenchymal Stem Cells by Modulating Autophagy.Oxid Med Cell Longev. 2019 May 12;2019:1523140 |
Molecular Formula |
C8H12N4O5
|
|
---|---|---|
Molecular Weight |
244.2
|
|
CAS # |
320-67-2
|
|
Related CAS # |
|
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
|
SMILES |
O=C1N([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)C=NC(N)=N1
|
|
Chemical Name |
4-amino-1-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1,3,5-triazin-2(1H)-one
|
|
Synonyms |
Vidaza; Abbreviations: 5AC; 5AZC. U 18496; U18496; 5-azacytidine; azacytidine; U-18496; ladakamycin. US brand names: Mylosar;
|
|
HS Tariff Code |
2934.99.9001
|
|
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)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% propylene glycol, 5% Tween 80, 65% D5W:30mg/mL Solubility in Formulation 5: 20 mg/mL (81.90 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.0950 mL | 20.4750 mL | 40.9500 mL | |
5 mM | 0.8190 mL | 4.0950 mL | 8.1900 mL | |
10 mM | 0.4095 mL | 2.0475 mL | 4.0950 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT06190067 | Recruiting | Drug: Azacitidine Plus PD-1 therapy | Relapsed Classic Hodgkin Lymphoma Refractory Classic Hodgkin Lymphoma |
Navy General Hospital, Beijing | October 30, 2023 | Phase 2 |
NCT03466294 | Active, not recruiting | Drug: Azacitidine and Venetoclax | Acute Myeloid Leukemia | University of Colorado, Denver | May 15, 2018 | Phase 2 |
NCT04891068 | Recruiting | Drug: Azacitidine | Breast Cancer Female Breast Cancer Invasive |
University of Illinois at Chicago | January 10, 2022 | Phase 2 |
NCT04187703 | Recruiting | Drug: 5-azacytidine Drug: Decitabine |
Myelodysplastic Syndromes MDS/MPN Crossover Syndromes |
Benjamin Tomlinson | November 16, 2020 | Early Phase 1 |