8-Azaadenosine is a potent ADAR1 inhibitor. 8-Azaadenosine is an A-to-I editing inhibitor. 8-Azaadenosine blocks RNA editing and inhibits proliferation, 3D growth, invasion, and migration of thyroid cancer cells.

Physicochemical Properties

Molecular Formula	C9H12N6O4
Molecular Weight	268.23
Exact Mass	268.092
CAS #	10299-44-2
PubChem CID	96410
Appearance	White to off-white solid powder
Density	2.29 g/cm3
Boiling Point	702.6ºC at 760 mmHg
Flash Point	378.7ºC
Vapour Pressure	1.01E-20mmHg at 25°C
Index of Refraction	2
LogP	-2.2
Hydrogen Bond Donor Count	4
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	2
Heavy Atom Count	19
Complexity	336
Defined Atom Stereocenter Count	4
SMILES	C1=NC(=C2C(=N1)N(N=N2)[C@H]3[C@@H]([C@@H]([C@H](O3)CO)O)O)N
InChi Key	OAUKGFJQZRGECT-UUOKFMHZSA-N
InChi Code	InChI=1S/C9H12N6O4/c10-7-4-8(12-2-11-7)15(14-13-4)9-6(18)5(17)3(1-16)19-9/h2-3,5-6,9,16-18H,1H2,(H2,10,11,12)/t3-,5-,6-,9-/m1/s1
Chemical Name	(2R,3R,4S,5R)-2-(7-aminotriazolo[4,5-d]pyrimidin-3-yl)-5-(hydroxymethyl)oxolane-3,4-diol
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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	8-Azaadenosine does not alter the levels of ADAR1 mRNA; instead, it solely targets the activity of ADAR (adenosine deaminases acting on double-stranded RNA)[1][2]. After two weeks in stromal co-culture, 8-adenosine (10–25 nM) restores let-7 miRNA biogenesis in proportion to a decrease in ADAR1 expression, RNA editing activity, and LIN28B expression in JAK2/BCR-ABL1 transduced progenitors[1]. Based on qRT-PCR and Western blot analysis of p-CRKL and p-STAT5a, 8-azaadenosine (10, 100 nM) has no effect on BCR-ABL and JAK2 signaling[1]. In TPC1 and Cal62 cells, 8-azaadenosine (0.1, 0.5, 1, 2 µM; 5 days) reduces cell viability/proliferation in a dose-dependent manner[2]. 8-Azaadenosine (1, 2 µM; 16 hours) inhibits TPC1 and Cal62 cell invasion and migration[2]. In TPC1 and Cal62 cells, 8-azaadenosine (1, 2 µM) suppresses the editing activity. In contrast, both cell lines' levels of ADAR1 mRNA stay constant[2].
References	[1]. ADAR1 Activation Drives Leukemia Stem Cell Self-Renewal by Impairing Let-7 Biogenesis. Cell Stem Cell. 2016 Aug 4;19(2):177-191. [2]. ADAR1-mediated RNA editing is a novel oncogenic process in thyroid cancer and regulates miR-200 activity. Oncogene. 2020 Apr;39(18):3738-3753.
Additional Infomation	8-Azaadenosine is a N-glycosyl compound.

Solubility Data

Solubility (In Vitro)

DMSO: 250 mg/mL (932.04 mM) H2O: 3.33 mg/mL (12.41 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (7.75 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 (7.75 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. Solubility in Formulation 3: ≥ 2.08 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.7281 mL	18.6407 mL	37.2814 mL
	5 mM	0.7456 mL	3.7281 mL	7.4563 mL
	10 mM	0.3728 mL	1.8641 mL	3.7281 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.