8-aminoadenosine

8-Aminoadenosine (8-NH2-Ado) is an RNA-directed purine nucleoside analog under preclinical investigation for the treatment of various hematological malignancies and solid tumors, including multiple myeloma, chronic lymphocytic leukemia, mantle cell lymphoma, chronic myelogenous leukemia, breast cancer, and lung cancer. It is metabolized intracellularly by adenosine kinase into its active triphosphate form, 8-amino-ATP. This active metabolite competes with ATP, leading to a depletion of the cellular ATP pool and direct incorporation into nascent mRNA transcripts, which causes premature transcription termination and inhibition of RNA synthesis. Additionally, 8-aminoadenosine inhibits key survival pathways, including Akt/mTOR and ERK signaling, and induces p53-independent apoptosis and autophagy.

Other names

6,8-diamino-9-beta-D-ribofuranosyl-9H-purine8-NH2-Ado8-amino-D-adenosine8-amino-adenosine