(Rp,Rp)-10

(Rp,Rp)-10 is a stereopure, alkyne-conjugated, esterase-sensitive prodrug of the deoxyribose cyclic dinucleotide (dCDN) 3',3'-c-di-dAMP. It acts as a potent agonist of the Stimulator of Interferon Genes (STING) pathway. By utilizing a phosphotriester modification with specific (Rp,Rp) chirality, the molecule exhibits enhanced cellular permeability and stability compared to its parent CDN. Upon enzymatic cleavage by intracellular esterases, it releases the active CDN, leading to robust activation of the TBK1/IRF3 signaling axis and subsequent production of Type I interferons (e.g., IFN-β). In preclinical models of colon carcinoma, (Rp,Rp)-10 has demonstrated superior antitumor efficacy, achieving high rates of complete tumor regression and inducing long-term immunological memory.

Other names

(Rp,Rp)-isomer of alkyne-conjugated dCDN prodrug 10(Rp,Rp)-phosphotriester dCDN prodrug