129054-67-7

Upstream product

• 75059-22-2 (2R,3S,4S,5R)-2-(6-amino-9H-purine-9-yl)-4-fluoro-5-(hydroxymethyl)tetrahydrofuran-3-ol 
• 98-88-4 benzoyl chloride 
• 1101107-81-6 (3S,4S,5R)-5-((benzyloxy)methyl)-4-fluoro-2-methoxytetrahydrofuran-3-ol 
• 1009818-08-9 (2R,3R,4R)-2-((benzyloxy)methyl)-5-methoxytetrahydrofuran-3,4-diol 
• 123484-12-8 ((2R,3R,4S)-5-acetoxy-4-(benzoyloxy)-3-fluorotetrahydrofuran-2-yl)methyl benzoate 
• 230632-62-9 ((2R,3R,4S,5R)-5-(6-amino-9H-purin-9-yl)-4-(benzoyloxy)-3-fluorotetrahydrofuran-2-yl)methyl benzoate 
• 168918-58-9 C₃₈H₂₈FN₅O₇ 

Downstream Products

• 168918-59-0 N⁶-Benzoyl-3'-fluoro-3'-deoxy-5'-O-(monomethoxytrityl)adenosine 
• 170871-87-1 N-(9-((2R,3S,4S,5R)-5-((bis(4-methoxyphenyl)(phenyl)methoxy)methyl)-4-fluoro-3-hydroxytetrahydrofuran-2-yl)-9H-purin-6-yl)benzamide 
• 168918-63-6 N⁶,N⁶,2'-O-Tribenzoyl-3'-fluoro-3'-deoxyadenosine 
• 168918-65-8 N⁶-Benzoyl-3'-fluoro-3'-deoxy-5'-O-(monomethoxytrityl)adenosine-2'-<2-chlorophenyl 2-(4-nitrophenyl)ethyl phosphate> 
• 168918-61-4 N⁶,N⁶,2'-O-Tribenzoyl-3'-fluoro-3'-deoxy-5'-O-(monomethoxytrityl)adenosine 

Relevant academic research and scientific papers

Solid phase synthesis of 2',5'-oligoadenylates containing 3'-fluorinated ribose

2',5'-phosphodiester bond-linked oligoadenylate trimers with 3'-fluoro- 3'-deoxyadenosine residues incorporated at specific positions of the nucleotide sequence were synthesized by the solid phase phosphite triester (phosphoramidite) method. The syntheses were in the 2' to 5' direction and were performed manually using commercially available microcolumns. The oligonucleotides were 5'-end phosphorylated on the support before deprotection.

Bis 2′-5′-RR-(3′F-A)(3′F-A) cyclic dinucleotide compound and uses thereof

The present invention provides the cyclic dinucleotide compound 2′2′-RR-(3′F-A)(3′F-A) as a highly active immune stimulator that activates DCs via the cytoplasmic receptor known as STING (Stimulator of Interferon Genes), and compositions and uses thereof.

DC-SIGN ANTIBODY CONJUGATES COMPRISING STING AGONISTS

Provided herein are immunoconjugates comprising an anti-DC-SiGN antibody conjugated to a STING agonist. Also disclosed are methods of making the immunoconjugates and methods of treating cancer using the immunoconjugates.

NOVEL STING AGONISTS

The present invention provides compounds of Formula I′: wherein , W, X, Y, Z, Z1, Z2, R1, R2, R3, R4 and R5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.

LOCKED NUCLEIC ACID CYCLIC DINUCLEOTIDE COMPOUNDS AND USES THEREOF

The present invention provides highly active locked nucleic acid cyclic-dinucleotide (LNA-CDN) immune stimulators that activate DCs via the cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the LNA-CDNs of the present in

Role of the stereochemistry of 3'-fluoro-3'-deoxy analogues of 2-5A in binding to and activation of mouse RNase L

The synthesis of two sets of analogues of 2-5A trimer containing 9-(3-fluoro-3-deoxy-β-D-xylo-furanosyl)adenine (AF) or 3'-fluoro-3'-deoxyadenosine (AF) at different positions of the chain is described, along with the preparation of the corresponding 5'-monophosphates and 5'-diphosphorylated (core) trimers.The ability of each ribo and xylo isomeric pair of fluorodeoxy analogues of 2-5A (i) to compete with p3(A2'p)3A3'pC3'p for binding to RNase L in L929 cell extracts, and (ii) to activate the partially purified RNase L from L929 cell extracts to hydrolyze poly(U), was compared to that of the related 3'-deoxy analogue and the parent trimer, p3A3, using radiobinding and RNase L-(2',5')pentaadenylate(core)-agarose assays, respectively.Evidence is presented to show that the stereochemistry of the trimers plays an important role, specifically in the second process.The most striking observation is that, compared to 2-5A, p3A(AF)A was found to be nine times more effective an activator of RNase L, whereas isomeric p3A(AF)A is 30 times less effective.