cd73-in-1

CD73-IN-1 is a CD73 inhibitor with anticancer activity.

CD73-IN-12 is a highly effective CD73 inhibitor that displays strong potential in tumor suppression. CD73, an enzyme intricately linked to tumor development, angiogenesis, and metastasis, is significantly inhibited by CD73-IN-12. This compound holds promise in the formulation of therapeutic medications targeting tumor-related diseases[1].

CD73-IN-10 can be used in preparing tumor-related diseases medicament. CD73-IN-10 is a potent CD73 inhibitor that can catalyze the adenosine production from extracellular 5'-phosphate adenosine (5'-AMP). Adenosine induces immunosuppression and can promote tumor proliferation and or metastasis [1].

CD73-IN-13 is able to be used in a medicament preparing for tumor-related diseases. CD73-IN-13 is a potent inhibitor of CD73 which is closely associated with tumor growth, angiogenesis and metastasis [1].

CD73-IN-11 is able to used for tumor-related diseases medicament preparing. CD73-IN-11 is an effective CD73 inhibitor. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP) which induce immunosuppression and promote tumor proliferation and or metastasis [1].

CD73-IN-17 (compound 19) is an inhibitor of CD73 with an IC50 of 0.1 μM against hCD73. It is applicable in cancer research.

CD73-IN-16 (compound 18) acts as an inhibitor of hCD73, exhibiting an IC50 value of 0.28 μM.

CD73-IN-18 (compound 35j) is an orally effective inhibitor of the extracellular 5'-nucleotidase (CD73) enzyme. It can be utilized in anticancer research.

CD73-IN-19 (Compound 4ab) is an inhibitor of CD73, demonstrating a 44% inhibition rate of CD73 enzyme activity at 100 μM. It entirely counters T cell proliferation blockade triggered by TCR activation (induced by CD73 activity) at 10 μM and 100 μM and inhibits hA2A receptor activity in HEK-293 cells with a Ki of 3.31 μM. CD73-IN-19 holds potential for research in the field of immune diseases.

Adenosine 5'-methylenediphosphate is an inhibitor of ecto-5'-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5'-monophosphate , adenosine 5'-diphosphate , or adenosine 5'-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5'-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) cells in a migration assay.2,3It increases tumor infiltration of CD3+CD8+T cells and reduces tumor growth in a K1735 murine melanoma model when administered at a dose of 400 μg mouse.4 1.Bruns, R.F.Adenosine receptor activation by adenine nucleotides requires conversion of the nucleotides to adenosineNaunyn Schmiedebergs Arch. Pharmacol.315(1)5-13(1980) 2.Braganhol, E., Tamajusuku, A.S.K., Bernardi, A., et al.Ecto-5′-nucleotidase CD73 inhibition by quercetin in the human U138MG glioma cell lineBiochim. Biophys. Acta1770(9)1352-1359(2007) 3.Shali, S., Yu, J., Zhang, X., et al.Ecto 5′ nucleotidase (CD73) is a potential target of hepatocellular carcinomaJ. Cell Physiol.234(7)10248-10259(2018) 4.Forte, G., Sorrentino, R., Montinaro, A., et al.Inhibition of CD73 improves B cell-mediated anti-tumor immunity in a mouse model of melanomaJ. Immunol.189(5)2226-2233(2021)

PSB-12379 disodium is a nucleotide analogue acting as a potent inhibitor of Ecto-5'-Nucleotidase (CD73), demonstrating inhibitory constants (Ki) of 9.03 nM in rats and 2.21 nM in humans [1] [2].

CD73-IN-8, a potent CD73 inhibitor, prevents the catalytic activity of CD73, an enzyme responsible for converting extracellular 5'-phosphate adenosine (5'-AMP) to adenosine. Adenosine, once produced, can induce immunosuppressive effects and facilitate tumor proliferation and or metastasis. Therefore, CD73-IN-8 holds promise in the development of therapeutic interventions for tumor-related diseases[1].

CD73-IN-7 is a potent CD73 inhibitor used for preparing medications for tumor-related diseases. CD73 catalyzes the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), inducing immunosuppressive effects and promoting tumor proliferation and or metastasis [1].

Uliledlimab, a humanized monoclonal antibody, exhibits potent activity against CD73, inhibiting the conversion of extracellular adenosine monophosphate (AMP) to adenosine. It holds potential for use in cancer research [1].

CD73-IN-9, a potent CD73 inhibitor, is used in preparing medication for tumor-related diseases. CD73 catalyzes the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), which can induce immunosuppressive effects and promote tumor proliferation and or metastasis [1].

CD73-IN-6, serves as a potent inhibitor of CD73. This compound finds utility in cancer research [1].

ORIC-533 is a selective CD73 inhibitor that is orally active and competes with AMP. It revitalizes the proliferation and activation of immunosuppressed CD8+ T cells and induces notable lysis and cell death in multiple myeloma cells within the bone marrow microenvironment [1].