CD73-IN-5 is a highly potent and selective small molecule inhibitor of CD73, demonstrating non-nucleotide characteristics. It exerts its inhibitory effects with a remarkable IC50 value of 19 nM.

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-4 is a potent and selective methylenephosphonic acid CD73 inhibitor

CD73-IN-7 is a potent CD73 inhibitor that can be used for preparing a medicament for tumor-related diseases. CD73 can catalyze 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-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-9 is a potent CD73 inhibitor that be used in preparing the tumor-related diseases medicament. CD73 can catalyze the adenosine production from extracellular 5'-phosphate adenosine (5'-AMP). The adenosine 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].

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-1 is a CD73 inhibitor with anticancer activity.

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-2 is a potent inhibitor of CD73 (IC50: 0.09 nM).

CD73-IN-3 (LY-3475070) is a potent and selective CD73 inhibitor with an IC50 of 28 nM, and its use alone or in combination with pembrolizumab is currently being tested in patients with advanced cancer.

PSB-12379 ditriethylamine salt, a nucleotide analogue, is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).

MethADP (Adenosine 5'-(α,β-methylene)diphosphate) is a specific CD73 inhibitor that inhibits the enzyme ecto-5′-nucleotidase (ecto), which has been used in the study of neurological and cardiovascular diseases.

Dresbuxelimab (AK-119), an IgG-κ monoclonal antibody, selectively targets CD73 and is commonly produced using a Chinese Hamster Ovary (CHO) cell expression system [1].

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)

Mupadolimab (CPI-006) is a humanized FC-γR binding deficient IgG1 anti-CD73 antibody with potential anticancer activity and activation of CD73POS B cells.

Oleclumab (MEDI9447), a human IgG1λ monoclonal antibody, targets and inhibits CD73 functionality, demonstrating anti-tumor activity [1].

5′-Nucleotidase (CD73), an ectoenzyme and intrinsic membrane glycoprotein, catalyzes the hydrolysis of 5-nucleotides into their corresponding nucleosides [1].

MethADP is a specific CD73 inhibitor.

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].

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].

AB-680 ammonium is a potent, reversible, and selective CD73 inhibitor (an ecto-nucleotidase), demonstrating a K i of 4.9 pM against hCD73 and exhibiting more than 10,000-fold selectivity over the related ecto-nucleotidase CD39, along with anti-tumor activity [1].

PSB-12379 is a potent inhibitor of Ecto-5'-Nucleotidase (CD73)(Kis of 9.03 nM (rat) and 2.21 nM (human)).

BK50164, a potent CD73 inhibitor, exhibits an IC50 of 13.089 µM and demonstrates affinity for CD99 with a KD value of 1.5 µM. This compound not only possesses antiproliferative activity but also induces apoptosis and cell cycle arrest at the Sub-G1 phase [1].

Dalutrafusp alfa (AGEN-1423; GS-1423) is a bifunctional antibody targeting CD73 and TGF-β, components of the immunosuppressive pathway [1].

AB-680 is a highly potent, reversible, and selective inhibitor of CD73 (an ectonucleotidase, Ki: 4.9 pM for hCD73) with anti-tumor activity, displays >10,000-fold selectivity over related ectonucleotidases CD39.

OP-5244 sodium is a potent, orally active inhibitor of CD73 (IC50: 0.25 nM). OP-5244 sodium has shown potential for cancer research by blocking adenosine production and thereby reversing immunosuppression.

AMPCP is an Ecto-5'-nucleotidase (CD73) inhibitor.

PSB-12489 is an optimized inhibitor of CD73.

OP-5244 has comparable potency to bisphosphonic acid series and targets CD73.

ZM514 is a potent inhibitor of CD73, acting on hCD73 (IC50: 1.39 μM) and mCD73 (IC50: 14.65 μM). zM514 has low cytotoxicity and can be used in anti-cancer studies.