cd73 in 5

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.

MethADP (Adenosine 5'-(α,β-methylene)diphosphate) 是一种特异性的 CD73 抑制剂，抑制 ecto-5′-核苷酸酶 （ecto），可用于研究神经系统疾病和心血管疾病。

CD73-IN-18（化合物35j）是一种高效的口服胞外5-核苷酸酶(CD73)抑制剂，主要应用于癌症治疗的研究领域。

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)

CD73-IN-7 是一种有效的CD73抑制剂，可用于制备治疗肿瘤相关疾病的药物。CD73 催化细胞外5'-磷酸腺苷 (5'-AMP) 产生腺苷，从而诱导免疫抑制作用并促进肿瘤增殖和 或转移。

CD73-IN-9 是 CD73 的有效抑制剂，可用于制备治疗肿瘤相关疾病的药物。CD73 可以催化细胞外5'-磷酸腺苷 (5'-AMP) 产生腺苷。腺苷能够诱导免疫抑制作用，并且促进肿瘤增殖和 或转移。

CD73-IN-10 可用于肿瘤相关疾病药物的制备。CD73-IN-10 是 CD73的有效抑制剂， 能够催化细胞外5'-磷酸腺苷 (5'-AMP) 产生腺苷。腺苷具有诱导免疫抑制的作用，能够促进肿瘤增殖和 或转移。

CD73-IN-11 可用于肿瘤相关疾病的药物制备。CD73-IN-11 是 CD73的有效抑制剂。CD73 可以催化细胞外5'-磷酸腺苷 (5'-AMP) 产生腺苷，从而诱导免疫抑制并促进肿瘤增殖和 或转移。

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].

PSB-12379 disodium 是一种核苷类似物，是一种有效的 Ecto-5'-Nucleotidase(CD73) 抑制剂，Kis 值为 9.03 nM (鼠) 和 2.21 nM (人)。

CD73-IN-4 是高选择性的亚甲基膦酸 CD73抑制剂，对人 CD73 作用的 IC50值为 2.6 nM，在癌症免疫学中具有研究潜力。