cd73 in 1

CD73-IN-1 是一种具有抗癌活性的 CD73 抑制剂。

CD73-IN-13 可用于制备肿瘤相关疾病的药物。CD73-IN-13 是CD73的有效抑制剂，CD73 与肿瘤生长、血管生成和转移密切相关。

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-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-17 (compound 19)，作为一种有效的CD73抑制剂，展现出对 hCD73 的强效抑制活性，IC50值仅为 0.1 μM。该化合物主要应用于抗癌领域的研究。

CD73-IN-16（compound 18）作为 hCD73 的一种有效抑制剂，显示出了0.28 μM 的IC50值。

CD73-IN-19 (Compound 4ab) 是一种CD73抑制剂，其在浓度为100 μM时对CD73酶活性的抑制率为44%。在10 μM和100 μM浓度下，CD73-IN-19 能够完全拮抗由TCR (T 细胞受体) 触发导致的 T 细胞增殖阻断（TCR 触发由CD73活性诱导），并在HEK-293细胞中抑制hA2A受体活性 (Ki为3.31 μM)。CD73-IN-19 可能在免疫疾病领域的研究中具有应用潜力。

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-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-6, serves as a potent inhibitor of CD73. This compound finds utility in cancer research [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)。

Uliledlimab 是一种有效的抗 CD73人源单克隆抗体。Uliledlimab 抑制胞外单磷酸腺苷 (AMP) 向腺苷的转化。Uliledlimab 可用于癌症的研究。

ORIC-533 是一种口服有效的、具有 AMP 竞争性的 CD73 选择性抑制剂。ORIC-533 能恢复被免疫抑制的 CD8+ T 细胞增殖和活化，导致骨髓微环境中多发性骨髓瘤细胞显著裂解和细胞死亡。