CD73-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/cd73.html CD73ecto-5-nucleotidase, NT5ECD73 (Ecto-5-nucleotidase) is a 70-kD glycosylphosphatidyl inositol (GPI)-anchored cell surface protein encoded by the NT5E genethat plays a crucial role in switching on adenosinergic signaling. CD73 is an ectonucleotidase

2、 which catalyzes the terminal step inextracellular adenine nucleotide breakdown: the conversion of AMP to adenosine. Adenosine, which binds to a discrete family ofcell surface receptors to initiate intracellular signaling cascades, has been shown to be anti-inflammatory and vasorelaxant.CD73 has bot

3、h enzymatic and non-enzymatic functions in cells: as a nucleotidase, CD73 catalyzes the hydrolysis of AMP intoadenosine and phosphate, and CD73-generated adenosine plays an important role in tumor immunoescape; moreover, CD73 alsofunctions as a signal and adhesive molecule that can regulate cell int

4、eraction with extracellular matrix components, such as lamininand fibronectin, to mediate the invasive and metastatic properties of cancers. Both the enzymatic and non-enzymatic functions ofCD73 are involved in cancer-associated processes and are not completely independent of each other. There is am

5、ple evidence toshow that CD73 is a key regulatory molecule in cancer development and is overexpressed in many cancers, including leukemia,glioblastoma, melanoma, ovarian cancer, esophageal cancer, prostate cancer and breast cancer.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/cd73.html CD73 H

6、YPERLINK https:/www.MedChemE/Targets/cd73.html HYPERLINK https:/www.MedChemE/Targets/cd73.html Inhibitors HYPERLINK https:/www.MedChemE/AB-680.html AB-680 HYPERLINK https:/www.MedChemE/AB-680.html HYPERLINK https:/www.MedChemE/ab-680-ammonium.html AB-680 HYPERLINK https:/www.MedChemE/ab-680-ammonium

7、.html HYPERLINK https:/www.MedChemE/ab-680-ammonium.html ammoniumCat. No.: HY-125286 Cat. No.: HY-125286AAB-680 is a highly potent, reversible andselective inhibitor of CD73 (anecto-nucleotidase), with a K of 4.9 pM for hCD73,idisplays 10,000-fold selectivity over relatedecto-nucleotidases CD39. Ant

8、i-tumor activity.AB-680 ammonium is a highly potent, reversible andselective inhibitor of CD73 (anecto-nucleotidase), with a K of 4.9 pM for hCD73,idisplays 10,000-fold selectivity over relatedecto-nucleotidases CD39. Anti-tumor activity.Purity: 99.71%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10

9、 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/CD73-IN-1.html CD73-IN-1 HYPERLINK https:/www.MedChemE/CD73-IN-1.html HYPERLINK https:/www.MedChemE/cd73-in-2.html CD73-IN-2Cat. No.: HY-103695 Cat. No.: HY-131435CD73-IN-1 is an

10、inhibitor of CD73 which can beused in the treatment of cancer extracted frompatent WO 2017153952 A1, example 80.CD73-IN-2 is a potent CD73 inhibitor extractedfrom WO2020151707A1, example 1, has an IC of500.09 nM.Purity: 98.54%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg,

11、 25 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cd73-in-3.html CD73-IN-3 HYPERLINK https:/www.MedChemE/cd73-in-3.html HYPERLINK https:/www.MedChemE/cd73-in-4.html CD73-IN-4Cat. No.: HY-137246 Cat. No.: HY-131967CD73-IN-3 is a potent CD73 i

12、nhibitor (IC =7.3 nM50in Calu6 human cell assay). CD73-IN-3, example 2extracted from patent WO2019168744 A1, has thepotential for cancer research.CD73-IN-4 is a potent and selectivemethylenephosphonic acid CD73 inhibitor, with anIC of 2.6 nM for human CD73. CD73-IN-4 is50potential for the research o

13、f cancer immunology.Purity: 99.89%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.54%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cd73-in-5.html CD73-IN-5 HYPERLINK https:/www.MedChemE/

14、cd73-in-5.html HYPERLINK https:/www.MedChemE/cd73-in-6.html CD73-IN-6Cat. No.: HY-145334 Cat. No.: HY-144209CD73-IN-5 is a potent and selective non-nucleotidesmall molecule inhibitor of CD73 (IC = 19 nM).50CD73-IN-6 is a CD73 inhibitor extracted frompatent WO2022007677A1 compound 2. CD73-IN-6 can be

15、used for the research of cancer.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/MethADP.html MethADP HYPERLINK https:/www.MedChemE/MethADP.html HYPERLINK https:/www.MedChe

16、mE/methadp-sodium-salt.html MethADP HYPERLINK https:/www.MedChemE/methadp-sodium-salt.html HYPERLINK https:/www.MedChemE/methadp-sodium-salt.html sodium HYPERLINK https:/www.MedChemE/methadp-sodium-salt.html HYPERLINK https:/www.MedChemE/methadp-sodium-salt.html salt(Adenosine 5-(,-methylene)diphosp

17、hate) Cat. No.: HY-112502Cat. No.: HY-112502BMethADP is a specific CD73 inhibitor.MethADP (sodium salt) is a specific CD73inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909

18、 Email: salesMedChemE HYPERLINK https:/www.MedChemE/mrs4620.html MRS4620Cat. No.: HY-144072 HYPERLINK https:/www.MedChemE/oleclumab.html Oleclumab(MEDI9447) Cat. No.: HY-P99039MRS4620 is a potent CD73 inhibitor, with a K ofi0.436 nM. MRS4620 can be use for the research ofcancer immunotherapy.Oleclum

19、ab (MEDI9447) is a human IgG1 anti-CD73monoclonal antibody that inhibits CD73 function.Oleclumab has an anti-tumor activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/op-5244.html OP

20、-5244 HYPERLINK https:/www.MedChemE/op-5244.html HYPERLINK https:/www.MedChemE/op-5244-sodium.html OP-5244 HYPERLINK https:/www.MedChemE/op-5244-sodium.html HYPERLINK https:/www.MedChemE/op-5244-sodium.html sodiumCat. No.: HY-136978 Cat. No.: HY-136978AOP-5244 is a potent and orally active inhibitor

21、 ofCD73, with an IC of 0.25 nM. OP-5244 reverses50immunosuppression through blocking of adenosineproduction, and has the potential for the cancerresearch.OP-5244 sodium is a potent and orally activeinhibitor of CD73, with an IC of 0.25 nM.50OP-5244 sodium reverses immunosuppression throughblocking o

22、f adenosine production, and has thepotential for the cancer research.Purity: 99.63%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/PSB-12379.html PSB-12379 HYPERLINK https:/www.MedChemE/PSB-12379.html HYPERLINK https:/www.MedChemE/psb-12379-disodium.html PSB-12379 HYPERLINK https:/www.MedChemE/psb-12379-disodium.html HYPERLINK https:/www.MedChemE/psb-12379-disodium.html disodiumCat. No.: HY-100