| Identification | Back Directory | [Name]
1H-Cyclopenta[d][1,2,4]triazolo[1,5-a]pyrimidine-2-carboxamide, N-[2,5-dimethyl-4-[[1-oxo-3-(5-phenyl-1,3,4-oxadiazol-2-yl)propyl]amino]phenyl]-5,6,7,8-tetrahydro-8-oxo- | [CAS]
2083618-79-3 | [Synonyms]
PDZ1i
1H-Cyclopenta[d][1,2,4]triazolo[1,5-a]pyrimidine-2-carboxamide, N-[2,5-dimethyl-4-[[1-oxo-3-(5-phenyl-1,3,4-oxadiazol-2-yl)propyl]amino]phenyl]-5,6,7,8-tetrahydro-8-oxo- | [Molecular Formula]
C28H26N8O4 | [MOL File]
2083618-79-3.mol | [Molecular Weight]
538.56 |
| Hazard Information | Back Directory | [Description]
PDZ1i, also known as 113B7, is an inhibitor of MDA-9/Syntenin activity. PDZ1i radiosensitized GBM cells. PDZ1i inhibited crucial GBM signaling involving FAK and mutant EGFR, EGFRvIII, and abrogated gains in secreted proteases, MMP-2 and MMP-9, following radiation. In an in vivo glioma model, PDZ1i resulted in smaller, less invasive tumors and enhanced survival. When combined with radiation, survival gains exceeded radiotherapy alone. | [Uses]
PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion[1]. | [References]
[1] Kegelman TP, et al. Inhibition of radiation-induced glioblastoma invasion by genetic and pharmacological targeting of MDA-9/Syntenin. Proc Natl Acad Sci U S A. 2017 Jan 10;114(2):370-375. DOI:10.1073/pnas.1616100114 |
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| Company Name: |
Biorbyt Ltd.
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| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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