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PLB-1001

Names

[ CAS No. ]:
1440964-89-5

[ Name ]:
PLB-1001

Biological Activity

[Description]:

Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR

[In Vitro]

Bozitinib (PLB-1001) (30 μM; 6 hours) inhibits the phosphorylation of MET and STAT3, has a robust inhibitory effect of PLB-1001 on MET and its downstream signaling pathways. Western Blot Analysis[1] Cell Line: Human astrocytes (HA) cells Concentration: 30 μM Incubation Time: 6 hours Result: Decreased p-STAT3,p-MET expression.

[References]

[1]. Hu H, et al. Mutational Landscape of Secondary Glioblastoma Guides MET-Targeted Trial in Brain Tumor. Cell. 2018 Nov 29;175(6):1665-1678.e18.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H15F3N8

[ Molecular Weight ]:
424.38

[ Storage condition ]:
-20°C


Related Compounds