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PLB-1001

Chemical Structure : PLB-1001

CAS No.: 1440964-89-5

PLB-1001 (Bozitinib, Vebreltinib, PLB1001, CBI-3103, CBT-101)

Catalog No.: PC-35732Not For Human Use, Lab Use Only.

PLB-1001 (Bozitinib, PLB1001, CBI-3103, CBT-101) is a potent, highly selective, ATP-competitive, BBB-permeable MET kinase inhibitor, potently inhibits MET activity by 95.1% at 2 uM.

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Purity & Documentation Purity: 98.25% (HPLC) Select Batch:

Biological Activity

PLB-1001 (Bozitinib, Vebreltinib, PLB1001, CBI-3103, CBT-101) is a potent, highly selective, ATP-competitive, BBB-permeable MET kinase inhibitor, potently inhibits MET activity by 95.1% at 2 uM.
Similar with crizotinib, PLB-1001 inhibited the phosphorylation of MET and STAT3, indicating a robust inhibitory effect of PLB-1001 on MET and its downstream signaling pathways.
PLB-1001 demonstrates remarkable potency in selectively inhibiting MET-altered tumor cells (METex14) in preclinical models.
PLB-1001 also exhibits clinical potential for precisely treating gliomas.

Physicochemical Properties

M.Wt 424.391
Formula C20H15F3N8
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(1-cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6-fluoro-2-methyl-2H-indazol-5-yl)methyl)-[1,2,4]triazolo[4,3-b]pyridazine

References

1. Hu H, et al. Cell. 2018 Oct 12. pii: S0092-8674(18)31250-9.

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