PLB-1001( Bozitinib | PLB1001 | CBI-3103 | CBT-101 )

Catalog No. M11870 CAS No. 1440964-89-5

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PLB-1001
Note

Research use only, not for human use.
Brief Description

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.
Description

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; 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; demonstrates remarkable potency in selectively inhibiting MET-altered tumor cells (METex14) in preclinical models; also exhibits clinical potential for precisely treating gliomas.Liver Cancer Phase 2 Clinical.
In Vitro

Western Blot Analysis Cell Line:Human astrocytes (HA) cells Concentration:30 μM Incubation Time:6 hours Result:Decreased p-STAT3,p-MET expression.
In Vivo

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Synonyms

Bozitinib | PLB1001 | CBI-3103 | CBT-101
Pathway

Angiogenesis
Target

c-Met/HGFR
Recptor

c-Met/HGFR
Research Area

Cancer
Indication

Liver Cancer

CAS Number

1440964-89-5
Formula Weight

424.391
Molecular Formula

C20H15F3N8
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 50 mg/mL (117.82 mM)
SMILES

CN1C=C2C=C(C(=CC2=N1)F)C(C3=NN=C4N3N=C(C=C4)C5=CN(N=C5)C6CC6)(F)F
Chemical Name

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

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

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