PLB-1001|Bozitinib|DC Chemicals

Cas No.:	1440964-89-5
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
Synonyms:	Bozitinib;PLB1001;CBI-3103;CBT-101
SMILES:	C12=NN=C(C(F)(F)C3C(F)=CC4C(C=3)=CN(C)N=4)N1N=C(C1=CN(C3CC3)N=C1)C=C2
Formula:	C₂₀H₁₅F₃N₈
M.Wt:	424.391
Purity:	>98%
Sotrage:	Please store the product under the recommended conditions in the Certificate of Analysis.
Publication:	[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.

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.
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.

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