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Pebezertinib

Chemical Structure : Pebezertinib

CAS No.: 2769954-39-2

Pebezertinib (BLU-451, LNG-451, BLU451, LNG451)

Catalog No.: PC-24971Not For Human Use, Lab Use Only.

Pebezertinib (BLU-451, LNG-451) is a potent, CNS-penetrant, wild-type EGFR sparing inhibitor of EGFR exon 20 insertion mutations, as well as atypical (G719C, G719S, L861Q) and common EGFR mutants.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Pebezertinib (BLU-451, LNG-451) is a potent, CNS-penetrant, wild-type EGFR sparing inhibitor of EGFR exon 20 insertion mutations, as well as atypical (G719C, G719S, L861Q) and common EGFR mutants.
Pebezertinib (BLU-451, LNG-451) demonstrated nanomolar potency in multiple atypical and exon 20 insertion mutation cell lines with selectivity against WT EGFR in BaF3 cells.
Pebezertinib (BLU-451, LNG-451) shows potent antitumor activity, including in an intracranial xenograft model.

Physicochemical Properties

M.Wt 497.46
Formula C24H19F4N7O
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

2-Propenamide, N-[4-fluoro-3-[[2-[(1-methyl-1H-pyrazol-4-yl)amino]-5-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]amino]phenyl]-

References

1. Xiuning Le, et al. Mol Cancer Ther (2023) 22 (12_Supplement): C151.

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