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Perzebertinib

Chemical Structure : Perzebertinib

CAS No.: 2414056-31-6

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Perzebertinib (ZN-1041, ZN-A-1041)

Catalog No.: PC-24169Not For Human Use, Lab Use Only.

Perzebertinib (ZN-1041, ZN-A-1041) is a potent, selective BBB penetrable HER2 tyrosine kinase inhibitor.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Perzebertinib (ZN-1041, ZN-A-1041) is a potent, selective BBB penetrable HER2 tyrosine kinase inhibitor.
ZN-1041 selectively inhibits HER2 in BT474 cell with IC50 of 9.5 nM, while sparing wt-EGFR in H838 cells (IC50=12 μM).
ZN-1041 is not a substrate of  P-gp and BCRP and has high BBB permeability.
ZN-1041 alone demonstrated dose-dependent and significant anti-tumor activity when compared to tucatinib in BM model.

Physicochemical Properties

M.Wt 548.55
Formula C27H26F2N8O3
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

4-Quinazolinamine, 5-[[(4R)-3,3-difluoro-1-methyl-4-piperidinyl]oxy]-6-methoxy-N-[3-methyl-4-([1,2,4]triazolo[1,5-c]pyrimidin-7-yloxy)phenyl]-

References

1. Fei Ma, et al. ournal of Clinical Oncology. Volume 41, Number 16_suppl

2. Patent WO2020057511 A1.

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