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Pyrotinib

Chemical Structure : Pyrotinib

CAS No.: 1269662-73-8

Pyrotinib (SHR-1258;SHR1258)

Catalog No.: PC-70084Not For Human Use, Lab Use Only.

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively.

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Biological Activity

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively.
Pyrotinib (SHR-1258) displays high selectivity in a panel of different kinases such as KDR, c-Kit, PDGFRβ, c-Src and c-Met (c-Src with an IC50 of 790 nM, and others >3,000 nM).
Pyrotinib (SHR-1258) exhibits robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.

Physicochemical Properties

M.Wt 583.089
Formula C32H31ClN6O3
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

(R,E)-N-(4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)acrylamide

References

1. Li X, et al. Eur J Pharm Sci. 2017 Jan 21. pii: S0928-0987(17)30043-X.

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