Pyrotinib dimaleate 是选择性的EGFR/HER2双重抑制剂，IC50值分别为 13 和 38 nM。

Pyrotinib dimaleate is a potent and selective dual inhibitor of EGFR/HER2 with IC50s of 13 and 38 nM, respectively.

Pyrotinib dimaleate has high potency in HER2-dependent cell lines (BT474, SK-OV-3) while showing much weaker inhibition in the HER2 negative cell line (MDA-MB-231). Pyrotinib dimaleate displays high selectivity as HKI-272 when tested 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 >3000 nM). Pyrotinib dimaleate inhibits BT474 and SK-OV-3 cells with IC50s of 5.1 and 43 nM, respectively.

Pyrotinib dimaleate has favorable drug-like physicochemical properties and shows relatively higher oral exposure in human subjects (oral; t1/2=15 h) with a much longer half-life than that of preclinical animal species such as mice (i.v.; t1/2=1.56 h; i.g.; t1/2=2.52 h) and rat (i.v.; t1/2=4.42 h; i.g.; t1/2=3.38 h). Pyrotinib dimaleate has acceptable bioavailability of 20.6%, 43.5%, and 13.5% in nude mice, rats, and dogs, respectively.

1397922-61-0

C40H39ClN6O11

815.23

SHR-1258 dimaleate

Ethanol:40mg/mL (49.07mM)
DMSO:100mg/mL (122.67mM)
H2O:50mg/mL (61.33mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years