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Pyrotinib dimaleate

CAS No. : 1397922-61-0

MCE 站：Pyrotinib dimaleate

产品活性：Pyrotinib dimaleate (SHR-1258 dimaleate) 是有效、选择性的 EGFR/HER2 双重抑制剂，IC ₅₀ 值分别为 13 nM 和 38 nM。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR

In Vitro: 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 inhibits BT474 and SK-OV-3 cells with IC₅₀s of 5.1 and 43 nM, respectively. 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).

In Vivo: Pyrotinib dimaleate has acceptable bioavailability of 20.6%, 43.5% and 13.5% in nude mice, rats and dogs, respectively. Pyrotinib dimaleate has favorable drug-like physicochemical properties and shows relatively higher oral exposure in human subjects (oral; t_1/2=15 h) with a much longer half life than that of preclinical animal species such as mouse (i.v.; t_1/2=1.56 h; i.g.; t_1/2=2.52 h) and rat (i.v.; t_1/2=4.42 h; i.g.; t_1/2=3.38 h).

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