中文名 | 化合物PYROTINIB DIMALEATE |
英文名 | Pyrotinib Maleate |
别名 | 化合物PYROTINIB DIMALEATE |
英文别名 | SHR1258 maleate Pyrotinib Maleate Pyrotinib dimaleate |
CAS | 1397922-61-0 |
化学式 | C36H35ClN6O7 |
分子量 | 699.161 |
溶解度 | 溶于DMSO |
存储条件 | -20℃ |
物化性质 | 生物活性 Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate 是一种有效的、具有选择性的、不可逆的 EGFR 和 HER2 双重酪氨酸激酶抑制剂,其对应的IC50值分别为0.013 μM和0.038 μM。 |
产品用途 | Pyrotinib maleate is a salt of Pyrotinib. Pyrotinib also known as SHR-1258, is an orally bioavailable, dual kinase inhibitor of the epidermal growth factor receptor (EGFR or HER-1) and the human epidermal growth factor receptor 2 (ErbB2 or HER-2), with potential antineoplastic activity. Upon oral administration, pyrotinib binds to and inhibits both EGFR and HER2, which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumor cells. EGFR and HER2 are receptor tyrosine kinases that are upregulated in various tumor cell types and play major roles in tumor cell proliferation and tumor vascularization. |
靶点 | HER2 EGFR |
参考资料 展开查看 | 1. Li X, et al. Discovery and development of Pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment of breast cancer. Eur J Pharm Sci. 2017 Jan 21. pii: S0928-0987(17)30043-X. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.43 ml | 7.151 ml | 14.303 ml |
5 mM | 0.286 ml | 1.43 ml | 2.861 ml |
10 mM | 0.143 ml | 0.715 ml | 1.43 ml |
5 mM | 0.029 ml | 0.143 ml | 0.286 ml |
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