Pyrotinib dimaleate

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Chemical Structure| 1397922-61-0 同义名 : SHR-1258; SHR-1258 dimaleate; Pyrroltinib dimaleate; BLTN
CAS号 : 1397922-61-0
货号 : A891704
分子式 : C40H39ClN6O11
纯度 : 98%
分子量 : 815.22
MDL号 : N/A
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(128.8 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(122.67 mM)
生物活性
靶点

  • EGFR/ErbB1

    EGFR, IC50:0.013 μM

  • HER2/ErbB2

    HER2, IC50:0.038 μM
描述 Pyrotinib maleate is an irreversible pan-ErbB receptor tyrosine kinase inhibitor, in patients with HER2-Positive metastatic breast cancer.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.23mL

0.25mL

0.12mL

6.13mL

1.23mL

0.61mL

12.27mL

2.45mL

1.23mL
参考文献

[1]Ma F, Li Q, et al. Phase I Study and Biomarker Analysis of Pyrotinib, a Novel Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor, in Patients With Human Epidermal Growth Factor Receptor 2-Positive Metastatic Breast Cancer. J Clin Oncol. 2017 May 12:JCO2016696179.

[2]Li X, Yang C, 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.