Pyrotinib dimaleate - Names and Identifiers
Pyrotinib dimaleate - Physico-chemical Properties
Molecular Formula | C36H35ClN6O7
|
Molar Mass | 699.161 |
Solubility | Soluble in DMSO |
Storage Condition | -20℃ |
Physical and Chemical Properties | Bioactive Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is an effective, selective and irreversible dual tyrosine kinase inhibitor of EGFR and HER2, with corresponding IC50 values of 0.013 μM and 0.038 μM respectively. |
Use | 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. |
Target | HER2 EGFR |
Pyrotinib dimaleate - Reference
Reference Show more | 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. |
Pyrotinib dimaleate - Preparation solution concentration reference
| 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 |
Last Update:2024-01-02 23:10:35
Pyrotinib dimaleate - Cell Experiment
Cell lines: A431, SK-BR-3, NCI-N87Concentrations: 6-7 concentrations (not specific)Incubation Time: 72 hMethod:Cells are incubated in a carbon dioxide (5%CO2) incubator until they reached 85% confluency, subsequently, cell culture medium is replaced by fresh one with Pyrotinib (SHR1258) added in a series of concentrations (6 to 7 concentrations). The cells are then put back to the incubator and cultured continuously. After 72 hours, the activity of the test compounds for inhibiting the cell proliferation is determined by a sulforhodamine B (SRB) method.(Only for Reference)
Last Update:2023-08-16 21:32:38
Pyrotinib dimaleate - Animal Experiment
Animal Models: 6-7-week-old female BALB/Ca-nude mice with BT-474/SK-OV-3 xenograftsDosages: 2.5-20 mg/kg, 100 mg/kgAdministration: IV, IG(Only for Reference)
Last Update:2023-08-16 21:32:38