Name | Pyrotinib dimaleate |
Description | Pyrotinib dimaleate is a selective EGFR/HER2 dual inhibitor with IC50 values of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer. |
In vitro | METHODS: SK-BR-3 cells were treated with Pyrotinib dimaleate (10nM) + chrysin (20μM) or drug + mimics and drug + si-ZBTB16, and the cells were collected for apoptosis analysis.
RESULTS Pyrotinib dimaleate + chrysin treatment led to a significant upregulation of ZBTB16 expression, and this effect was neutralized by knockdown of ZBTB16 by siRNA-ZBTB16; miR-16-5p overexpression or ZBTB16 knockdown correspondingly reduced the apoptosis rate induced by Pyrotinib dimaleate + chrysin treatment. [2] |
In vivo | METHODS: Nude mice with tumor xenografts of BT-474 or SK-BR-3 cells were treated with Pyrotinib dimaleate (10 mg/kg, gavage, 21 days), chrysin (50 mg/kg), or their combination, and the effect of miR-16-5p expression level on anti-tumor efficacy was analyzed.
RESULTS Combination therapy of pyrotinib dimaleate and chrysin synergistically enhanced autophagy in HER2-positive breast cancer cells by regulating the miR-16-5p/ZBTB16/G6PD axis.[2] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O : 50 mg/mL (61.33 mM) Ethanol : 40 mg/mL (49.07 mM) DMSO : 100 mg/mL (122.67 mM)
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Keywords | Pyrotinib | Epidermal growth factor receptor | inhibit | Inhibitor | Pyrotinib Dimaleate | Pyrotinib dimaleate | SHR1258 | SHR1258 Dimaleate | SHR-1258 | HER1 | EGFR | SHR-1258 Dimaleate | SHR 1258 | ErbB-1 | SHR 1258 Dimaleate |
Inhibitors Related | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib |
Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Kinase Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |