| 产品描述： | 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 |
| 靶点： |
EGFR(Cell-free assay):0.013 μM; HER2(Cell-free assay):0.038 μM;EGFR; HER |
| 体外研究： |
Pyrotinib (SHR1258), as an EGFR/HER2 dual tyrosine kinase inhibitor, shows excellent in vitro potency, selectivity, and favorable PK profiles |
| 体内研究： |
Pyrotinib (SHR1258) displays robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human. |
| 细胞实验： |
Cell lines: A431, SK-BR-3, NCI-N87 Concentrations: 6-7 concentrations (not specific) Incubation Time: 72 h Method: 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. |
| 动物实验： |
Animal Models: 6-7-week-old female BALB/Ca-nude mice with BT-474/SK-OV-3 xenografts Dosages: 2.5-20 mg/kg, 100 mg/kg Administration: IV, IG |
| 参考文献： |
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. |
| 溶解性： |
Soluble in DMSO、Ethanol、H2O |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
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 |
| 50 mM |
0.029 ml |
0.143 ml |
0.286 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京