受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
Synonyms | SHR-1258, BLTN, Pyrroltinib dimaleate | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C40H39ClN6O11 |
|||
分子量 | 815.22 | CAS No. | 1397922-61-0 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (122.66 mM) | |
Water | 50 mg/mL (61.33 mM) | |||
Ethanol | 40 mg/mL (49.06 mM) | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Pyrotinib dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively. |
---|---|
in vitro | Pyrotinib (SHR1258), as an EGFR/HER2 dual tyrosine kinase inhibitor, shows excellent in vitro potency, selectivity, and favorable PK profiles.[1] |
in vivo | 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.[1] |
細胞アッセイ | 細胞株 | A431, SK-BR-3, NCI-N87 |
---|---|---|
濃度 | 6-7 concentrations (not specific) | |
反応時間 | 72 h | |
実験の流れ | 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. |
|
動物実験 | 動物モデル | 6-7-week-old female BALB/Ca-nude mice with BT-474/SK-OV-3 xenografts |
投薬量 | 2.5-20 mg/kg, 100 mg/kg | |
投与方法 | IV, IG |
Activity and mechanism of acquired resistance to tarloxotinib in HER2 mutant lung cancer: an in vitro study [ Transl Lung Cancer Res, 2021, 10(8):3659-3670] | PubMed: 34584864 |
UPLC-MS/MS assay for the simultaneous determination of pyrotinib and its oxidative metabolite in rat plasma: Application to a pharmacokinetic study [ Biomed Chromatogr, 2021, e5221] | PubMed: 34331710 |
Clinical implications of plasma ctDNA features and dynamics in gastric cancer treated with HER2-targeted therapies [ Clin Transl Med, 2020, 10(8):e254] | PubMed: 33377634 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。