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BI-4464

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Chemical Structure| 1227948-02-8 同义名 : -
CAS号 : 1227948-02-8
货号 : A1145670
分子式 : C28H28F3N5O4
纯度 : 99%+
分子量 : 555.548
MDL号 : MFCD32062817
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(28.8 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
动物实验配方：
生物活性
描述 Focal adhesion tyrosine kinase (PTK2) is a cytoplasmic enzyme that has been found to be overexpressed and activated in various advanced solid cancers. BI-4464 is an ATP-competitive inhibitor of PTK2 that results in PTK2 degradation in A549 cells with an IC50 value of 17 nM. BI-4464 also showed anti-proliferative property in SNU-387, HUH-1, Hep3B2.1-7, HepG2, SK-Hep-1, HLF, SNU-398, HUCCT1, HLE, HuH-7, and SNU-423 cell lines with pIC50 values of 5.2, 5.4, 5.3, 5.5, 5.2, 5.4, 5.2, 5.2, 5.1, 5.4, and 5.4, respectively[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.00mL

1.80mL

0.90mL

18.00mL

3.60mL

1.80mL
参考文献

[1]Popow J, Arnhof H, Bader G, Berger H, Ciulli A, Covini D, Dank C, Gmaschitz T, Greb P, Karolyi-Özguer J, Koegl M, McConnell DB, Pearson M, Rieger M, Rinnenthal J, Roessler V, Schrenk A, Spina M, Steurer S, Trainor N, Traxler E, Wieshofer C, Zoephel A, Ettmayer P. Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J Med Chem. 2019 Mar 14;62(5):2508-2520. doi: 10.1021/acs.jmedchem.8b01826. Epub 2019 Feb 22. PMID: 30739444.