Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC 50 =1?nM). Ifebemtinib shows anti-proliferative activity against cancer cells.
性状
Solid
体外研究(In Vitro)
Ifebemtinib (BI 853520) (0-3 μM; 2 h) inhibits cancer cells growth.Ifebemtinib (BI 853520) (0-30 μM; 4-6 d) represses tumor cell proliferation and invasion only in 3D culture.Ifebemtinib (0-10 μM; 24 h) represses Y397-FAK autophosphorylation.Ifebemtinib (0.1 μM; 96 h) shows a fast and potent inhibition of FAK in this highly metastatic murine breast cancer cell line. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Ifebemtinib (BI 853520) (oral gavage; 50 mg/kg; once daily; 0-8 weeks) treatment significantly suppresses primary tumor growth of all three cell lines in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
ClinicalTrial
参考文献
[1]. Stefanie Tiede, et al. The FAK inhibitor BI 853520 exerts anti-tumor effects in breast cancer. Oncogenesis. 2018 Sep 20;7(9):73.[2]. Ulrich A Hirt, et al. Efficacy of the highly selective focal adhesion kinase inhibitor BI 853520 in adenocarcinoma xenograft models is linked to a mesenchymal tumor phenotype. Oncogenesis. 2018 Feb 23;7(2):21.
溶解度数据
In Vitro: DMSO : 66.67 mg/mL (113.28 mM; Need ultrasonic)配制储备液