Ifebemtinib

Research use only, not for human use.

Ifebemtinib (BI-853520) is an orally active and potent inhibitor of adhesion plaque kinase (FAK) (IC50=1 nM) with anti-tumour activity that inhibits globule formation and in situ tumour growth in malignant pleural mesotheliomas.

Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1?nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900?nM and 1040?nM, respectively.

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.Cell Viability Assay Cell Line:PC-3 cells Concentration:0-3 μM Incubation Time:2 hours Result:Resulted in a concentration-dependent reduction of the signal with a median EC50 value of 1?nM.Cell Proliferation Assay Cell Line:4T1, Py2T, and Py2T-LT cells Concentration:0-30 μM Incubation Time:4-6 days Result:Indicated that the specific inhibition of cell proliferation and invasion at low doses is functional only in three-dimensional cell culture conditions, whereas cells cultured on plastic only respond to BI 853520 at very high, toxic doses.Western Blot Analysis Cell Line:4T1, Py2T, and Py2T-LT cells Concentration:0-10 μM Incubation Time:24 hours Result:Reduced Y397-FAK autophosphorylation in all cell types.Western Blot Analysis Cell Line:4T1, Py2T, and Py2T-LT cells Concentration:0.1 μM Incubation Time:96 hours Result:Decreased Y397-FAK autophosphorylation following 0.1?μM BI 853520 treatment occurred within 10?min and was substantially reduced at least for the following 48?h.

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.Animal Model:FVB/N, Balb/c, or immunodeficient nude (nu/nu) mice transplanted with Py2T, 4T1, or MTflECad cells, respectively Dosage:50 mg/kg Administration:Oral gavage; 50 mg/kg; once daily; 0-8 weeks Result:Decreased tumor volume significantly over time.

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Angiogenesis

FAK

FAK

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1227948-82-4

588.55

C28H28F4N6O4

>98% (HPLC)

In Vitro:?DMSO : 66.67 mg/mL (113.28 mM; Ultrasonic )

COc1cc(C(=O)NC2CCN(C)CC2)c(F)cc1Nc1ncc(c(Oc2cccc3CN(C)C(=O)c23)n1)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years