BI 853520 (IN-10018) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). BI 853520 shows anti-proliferative activity against cancer cells[1][2].
BI 853520 (0-3 μM; 2 h) inhibits cancer cells growth[2].
BI 853520 (0-30 μM; 4-6 d) represses tumor cell proliferation and invasion only in 3D culture[1].
BI 853520 (0-10 μM; 24 h) represses Y397-FAK autophosphorylation[1].
BI 853520 (0.1 μM; 96 h) shows a fast and potent inhibition of FAK in this highly metastatic murine breast cancer cell line[1].
Cell Viability Assay[2]
| 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[1]
| 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[1]
| 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[1]
| 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. |
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[1].
| Animal Model: | FVB/N, Balb/c, or immunodeficient nude (nu/nu) mice transplanted with Py2T, 4T1, or MTflECad cells, respectively[1] |
| Dosage: | 50 mg/kg |
| Administration: | Oral gavage; 50 mg/kg; once daily; 0-8 weeks |
| Result: | Decreased tumor volume significantly over time. |