BI 853520 (IN-10018) 是一种具有口服活性的粘附斑激酶 (FAK) 强效抑制剂 (重组 FAK IC50=1 nM)，BI 853520 表现出对癌细胞的抗增殖活性。
| Cas No. | 1227948-82-4 |
| 别名 | IN-10018 |
| 分子式 | C28H28F4N6O4 |
| 分子量 | 588.55 |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | BI 853520 (IN-10018) is an orally active and potentfocal adhesion kinase(FAK) inhibitor (recombinant FAKIC50=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 EC50value 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. |
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