Ifebemtinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ifebemtinib (BI 853520) 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)，Ifebemtinib 表现出对癌细胞的抗增殖活性。

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 中的溶解度 : 66.67 mg/mL (113.28 mM; 超声助溶 )

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