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 FAKIC50=1 nM)，Ifebemtinib 表现出对癌细胞的抗增殖活性。
| 生物活性 | Ifebemtinib (BI 853520) is an orally active and potentfocal adhesion kinase(FAK) inhibitor (recombinantFAKIC50=1 nM). Ifebemtinib shows anti-proliferative activity againstcancercells[1][2]. |
体外研究
(In Vitro) | Ifebemtinib (BI 853520) (0-3 μM; 2 h) inhibits cancer cells growth[2].
Ifebemtinib (BI 853520) (0-30 μM; 4-6 d) represses tumor cell proliferation and invasion only in 3D culture[1].
Ifebemtinib (0-10 μM; 24 h) represses Y397-FAK autophosphorylation[1].
Ifebemtinib (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. |
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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[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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| 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) |
| 溶解性数据 | In Vitro: DMSO : 66.67 mg/mL(113.28 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.6991 mL | 8.4955 mL | 16.9909 mL | | 5 mM | 0.3398 mL | 1.6991 mL | 3.3982 mL | | 10 mM | 0.1699 mL | 0.8495 mL | 1.6991 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1 mg/mL (1.70 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (1.70 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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