Ifebemtinib BI-853520; IN-10018|cas:1227948-82-4|西域试剂

Ifebemtinib BI-853520; IN-10018,99.61%

产品编号：Bellancom-122844| CAS NO：1227948-82-4| 分子式：C₂₈H₂₈F₄N₆O₄| 分子量：588.55

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-122844		￥5000.00	杭州北京（现货）
Bellancom-122844		￥8500.00	杭州北京（现货）

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Ifebemtinib BI-853520; IN-10018

产品介绍

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。

生物活性

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 66.67 mg/mL (113.28 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 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。