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BI-853520
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BI-853520图片
CAS NO:1227948-82-4
包装:10mg
市场价:7650元

产品介绍
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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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.