BI-853520
(Synonyms: IN-10018) 目录号 : GC65886
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
Sample solution is provided at 25 µL, 10mM.
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BI 853520 (IN-10018) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=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 EC50 value 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. |
| Cas No. | 1227948-82-4 | SDF | Download SDF |
| 别名 | IN-10018 | ||
| 分子式 | C28H28F4N6O4 | 分子量 | 588.55 |
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet