PF-573228
(Synonyms: 6-[(4-((3-(甲磺酰基)苄基)氨基)-5-三氟甲基嘧啶-2-基)氨基]-3,4-二氢-1H-喹啉-2-酮) 目录号 : GC11107
A selective focal adhesion kinase inhibitor
Cas No.:869288-64-2
Sample solution is provided at 25 µL, 10mM.
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PF573228 is an inhibitor of FAK with IC50 value of 4 nM [1].
FAK (Focal adhesion kinase) is a non-receptor protein-tyrosine kinase that resides at the sites of focal adhesions. FAK protein is encoded by the FAK gene located on human chromosome 8q24 and the molecular weight is 125 kDa. FAK works as an important mediator of cell activities, like cell adhesion, growth, proliferation, survival, angiogenesis and migration, it is reported that normal tissues FAK are significantly lower than in primary and metastatic tumors [2].
PF573228 is a specific inhibitor of FAK and is regarded as potent anti-angiogenic agents. When tested with HUVEC (primary human umbilical vein endothelial cells), PF573228 treatment increased the proportion of cell apoptosis, reduced the ability of endothelial cell migration and sprout formation via inhibiting the autophosphorylation of FAK [3]. In A431 epithelial carcinoma cells, incubation with PF573228 resulted in the reduced phosphorylation of FAK with IC50 value of 11 nM and PF573228 also observed to inhibit the FAK phosphorylation in many other cancer cells, such as PC3 cells, SKOV-3 cells, L3.6p1 cells, F-G cells and MDCK cells with IC50 value of 30-500 nM [1]. When tested with MSCs (mesenchymal stem cells), PF573228 treatment depressed the MSCs pro-inflammatory response to CM from FaDu, MDA-MB-231, PC-3 and NCI-H522 via inhibiting FAK phosphorylation [4].
PF573228 is also reported functioned in the process of BK (Ca)-channel. When tested with pituitary tumor (GH (3)) cells transfected with K (Ca) 1.1 siRNAs, 3 uM PF573228 treatment stimulated the BK (Ca)-channel activity which subsequently may influence cell behavior [5].
References:
[1]. Slack-Davis, J.K., et al., Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem, 2007. 282(20): p. 14845-52.
[2]. Golubovskaya, V.M., Focal adhesion kinase as a cancer therapy target. Anticancer Agents Med Chem, 2010. 10(10): p. 735-41.
[3]. Cabrita, M.A., et al., Focal adhesion kinase inhibitors are potent anti-angiogenic agents. Mol Oncol, 2011. 5(6): p. 517-26.
[4]. Al-toub, M., et al., Pleiotropic effects of cancer cells' secreted factors on human stromal (mesenchymal) stem cells. Stem Cell Res Ther, 2013. 4(5): p. 114.
[5]. So, E.C., et al., Evidence for activation of BK Ca channels by a known inhibitor of focal adhesion kinase, PF573228. Life Sci, 2011. 89(19-20): p. 691-701.
| Cell experiment [1]: | |
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Cell lines |
REF52, PC3 or MDCK cells, REF52 cells |
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Preparation method |
The solubility of this compound in DMSO is >166.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1-10 μM, 24 h |
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Applications |
PF-228 inhibited FAK phosphorylation in A431 cells with IC50 of 11 nM. PF-228 blocked FAK Tyr397 phosphorylation in PC3 (prostate carcinoma), SKOV-3 (ovarian carcinoma), L3.6p1 and F-G (pancreatic carcinomas), and MDCK cells with IC50 of 30-500 nM. In REF52 cells, treatment with 1-3 μM PF-228 reduced FN-stimulated FAK Tyr397 phosphorylation by ~65–85%. Treatment with 10 μM PF-228 blocked random migration and efficiently blocked serum and FN-stimulated migration. Treatment of cultures with 1 μM PF-228 significantly reduced the rate of movement of individual cells into the wound. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Slack-Davis J K, Martin K H, Tilghman R W, et al. Cellular characterization of a novel focal adhesion kinase inhibitor[J]. Journal of Biological Chemistry, 2007, 282(20): 14845-14852. | |
| Cas No. | 869288-64-2 | SDF | |
| 别名 | 6-[(4-((3-(甲磺酰基)苄基)氨基)-5-三氟甲基嘧啶-2-基)氨基]-3,4-二氢-1H-喹啉-2-酮 | ||
| 化学名 | 6-[[4-[(3-methylsulfonylphenyl)methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-quinolin-2-one | ||
| Canonical SMILES | CS(=O)(=O)C1=CC=CC(=C1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)CC4 | ||
| 分子式 | C22H20F3N5O3S | 分子量 | 491.49 |
| 溶解度 | ≥ 166.6mg/mL in DMSO | 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 | 2.0346 mL | 10.1731 mL | 20.3463 mL |
| 5 mM | 0.4069 mL | 2.0346 mL | 4.0693 mL |
| 10 mM | 0.2035 mL | 1.0173 mL | 2.0346 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet