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PF-573228

现货
Catalog No.
B1523
FAK抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 900.00
现货
50mg
¥ 3,500.00
现货

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Background

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.

文献引用

1. Kath C, Goni-Oliver P, et al. "PTEN suppresses axon outgrowth by down-regulating the level of detyrosinated microtubules." PLoS One. 2018 Apr 4;13(4):e0193257. PMID:29617365

Chemical Properties

StorageStore at -20°C
M.Wt491.49
Cas No.869288-64-2
FormulaC22H20F3N5O3S
Solubility≥166.6mg/mL in DMSO
Chemical Name6-[[4-[(3-methylsulfonylphenyl)methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-quinolin-2-one
SDFDownload SDF
Canonical SMILESCS(=O)(=O)C1=CC=CC(=C1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)CC4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

REF52、PC3或MDCK细胞,REF52细胞

溶解方法

该化合物在DMSO中的溶解度大于166.6mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

1-10 μM,24 h

应用

PF-228抑制A431细胞中的FAK磷酸化,IC50为11 nM。PF-228阻断PC3(前列腺癌)、SKOV-3(卵巢癌)、L3.6p1和F-G(胰腺癌)以及MDCK细胞中的FAK Tyr397磷酸化,IC50为30-500 nM。在REF52细胞中,1-3 μM PF-228处理将FN-刺激的FAK Tyr397磷酸化减少约65-85%。10 μM PF-228阻断随机迁移并有效阻断血清和FN刺激的迁移。用1 μM PF-228处理培养物可显著降低单个细胞进入伤口的运动速率。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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.

生物活性

描述 PF-573228是一种ATP竞争性的FAK抑制剂,IC50值为4 nM。
靶点 FAK          
IC50 4 nM          

质量控制

化学结构

PF-573228

相关生物数据

PF-573228