PF-573228
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PF573228是FAK的抑制剂,IC50值为4 nM[1]。
粘着斑激酶(FAK)是一种非受体蛋白酪氨酸激酶,驻留在粘着斑部位。FAK蛋白是由位于人染色体8q24上的FAK基因编码,分子量为125 kDa。FAK是细胞活性的重要介体,如细胞粘附、生长、增殖、存活、血管生成和迁移。据报道,正常组织的FAK要显著低于原发性和转移性肿瘤组织[2]。
PF573228是一种特异性的FAK抑制剂,被认为是有效的抗血管生成剂。在原代人脐静脉内皮细胞(HUVEC)中,PF573228通过抑制FAK的自磷酸化,从而增加细胞凋亡的比例,降低内皮细胞迁移和芽形成的能力[3]。在A431上皮癌细胞中,PF573228导致FAK磷酸化的减少,IC50值为11 nM。在许多其它的癌细胞中,如PC3细胞、SKOV-3细胞、L3.6p1 细胞、F-G细胞、和MDCK细胞,PF573228也抑制FAK的磷酸化,IC50范围介于30-500 nM之间[1]。在间充质干细胞(MSCs)中,PF573228通过抑制FAK的磷酸化,从而减少FaDu、MDA-MB-231、PC-3和NCI-H522来源的CM诱导的MSCs的促炎反应[4]。
据报道,PF573228也在BK(Ca)通道中起作用。在转染K(Ca)1.1 siRNAs的垂体瘤(GH(3))细胞中,3 μM PF573228刺激BK(Ca)通道活性,其随后可能影响细胞行为[5]。
参考文献:
[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.
- 1. Qi S, Sun X, et al. "FAK Promotes Early Osteoprogenitor Cell Proliferation by Enhancing mTORC1 Signaling." J Bone Miner Res. 2020;10.1002/jbmr.4029. PMID:32286710
- 2. Lee S, Jeon YM, et al. "PTK2/FAK regulates UPS impairment via QSTM1/p62 phosphorylation in TARDBP/TDP-43 proteinopathies." Autophagy. 2019 Nov 5:1-17. PMID:31690171
- 3. 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
Storage | Store at -20°C |
M.Wt | 491.49 |
Cas No. | 869288-64-2 |
Formula | C22H20F3N5O3S |
Solubility | insoluble in EtOH; insoluble in H2O; ≥166.6 mg/mL in DMSO |
Chemical Name | 6-[[4-[(3-methylsulfonylphenyl)methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-quinolin-2-one |
SDF | Download SDF |
Canonical SMILES | CS(=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 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
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 |
质量控制和MSDS
- 批次: