PF-00562271
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.
PF-562271是一种有效的、ATP竞争性的和可逆的FAK/Pyk2抑制剂,相应IC50值为1.5 nmol/L和14 nmol/L。粘着斑激酶(FAK)是一种非受体酪氨酸激酶,参与多种细胞活动,而富含脯氨酸的酪氨酸激酶2(Pyk2)与FAK同源,具有48%的氨基酸序列一致性。PF-562271作为一个潜在的抗癌药物,可以单独使用或与其它抗癌药物联合使用。据报道,在异种移植和转基因小鼠模型中,PF-562271呈剂量依赖性地抑制荷瘤小鼠中的FAK磷酸化(EC50 = 93 ng/mL),有效地抑制肿瘤增殖。
参考文献:
[1]Stokes JB, Adair SJ, Slack-Davis JK, Walters DM, Tilghman RW, Hershey ED, Lowrey B, Thomas KS, Bouton AH, Hwang RF, Stelow EB, Parsons JT, Bauer TW. Inhibition of focal adhesion kinase by PF-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. Mol Cancer Ther. 2011 Nov;10(11):2135-45. doi: 10.1158/1535-7163.MCT-11-0261. Epub 2011 Sep 8.
[2]Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J, Coleman K, Yao L, Martinez-Alsina L, Lorenzen M, Berliner M, Luzzio M, Patel N, Schmitt E, LaGreca S, Jani J, Wessel M, Marr E, Griffor M, Vajdos F. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res. 2008 Mar 15;68(6):1935-44. doi: 10.1158/0008-5472.CAN-07-5155.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 665.66 |
Cas No. | 939791-38-5 |
Formula | C21H20F3N7O3S·C6H6O3S |
Synonyms | PF-562271;PF00562271;PF62271 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥11.1 mg/mL in DMSO with gentle warming |
Chemical Name | benzenesulfonic acid;N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide |
SDF | Download SDF |
Canonical SMILES | CN(C1=C(C=CC=N1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)C4)S(=O)(=O)C.C1=CC=C(C=C1)S(=O)(=O)O |
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 |
鳞状细胞癌细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。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 μM,48 hr |
应用 |
在鳞状细胞癌中,用FAK激酶抑制剂PF-562,271处理表达野生型FAK的细胞,导致细胞迁移减少,在FAK-/-细胞中有类似情况。PF-562,271以剂量依赖性方式抑制FAK Y397的自磷酸化。PF-562,271抑制高尔基体朝向。在PF-562,271处理细胞中,PF-562,271抑制Pyk2和Pyk2自磷酸化。在FAK wt细胞中,PF-562,271以剂量依赖性方式抑制细胞增殖。在FAK wt细胞中,PF-562,271(0.25 μM)以剂量依赖性方式抑制集落形成。用溶解在甲基纤维素中的PF-562,271处理导致微小但显著地降低S期细胞数量,而对应的G1期细胞数量的增加不显著。 |
动物实验 [2,3]: | |
动物模型 |
携带PC-3M、BT474、BxPc3和LoVo肿瘤的小鼠 |
给药剂量 |
口服,25-50 mg/kg,每天两次 |
应用 |
在几个人类皮下异种移植模型中,PF-562271以剂量依赖性方式抑制肿瘤生长,并且对PC-3M、BT474、BxPc3和LoVo产生最大的肿瘤抑制,剂量为25至50 mg/kg,每天两次,其抑制率为78%至94%,无体重下降、发病或死亡现象。口服PF-562271(25 mg/kg)显著降低皮下和骨转移PC3M-luc-C6异种移植模型中的肿瘤进展。 |
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]. Serrels A, McLeod K, Canel M, et al. The role of focal adhesion kinase catalytic activity on the proliferation and migration of squamous cell carcinoma cells[J]. International journal of cancer, 2012, 131(2): 287-297. [2]. Roberts W G, Ung E, Whalen P, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271[J]. Cancer research, 2008, 68(6): 1935-1944. [3]. Roberts W G, Ung E, Whalen P, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271[J]. Cancer research, 2008, 68(6): 1935-1944. |
Description | PF-00562271,PF-562271的苯磺酸盐,是一种有效的、ATP竞争性的和可逆的FAK抑制剂,其IC50值为1.5 nM,而其对Pyk2的效力约少10倍。PF-00562271对FAK的选择性比对其它蛋白激酶(除一些CDK外)高100倍以上。 | |||||
靶点 | FAK | Pyk2 | ||||
IC50 | 1.5 nM | 14 nM |
质量控制和MSDS
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