PF-562271 HCl
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 是一种强效的、ATP竞争性的和可逆的局部粘着斑激酶(FAK)和富含脯氨酸的酪氨酸激酶2 (Pyk2)抑制剂,半数最大抑制浓度(IC50)分别为1.5 nmol/L和14 nmol/L。FAK是一种参与多种细胞活动的非受体酪氨酸激酶,而Pyk2是一种含有48% 氨基酸同源性的FAK 同系物。据报道,作为用于癌症治疗的一种潜在的治疗剂,无论单一用药或是与其他治疗剂联合用药,PF-562271在异种移植和转基因小鼠模型中都有效抑制肿瘤的扩散,其中在带有肿瘤的小鼠中剂量依赖性地抑制FAK 磷酸化,半数最大有效浓度(EC50)为93 ng/mL。
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 | 543.95 |
Cas No. | 939791-41-0 |
Formula | C21H21ClF3N7O3S |
Synonyms | PF562271 HCl;PF 562271 HCl |
Solubility | ≥26.35 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH |
Chemical Name | N-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide hydrochloride |
SDF | Download SDF |
Canonical SMILES | O=C1NC2=C(C1)C=C(C=C2)NC3=NC=C(C(F)(F)F)C(NCC4=C(N(S(=O)(C)=O)C)N=CC=C4)=N3.Cl |
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。 |
Description | PF-562271 HCl,是PF-562271的盐酸盐,一种强效的、ATP竞争性的和可逆的FAK抑制剂,IC50值为1.5 nM,作用于Pyk2的效力比FAK弱约10倍,比对除某些CDKs以外的其他蛋白激酶的选择性高 100倍。 | |||||
靶点 | FAK | Pyk2 | ||||
IC50 | 1.5 nM | 14 nM |
质量控制和MSDS
- 批次: