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PZ0387

Sigma-Aldrich

PF-562,271

≥98% (HPLC)

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Synonym(s):
N-(3-(((2-((2,3-Dihydro-2-oxo-1H-indol-5-yl)amino)-5- (trifluoromethyl)-4-pyrimidinyl)amino)methyl)-2-pyridinyl)-N-methyl-methanesulfonamide benzenesulfonate, PF 562271, PF-00562271, PF-562271
Empirical Formula (Hill Notation):
C21H20F3N7O3S · C6H6O3S
CAS Number:
Molecular Weight:
665.66
MDL number:
UNSPSC Code:
41121800
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

color

white to brown

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

CN(S(=O)(C)=O)C1=NC=CC=C1CNC2=C(C(F)(F)F)C=NC(NC3=CC4=C(C=C3)NC(C4)=O)=N2.O=S(C5=CC=CC=C5)(O)=O

InChI

1S/C21H20F3N7O3S.C6H6O3S/c1-31(35(2,33)34)19-12(4-3-7-25-19)10-26-18-15(21(22,23)24)11-27-20(30-18)28-14-5-6-16-13(8-14)9-17(32)29-16;7-10(8,9)6-4-2-1-3-5-6/h3-8,11H,9-10H2,1-2H3,(H,29,32)(H2,26,27,28,30);1-5H,(H,7,8,9)

InChI key

LKLWTLXTOVZFAE-UHFFFAOYSA-N

Application

PF-562,271 has been used as a focal adhesion kinase (FAK) inhibitor to study its effects on the S100A9-induced tumor cell invasion in prostate cancer cell lines. It has also been used to study its effects on syndecan-1 (SDC-1) knockdown-induced upregulation of early growth regulator 1 (EGR1) in colon cancer cells.

Biochem/physiol Actions

PF-562,271 is a potent, ATP-competitive, reversible and selective inhibitor of FAK and Pyk2. PF-562,271 inhibits FAK phosphorylation in vivo.

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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Sampath Kumar Katakam et al.
Frontiers in oncology, 10, 774-774 (2020-06-02)
The heparan sulfate proteoglycan Syndecan-1 binds cytokines, morphogens and extracellular matrix components, regulating cancer stem cell properties and invasiveness. Syndecan-1 is modulated by the heparan sulfate-degrading enzyme heparanase, but the underlying regulatory mechanisms are only poorly understood. In colon cancer
Brittelle E Kessler et al.
Molecular cancer research : MCR, 14(9), 869-882 (2016-06-05)
There are limited therapy options for advanced thyroid cancer, including papillary and anaplastic thyroid cancer (PTC and ATC). Focal adhesion kinase (FAK) regulates cell signaling by functioning as a scaffold and kinase. Previously, we demonstrated that FAK is overexpressed and
Jayme B Stokes et al.
Molecular cancer therapeutics, 10(11), 2135-2145 (2011-09-10)
Current therapies for pancreatic ductal adenocarcinoma (PDA) target individual tumor cells. Focal adhesion kinase (FAK) is activated in PDA, and levels are inversely associated with survival. We investigated the effects of PF-562,271 (a small-molecule inhibitor of FAK/PYK2) on (i) in
Kimberleve Rolón-Reyes et al.
PloS one, 10(6), e0131059-e0131059 (2015-06-23)
Glioblastoma is one of the most aggressive and fatal brain cancers due to the highly invasive nature of glioma cells. Microglia infiltrate most glioma tumors and, therefore, make up an important component of the glioma microenvironment. In the tumor environment
Zhonghua Lv et al.
OncoTargets and therapy, 13, 6443-6452 (2020-09-05)
S100A9, which is expressed in prostate cancer, has been reported in association with prostate cancer progression. However, the role of S100A9 in prostate cancer metastasis is largely unknown. The aim of this study was to investigate the effect of S100A9

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