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Merck
CN

PZ0387

PF-562,271

≥98% (HPLC)

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

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About This Item

Empirical Formula (Hill Notation):
C21H20F3N7O3S · C6H6O3S
CAS Number:
Molecular Weight:
665.66
UNSPSC Code:
41121800
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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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.


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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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
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
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



Global Trade Item Number

SKUGTIN
PZ0387-25MG04061835503414
PZ0387-5MG04061835503421