Name: PF-573228
Brand: Selleck Chemicals
SKU: S2013
Rating: 5 (98 reviews)

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Control de calidad (Quality Control)

Lote: Pureza: 99.92%

99.92

Dianas relacionadas	EGFR VEGFR JAK FGFR PDGFR Src HIF HER2 FLT3 FLT
Otros FAK Inhibidores	Defactinib (VS-6063) PF-562271 (VS-6062) VS-4718 (PND-1186) PF-562271 HCl PF-562271 Besylate TAE226 (NVP-TAE226) GSK2256098 PF-431396 Y15 Solanesol (Nonaisoprenol)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Formulación	Descripción de la actividad	PMID
A431	Kinase assay	~10 μM	DMSO	inhibits FAK phosphorylation with IC50 of 11 nM	17395594
REF52	Kinase assay	~10 μM	DMSO	inhibits the phosphorylation of FAK Tyr397 with IC50 of ~100 nM	17395594
PC3	Kinase assay	~10 μM	DMSO	inhibits the phosphorylation of FAK Tyr397 with IC50 of 100 nM	17395594
SKOV-3	Kinase assay	~10 μM	DMSO	inhibits the phosphorylation of FAK Tyr397 with IC50 of 50 nM	17395594
L3.6p1	Kinase assay	~10 μM	DMSO	inhibits the phosphorylation of FAK Tyr397 with IC50 of 300 nM	17395594
F-G	Kinase assay	~10 μM	DMSO	inhibits the phosphorylation of FAK Tyr397 with IC50 of 30 nM	17395594
MDCK	Kinase assay	~10 μM	DMSO	inhibits the phosphorylation of FAK Tyr397 with IC50 of 500 nM	17395594
PC3	Growth inhibitory assay	10 μM	DMSO	significantly inhibits cell growth.	17395594
REF52	Growth inhibitory assay	10 μM	DMSO	significantly inhibits cell growth.	17395594
MDCK	Apoptosis assay	10 μM	DMSO	induces apoptosis	17395594
REF52	Apoptosis assay	10 μM	DMSO	induces apoptosis	17395594
REF52	Function assay	10 μM	DMSO	blocks serum and FN-stimulated migration	17395594
platelet	Function assay	1 μM	DMSO	inhibits platelet aggregation and spreading	19716803
platelet	Function assay	1 μM	DMSO	leads to inhibition of PAK and AKT	19716803
platelet	Function assay	1 μM	DMSO	blocks calcium mobilization and dense granule secretion	19716803
4T1	Function assay		DMSO	abolishes the interaction between β3 integrin and TβR-II	19740433
MCF7	Kinase assay	~10 μM	DMSO	inhibits the phosphorylation of FAK Tyr397 with IC50 of 430 nM	20354780
TamR	Kinase assay	~10 μM	DMSO	inhibits the phosphorylation of FAK Tyr397 with IC50 of 50 nM	20354780
FasR	Kinase assay	~10 μM	DMSO	inhibits the phosphorylation of FAK Tyr397 with IC50 of 130 nM	20354780
TamR	Function assay	1 μM	DMSO	inhibits cell migration	20354780
FasR	Function assay	1 μM	DMSO	inhibits cell migration	20354780
endothelial cell	Kinase assay	40 nM	DMSO	inhibits H2O2-induced phosphorylation of FAK	21212402
endothelial cell	Function assay	40 nM	DMSO	inhibits H2O2-induced stress fiber formation	21212402
endothelial cell	Apoptosis assay	40 nM	DMSO	inhibits apoptosis	21212402
GH3	Function assay	3 μM	DMSO	increases IK(Ca) amplitude	21925512
GH3	Function assay	3 μM	DMSO	enhances BKCa-channel activity	21925512
HUVEC	cytotoxicity assay	~10 μM	DMSO	impairs endothelial cell viability	22075057
HUVEC	Kinase assay	5 μM	DMSO	inhibits FAK kinase activity	22075057
HUVEC	Function assay	5 μM	DMSO	induces cell cycle arrest	22075057
HUVEC	Apoptosis assay	5 μM	DMSO	induces apoptosis	22075057
HUVEC	Function assay	5 μM	DMSO	impedes endothelial cell migration and alters the cellular actin cytoskeleton	22075057
HUVEC	Function assay	5 μM	DMSO	blocks HUVEC sprouting on collagen I gels	22075057
human peripheral blood T cells	Kinase assay	~10 μM	DMSO	inhibits site-specific phosphorylation of FAK	23928188
human peripheral blood T cells	Function assay	~10 μM	DMSO	impairs TCR-induced T cell morphological changes and alters activity of RhoA	23928188
human peripheral blood T cells	Function assay	~10 μM	DMSO	inhibits phosphorylation of ZAP-70 and LAT	23928188
human peripheral blood T cells	Function assay	~10 μM	DMSO	impairs Antigen-dependent T cell conjugation	23928188
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	491.49	Fórmula	C₂₂H₂₀F₃N₅O₃S	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	869288-64-2	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	N/A			Smiles	CS(=O)(=O)C1=CC=CC(=C1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)CC4

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 26 mg/mL (52.9 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	1.640mg/ml (3.34mM)	Taking the 1 mL working solution as an example, add 50 μL of 32.7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 2%Tween80 2 30%PEG300 3 63%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	5.000mg/ml (10.17mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 20 μL of Tween80, mix evenly to clarify it; add 300 μL PEG 300 to the above system, mix evenly to clarify; then continue to add 630 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC₅₀/Ki	FAK (Cell-free assay) 4 nM
In vitro	PF 573228 blocks the phosphorylation of FAK Tyr³⁹⁷ in REF52 cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of 30-500 nM. However, this compound (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with this chemical resulted in inhibition of serum or FN-directed migration and decreased focal adhesion turnover.
Ensayo de quinasa	Determinación de la afinidad
Ensayo de quinasa	El dominio cinasa de FAK activado purificado (aminoácidos 410–689) se hace reaccionar con 50 μM de ATP y 10 μg/pocillo de un polímero peptídico aleatorio de Glu y Tyr (relación molar de 4:1), poli(Glu/Tyr) en tampón de cinasa (50 mM HEPES, pH 7,5, 125 mM NaCl, 48 mM MgCl₂) durante 15 min. La fosforilación de poli(Glu/Tyr) se desafía con compuestos diluidos en serie a concentraciones de 1/2-Log, comenzando con una concentración máxima de 1 μM. Cada concentración se ejecuta por triplicado. La fosforilación de poli(Glu/Tyr) se detecta con un anticuerpo general anti-fosfotirosina (PY20), seguido de un anticuerpo IgG de cabra anti-ratón conjugado con peroxidasa de rábano picante. El sustrato estándar de peroxidasa de rábano picante 3, 3
In vivo	Inhibition of FAK by PF-573,228 in Ctrl-MT mice leads to a significant suppression of mammary tumorigenesis as well as lung metastasis. In contrast, treatment of MFCKO-MT mice with this compound did not affect the initiation of mammary tumors in these mice, as would be expected due to the absence of FAK in mammary epithelial cells of these mice .
Referencias	[1] http://www.ncbi.nlm.nih.gov/pubmed?term=17395594 [2] https://pubmed.ncbi.nlm.nih.gov/21471206/

Aplicaciones (Applications)

Métodos	Biomarcadores	PMID
Western blot	cyclin B1 p-FAK / FAK Lamin A / Lamin C	30761269
Immunofluorescence	FAK / F-actin Emerin	30761269
Growth inhibition assay	Cell viability	30761269

Preguntas frecuentes (Frequently Asked Questions)

Pregunta 1:
Would you please let me know the detail of how to dissolve it for in vivo study (oral administration)? This compound is referred to as Catalog No.S2013.

Respuesta:
A suspension of this compound in 30% PEG400+0.5% Tween80+ 5% Propylene glycol at 30mg/ml is fine for oral gavage.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

PF-573228 FAK inhibitor

Estructura química

Peso molecular: 491.49

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Aplicaciones (Applications)

Preguntas frecuentes (Frequently Asked Questions)

PF-573228 FAK inhibitor

Estructura química

Peso molecular: 491.49

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo (Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Aplicaciones (Applications)

Preguntas frecuentes (Frequently Asked Questions)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)