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PF-573228

For research use only.

Catalog No.S2013

54 publications

PF-573228 Chemical Structure

CAS No. 869288-64-2

PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis.

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Selleck's PF-573228 has been cited by 54 publications

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Choose Selective FAK Inhibitors

Biological Activity

Description PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis.
Targets
FAK [1]
(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, PF 573228 (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with PF-228 resulted in inhibition of serum or FN-directed migration and decreased focal adhesion turnover. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A431 NVvJbW1WU2mwYYPlJIF{e2G7 NYnKbJpNhjFyIN88US=> MnzOSG1UVw>? M{Xt[IlvcGmkaYTzJGZCUyCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEGxJI5O MofiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
REF52 NUHi[5BDU2mwYYPlJIF{e2G7 MlHlglExKM7:TR?= MW\EUXNQ NXLvSZFocW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iC-MUCwJI5O M2CyRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
PC3 NH3ORlZMcW6jc3WgZZN{[Xl? MYj+NVAh|ryP NYruPZR{TE2VTx?= M3q3bolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTByIH7N M3nJXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
SKOV-3 MWnLbY5ie2ViYYPzZZk> NGTQZnd,OTBizszN MWHEUXNQ M3\wN4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPTBibl2= NXO0UoJKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVU2QTRpPkG3N|k2PTl2PD;hQi=>
L3.6p1 MVzLbY5ie2ViYYPzZZk> Mn3EglExKM7:TR?= NV[xOoxpTE2VTx?= MXXpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFMxOCCwTR?= NVS0TpFERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVU2QTRpPkG3N|k2PTl2PD;hQi=>
F-G M3;lW2tqdmG|ZTDhd5NigQ>? MWr+NVAh|ryP M4PsO2ROW09? MUHpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFMxKG6P NX36OHZWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVU2QTRpPkG3N|k2PTl2PD;hQi=>
MDCK M{O2PGtqdmG|ZTDhd5NigQ>? NX;0XVA1hjFyIN88US=> M13ufmROW09? MlnxbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2ODBibl2= NYnUO2RNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVU2QTRpPkG3N|k2PTl2PD;hQi=>
PC3 M4e0SWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUKxNEDPxE1? MmnVSG1UVw>? M{PYXZNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NXHxUIZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVU2QTRpPkG3N|k2PTl2PD;hQi=>
REF52 MlnUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlXPNVAh|ryP MknESG1UVw>? M3vjbpNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu MnHxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
MDCK M4DyR2Fxd3C2b4Ppd{Bie3OjeR?= M4exdVExKM7:TR?= M3HhZ2ROW09? M17GR4lv\HWlZYOgZZBweHSxc3nz MlXZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
REF52 NUTtXVZJSXCxcITvd4l{KGG|c3H5 NW\2eoE4OTBizszN M{T5OGROW09? MmnQbY5lfWOnczDhdI9xfG:|aYO= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
REF52 M{XUU2Z2dmO2aX;uJIF{e2G7 MlvSNVAh|ryP NHnaNm5FVVOR NG\hOY9jdG:la4Ogd4VzfW1iYX7kJGZPNXO2aX31cIF1\WRibXnndoF1cW:w MoPSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
platelet NGrN[plHfW6ldHnvckBie3OjeR?= MljUNUDPxE1? NFnR[mtFVVOR NX7LT3lycW6qaXLpeJMheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJJNxemWjZHnu[y=> NGr5UpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUexOlgxOyd-MUm3NVY5ODN:L3G+
platelet NYTxdlJJTnWwY4Tpc44h[XO|YYm= M{XmXFEh|ryP NXnnZWlsTE2VTx?= NIDaeWVt\WGmczD0c{BqdmirYnn0bY9vKG:oIGDBT{BidmRiQVvU MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTdzNkiwN{c,OTl5MU[4NFM9N2F-
platelet MlrKSpVv[3Srb36gZZN{[Xl? MlvaNUDPxE1? NF;qOGdFVVOR M4K2cYJtd2OtczDjZYxkcXWvIH3vZoltcXqjdHnvckBidmRiZHXud4Uh\3KjboXs[UB{\WO{ZYTpc44> M37rVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{G2PFA{Lz5zOUexOlgxOzxxYU6=
4T1 MoP6SpVv[3Srb36gZZN{[Xl? MnvSSG1UVw>? NUf0TVNv[WKxbHnzbIV{KHSqZTDpcpRmemGldHnvckBj\XS5ZXXuJO6zOyCrboTl[5JqdiCjbnSgWO6zWi2LSR?= MoTEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5NEC0N|MoRjF7N{SwOFM{RC:jPh?=
MCF7 Mo\1T4lv[XOnIHHzd4F6 NF\IW2h,OTBizszN NV60U2F{TE2VTx?= M3[5SolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPDNyIH7N MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN3NEe4NEc,OjB|NUS3PFA9N2F-
TamR NYTzSZU5U2mwYYPlJIF{e2G7 MnPSglExKM7:TR?= M2HGPWROW09? MlT1bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= NVjydGtmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzOVQ4QDBpPkKwN|U1PzhyPD;hQi=>
FasR M3rPPGtqdmG|ZTDhd5NigQ>? MlfTglExKM7:TR?= NYTZdm1ETE2VTx?= NIfKOGVqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDF|MDDuUS=> M1GzdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{W0O|gxLz5{MEO1OFc5ODxxYU6=
TamR MWHGeY5kfGmxbjDhd5NigQ>? NEGzS4MyKM7:TR?= MVrEUXNQ NH\BUW5qdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN3NEe4NEc,OjB|NUS3PFA9N2F-
FasR NHfyZnZHfW6ldHnvckBie3OjeR?= NHvjdlIyKM7:TR?= MkHQSG1UVw>? NFK3RphqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= NEOxeHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO1OFc5OCd-MkCzOVQ4QDB:L3G+
endothelial cell NELoenpMcW6jc3WgZZN{[Xl? NF[wUmI1OCCwTR?= NES4R|dFVVOR NIryfpdqdmirYnn0d{BJOk9{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=> MkDMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{MUK0NFIoRjJzMkGyOFAzRC:jPh?=
endothelial cell M{X1W2Z2dmO2aX;uJIF{e2G7 MUG0NEBvVQ>? MXrEUXNQ MYXpcohq[mm2czDINm8zNWmwZIXj[YQhe3S{ZYPzJIZq[mW{IH\vdo1ifGmxbh?= NWC4Z5NjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyNVI1ODJpPkKxNlEzPDB{PD;hQi=>
endothelial cell M1jsSGFxd3C2b4Ppd{Bie3OjeR?= MkP6OFAhdk1? M3vodGROW09? NWDUWYRmcW6qaXLpeJMh[XCxcITvd4l{ NWD5ToRURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyNVI1ODJpPkKxNlEzPDB{PD;hQi=>
GH3 M3zaSmZ2dmO2aX;uJIF{e2G7 MlPrN{DPxE1? MXXEUXNQ NX7Qc2hHcW6lcnXhd4V{KEmNKFPhLUBidXCuaYT1[IU> NVvETFJmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NlU2OTJpPkKxPVI2PTF{PD;hQi=>
GH3 NIDsN2RHfW6ldHnvckBie3OjeR?= NGTzO3Y{KM7:TR?= NIPpPFJFVVOR NGXTenBmdmijbnPld{BDU0OjLXPoZY5v\WxiYXP0bZZqfHl? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl{NUWxNkc,OjF7MkW1NVI9N2F-
HUVEC M2rZfoN6fG:2b4jpZ4l1gSCjc4PhfS=> NWPiVHdvhjFyIN88US=> MnXuSG1UVw>? M3m2XIlueGGrcoOg[Y5ld3SqZXzpZYwh[2WubDD2bYFjcWyrdIm= NHTkcZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3OVA2Pyd-MkKwO|UxPTd:L3G+
HUVEC M4fBWWtqdmG|ZTDhd5NigQ>? MkXZOUDPxE1? NYL3W29LTE2VTx?= NH\jd3VqdmirYnn0d{BHSUtia3nuZZNmKGGldHn2bZR6 MofEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{WwOVcoRjJ{MEe1NFU4RC:jPh?=
HUVEC MmjCSpVv[3Srb36gZZN{[Xl? M1[yTVUh|ryP NGHmdJhFVVOR M1nsbolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NHvlOIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3OVA2Pyd-MkKwO|UxPTd:L3G+
HUVEC NVztUmhHSXCxcITvd4l{KGG|c3H5 MkWzOUDPxE1? NXTsRWhDTE2VTx?= MWXpcoR2[2W|IHHwc5B1d3Orcx?= NVjHS4FLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|UxPTdpPkKyNFc2ODV5PD;hQi=>
HUVEC NG\rWnZHfW6ldHnvckBie3OjeR?= M1XWRVUh|ryP NF3RZmVFVVOR Ml3YbY1x\WSnczDlcoRwfGinbHnhcEBk\WyuIH3p[5JifGmxbjDhcoQh[Wy2ZYLzJJRp\SClZXzseYxieiCjY4TpckBkgXSxc3vlcIV1d25? Mlj2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{WwOVcoRjJ{MEe1NFU4RC:jPh?=
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human peripheral blood T cells NX7uOXFwU2mwYYPlJIF{e2G7 NVK4bm1XhjFyIN88US=> NHvYWJBFVVOR MmrqbY5pcWKrdIOgd4l1\S2|cHXjbYZq[yCyaH;zdIhwenmuYYTpc44hd2ZiRlHL M4OzcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUK4NVg5Lz5{M{myPFE5QDxxYU6=
human peripheral blood T cells MnPNSpVv[3Srb36gZZN{[Xl? NWfJdld{hjFyIN88US=> MYTEUXNQ NG\uXpFqdXCjaYLzJHREWi2rbnT1Z4VlKFRiY3XscEBud3KyaH;sc4dq[2GuIHPoZY5o\XNiYX7kJIFtfGW{czDhZ5Rqfmm2eTDv[kBTcG:D NXf2dG0xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NlgyQDhpPkKzPVI5OTh6PD;hQi=>
human peripheral blood T cells MoDGSpVv[3Srb36gZZN{[Xl? M{LseZ4yOCEQvF2= M1zQ[GROW09? MnSzbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHpCWC15MDDhcoQhVEGW M3Lle|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUK4NVg5Lz5{M{myPFE5QDxxYU6=
human peripheral blood T cells M3rEO2Z2dmO2aX;uJIF{e2G7 MoD5glExKM7:TR?= NH;acIdFVVOR M37CfolueGGrcoOgRY51cWenbj3k[ZBmdmSnboSgWEBk\WyuIHPvcop2\2G2aX;u NFqz[VM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{myPFE5QCd-MkO5NlgyQDh:L3G+
U-2 OS MnPVdWhVWyCjc4PhfS=> M1e3eZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCXLUKgU3Mh[2WubIO= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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Saos-2 MWTxTHRUKGG|c3H5 M37WdJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= M2DmUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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RD NWnReo5PeUiWUzDhd5NigQ>? NY\qfnR3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLEJINmdGy| NG\SWYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH NU\XWHRneUiWUzDhd5NigQ>? M2ftR5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz M2G1UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) NInwRXdyUFSVIHHzd4F6 Mn\MdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| NYrWbY8zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 NGS2d|ByUFSVIHHzd4F6 NIL6S5RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz Mnf1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 MlO4dWhVWyCjc4PhfS=> NWfINJdUeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 Mof0dWhVWyCjc4PhfS=> MnfHdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= Mn7yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC M1fnOpFJXFNiYYPzZZk> MoPKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MnrwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 NVf4b5Q6eUiWUzDhd5NigQ>? NV\yc3FHeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> M1PZXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 NHjRU4tyUFSVIHHzd4F6 MmOxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MnTDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
cyclin B1; 

PubMed: 30761269     


(D) On the third day, PF-573228-treated cells were harvested and subjected to Western blot analysis for cyclin B1. Cyclin B1 levels were much higher in A549 cells with 1 μM PF-573228 or without PF-573228 treatment than in the cells treated with higher concentrations of PF-573228. (E) After 10 μM PF-573228 treatment, cyclin B1 levels declined markedly in H460 cells. (F) PF-573228 administration slightly reduced cyclin B1 levels in H1299 cells. 

p-FAK / FAK ; 

PubMed: 30761269     


FAK expression levels and FAK activity, as measured by the phosphorylation of FAK at tyrosine 576 and 577, were quantified by Western blot analysis after treatment of lung cancer cells with PF-573228 for 3 days.

Lamin A / Lamin C; 

PubMed: 30761269     


(B) The cells treated with 10 μM PF-573228 exhibited a decrease in p-FAK levels. Lamin A and lamin C expression levels were much lower in A549 cells exposed to 10 μM PF-573228. 

30761269
Immunofluorescence
FAK / F-actin; 

PubMed: 30761269     


(B) The cells were stained with phalloidin to visualize F-actin (red) and a FAK antibody to visualize the FAK distribution (green). In cells without PF-573228 administration, FAK translocated to focal adhesions at the tips of actin stress fibers, and the focal adhesions were relatively large. When cells were exposed to 10 μM PF-573228, FAK translocation to focal adhesions was reduced, and the sizes of the focal adhesions were smaller. Nuclei in cells treated with PF-573228 were deformed, as visualized with DAPI staining, whereas most nuclei in cells without PF-573228 treatment were oval shaped. 

Emerin; 

PubMed: 30761269     


(A) After PF-573228 treatment of A549 cells, the cells were fixed and stained with phalloidin to label F-actin (red) and an antibody against emerin (green) to outline the nuclear shape. Cells treated with PF-573228 were extremely large and had deformed nuclei, whereas mostly oval-like nuclei were present in the cells without PF-573228 treatment. 

30761269
Growth inhibition assay
Cell viability; 

PubMed: 30761269     


Three different types of lung cancer cells, (A) A549 lung adenocarcinoma and (B) H460, and (C) H1299 large cell carcinoma, were selected for the PF-573228 administration regimen. Cell growth curves of the three lung cancer cell lines treated with various doses of PF-573228 for 4 days were established. The administration of PF-573228 at 10 μM to the lung cancer cells effectively suppressed cell growth in vitro, as proliferative activity totally ceased in the cells exposed to 10 μM PF-573228.

30761269
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 PF-573,228 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 [2].

Protocol

Kinase Assay:

[1]
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Affinity determination:

Purified activated FAK kinase domain (amino acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3
Cell Research:

[1]
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  • Cell lines: REF52 or PC3 cells
  • Concentrations: ~10 μM
  • Incubation Time: 3 days
  • Method:

    Growth assays are performed by seeding 1 × 104 REF52 or PC3 cells/well of a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor for 3 days. Subsequently, the cells are harvested and counted.


    (Only for Reference)
Animal Research:

[2]
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  • Animal Models: Ctrl-MT and MFCKO-MT mice
  • Dosages: 5 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 26 mg/mL (52.9 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+2% Tween 80+30% PEG 300+ddH2O
For best results, use promptly after mixing. 		5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 491.49
Formula

C22H20F3N5O3S
CAS No. 869288-64-2
Storage powder
in solvent
Synonyms 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
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    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    Would you please let me know the detail of how to dissolve PF-573228 (Catalog No.S2013) for in vivo study (oral administration)?

  • Answer:

    PF-573228 in 30% PEG400+0.5% Tween80+ 5% Propylene glycol at 30mg/ml is a suspension. If you will use the compound for oral gavage, this suspension is fine for it.

selleck catalog

FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID