PF-573228

For research use only.

Catalog No.S2013

61 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 61 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 NEXqfolMcW6jc3WgZZN{[Xl? NXzsXpNqhjFyIN88US=> MmfkSG1UVw>? M{fj[IlvcGmkaYTzJGZCUyCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEGxJI5O Ml7tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
REF52 MUPLbY5ie2ViYYPzZZk> NIH6Smd,OTBizszN NH;OSGlFVVOR NW\2fGtEcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iC-MUCwJI5O MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
PC3 M3TnU2tqdmG|ZTDhd5NigQ>? NIfRWYd,OTBizszN NH7VS49FVVOR MUTpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFExOCCwTR?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
SKOV-3 NEXzcHlMcW6jc3WgZZN{[Xl? NEPOR3N,OTBizszN NUXuWZU4TE2VTx?= Mlj3bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
L3.6p1 MmqxT4lv[XOnIHHzd4F6 NF7BPI9,OTBizszN M1;SSmROW09? M{LIXIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOzByIH7N M4HuR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
F-G NFrNO|lMcW6jc3WgZZN{[Xl? NEDWe5Z,OTBizszN MYrEUXNQ NFvrPYJqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDNyIH7N M{X0eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
MDCK MmnvT4lv[XOnIHHzd4F6 M2mxW54yOCEQvF2= Mn2ySG1UVw>? M1zOSolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPTByIH7N MoLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
PC3 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M373V|ExKM7:TR?= NXHJcpduTE2VTx?= NFLWdFV{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> NUTGcFV7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVU2QTRpPkG3N|k2PTl2PD;hQi=>
REF52 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXLSVlRSOTBizszN M4nQfmROW09? MlXQd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MnLYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
MDCK MofyRZBweHSxc3nzJIF{e2G7 Mn3BNVAh|ryP NHi1d41FVVOR M1O2W4lv\HWlZYOgZZBweHSxc3nz M2K3UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
REF52 NGrTT|ZCeG:ydH;zbZMh[XO|YYm= MUCxNEDPxE1? MlTpSG1UVw>? NGqzVHhqdmS3Y3XzJIFxd3C2b4Ppdy=> NIL0T3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{O5OVU6PCd-MUezPVU2QTR:L3G+
REF52 MnmwSpVv[3Srb36gZZN{[Xl? MmPPNVAh|ryP NIfaN4xFVVOR NX\E[XdP[myxY3vzJJNmenWvIHHu[EBHVi2|dHnteYxifGWmIH3p[5JifGmxbh?= M2faUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
platelet NVn4XotxTnWwY4Tpc44h[XO|YYm= MnrSNUDPxE1? M4Xqe2ROW09? MkHIbY5pcWKrdIOgdIxifGWuZYSgZYdoemWpYYTpc44h[W6mIIPwdoVi\GmwZx?= NHH1TGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUexOlgxOyd-MUm3NVY5ODN:L3G+
platelet Ml3xSpVv[3Srb36gZZN{[Xl? MVixJO69VQ>? NIXQ[I5FVVOR MXvs[YFleyC2bzDpcohq[mm2aX;uJI9nKFCDSzDhcoQhSUuW NFXkd3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUexOlgxOyd-MUm3NVY5ODN:L3G+
platelet NF7oTpRHfW6ldHnvckBie3OjeR?= M33SUlEh|ryP NFLyXnpFVVOR Ml7zZoxw[2u|IHPhcINqfW1ibX;ibYxqgmG2aX;uJIFv\CCmZX7z[UBoemGwdXzlJJNm[3KndHnvci=> M3W2NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{G2PFA{Lz5zOUexOlgxOzxxYU6=
4T1 MkPZSpVv[3Srb36gZZN{[Xl? NIX0VopFVVOR Mn7mZYJwdGm|aHXzJJRp\SCrboTldoFkfGmxbjDi[ZR4\WWwIN8yN{BqdnSnZ4LpckBidmRiVN8yVk1KUQ>? NIqyZVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe0NFQ{Oyd-MUm3OFA1OzN:L3G+
MCF7 NW\TVm9TU2mwYYPlJIF{e2G7 MV;+NVAh|ryP MnPLSG1UVw>? MmrobY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA1OzBibl2= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN3NEe4NEc,OjB|NUS3PFA9N2F-
TamR MXvLbY5ie2ViYYPzZZk> NFrLOXR,OTBizszN M{PQXmROW09? M1\iWIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPTBibl2= NG\iOIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO1OFc5OCd-MkCzOVQ4QDB:L3G+
FasR MWjLbY5ie2ViYYPzZZk> MYX+NVAh|ryP M4O1e2ROW09? NXvCU4ttcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iBzM{Cgcm0> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN3NEe4NEc,OjB|NUS3PFA9N2F-
TamR M{\IeWZ2dmO2aX;uJIF{e2G7 M4OwSVEh|ryP MofHSG1UVw>? NH3NPIhqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= NGn0WJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO1OFc5OCd-MkCzOVQ4QDB:L3G+
FasR MXrGeY5kfGmxbjDhd5NigQ>? M3;3bFEh|ryP MmrtSG1UVw>? NXj2PGkycW6qaXLpeJMh[2WubDDtbYdz[XSrb36= NVzRbpBERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzOVQ4QDBpPkKwN|U1PzhyPD;hQi=>
endothelial cell MXLLbY5ie2ViYYPzZZk> NUfYO4RnPDBibl2= NGHNOZJFVVOR NIPKOHhqdmirYnn0d{BJOk9{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJzMkSwNkc,OjF{MUK0NFI9N2F-
endothelial cell M1zzSGZ2dmO2aX;uJIF{e2G7 MUW0NEBvVQ>? NX3pcmt6TE2VTx?= NEfyWmFqdmirYnn0d{BJOk9{LXnu[JVk\WRic4Ty[ZN{KG[rYnXyJIZwem2jdHnvci=> NXLKV2F4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyNVI1ODJpPkKxNlEzPDB{PD;hQi=>
endothelial cell NIj0[XRCeG:ydH;zbZMh[XO|YYm= NYf0XnFWPDBibl2= M1XJ[mROW09? M1XyVYlvcGmkaYTzJIFxd3C2b4Ppdy=> NWDSPWt6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyNVI1ODJpPkKxNlEzPDB{PD;hQi=>
GH3 M1m2[mZ2dmO2aX;uJIF{e2G7 M{T1RlMh|ryP NXjEUpk1TE2VTx?= M{O2VYlv[3KnYYPld{BKUyiFYTmgZY1xdGm2dXTl MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl{NUWxNkc,OjF7MkW1NVI9N2F-
GH3 M{\rUGZ2dmO2aX;uJIF{e2G7 NFTLNos{KM7:TR?= MojHSG1UVw>? NUKwNJhr\W6qYX7j[ZMhSkuFYT3jbIFvdmWuIHHjeIl3cXS7 M3;WU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUK1OVEzLz5{MUmyOVUyOjxxYU6=
HUVEC MmTXZ5l1d3SxeHnjbZR6KGG|c3H5 M1zocJ4yOCEQvF2= NUnKZVdSTE2VTx?= NUDyU|IxcW2yYXnyd{BmdmSxdHjlcIlidCClZXzsJJZq[WKrbHn0fS=> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5NUC1O{c,OjJyN{WwOVc9N2F-
HUVEC MYrLbY5ie2ViYYPzZZk> M4Xn[lUh|ryP NVr6PYV5TE2VTx?= M2HKUolvcGmkaYTzJGZCUyCtaX7hd4Uh[WO2aY\peJk> Mlv3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{WwOVcoRjJ{MEe1NFU4RC:jPh?=
HUVEC M37KTWZ2dmO2aX;uJIF{e2G7 NIO2WI42KM7:TR?= MUXEUXNQ NF;mNpVqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M4HXZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe1NFU4Lz5{MkC3OVA2PzxxYU6=
HUVEC NXHSWJVKSXCxcITvd4l{KGG|c3H5 MnrZOUDPxE1? MnjSSG1UVw>? NFzHUI1qdmS3Y3XzJIFxd3C2b4Ppdy=> NHXz[3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3OVA2Pyd-MkKwO|UxPTd:L3G+
HUVEC M1jETGZ2dmO2aX;uJIF{e2G7 MUe1JO69VQ>? M{Pa[mROW09? NXHXN|JjcW2yZXTld{BmdmSxdHjlcIlidCClZXzsJI1q\3KjdHnvckBidmRiYXz0[ZJ{KHSqZTDj[YxtfWyjcjDhZ5RqdiCleYTvd4tmdGW2b36= M4GyWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe1NFU4Lz5{MkC3OVA2PzxxYU6=
HUVEC MoizSpVv[3Srb36gZZN{[Xl? NGfqc5I2KM7:TR?= NWH6Rpo4TE2VTx?= MmHLZoxw[2u|IFjVWmVEKHOycn;1eIlv\yCxbjDjc4xt[WenbjDJJIdmdHN? NYXpVI5pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|UxPTdpPkKyNFc2ODV5PD;hQi=>
human peripheral blood T cells MnHjT4lv[XOnIHHzd4F6 M2\WWJ4yOCEQvF2= MmXQSG1UVw>? MmLBbY5pcWKrdIOgd4l1\S2|cHXjbYZq[yCyaH;zdIhwenmuYYTpc44hd2ZiRlHL MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl{OEG4PEc,OjN7MkixPFg9N2F-
human peripheral blood T cells NG\1R4NHfW6ldHnvckBie3OjeR?= NHe5dGx,OTBizszN MlXOSG1UVw>? NYDlbmNucW2yYXnyd{BVS1JvaX7keYNm\CCWIHPlcIwhdW:{cHjvcI9ocWOjbDDjbIFv\2W|IHHu[EBidHSncoOgZYN1cX[rdImgc4YhWmixQR?= M174Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUK4NVg5Lz5{M{myPFE5QDxxYU6=
human peripheral blood T cells MoLESpVv[3Srb36gZZN{[Xl? M3z3Zp4yOCEQvF2= NFPjU5BFVVOR MV7pcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gXmFRNTdyIHHu[EBNSVR? MljMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MkixPFgoRjJ|OUK4NVg5RC:jPh?=
human peripheral blood T cells NUfnOJZnTnWwY4Tpc44h[XO|YYm= MkfGglExKM7:TR?= M4LMU2ROW09? NG\zcGlqdXCjaYLzJGFvfGmpZX6t[IVx\W6mZX70JHQh[2WubDDjc45rfWejdHnvci=> M4\5OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUK4NVg5Lz5{M{myPFE5QDxxYU6=
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Saos-2 MVjxTHRUKGG|c3H5 MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NXTKNm9CRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 MYPxTHRUKGG|c3H5 M4XoZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= NEfuTVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD MofPdWhVWyCjc4PhfS=> NGm1Oo9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? NGSx[o89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH MlLZdWhVWyCjc4PhfS=> M1Lae5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz MlzWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) NHPjXmdyUFSVIHHzd4F6 NH3S[I1yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO= M3KxOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 NHO0c3lyUFSVIHHzd4F6 MV7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| NWnmNmE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NEXsUHlyUFSVIHHzd4F6 M1WzNpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NFX6e2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MlnCdWhVWyCjc4PhfS=> MlzZdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NYL1[5NxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC MWLxTHRUKGG|c3H5 M{XafpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz NHHxVIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 NES3NXlyUFSVIHHzd4F6 NWT1b2FPeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MmH5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 NXvRZlhSeUiWUzDhd5NigQ>? MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NFOwUG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+

... 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 SDS / 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 SDS / 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):
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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.

  • * Indicates a Required Field

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