PF-573228

Catalog No.S2013

For research use only.

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.

PF-573228 Chemical Structure

CAS No. 869288-64-2

Selleck's PF-573228 has been cited by 73 publications

Purity & Quality Control

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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 NF:3WVNMcW6jc3WgZZN{[Xl? NXfzWpY5hjFyIN88US=> MoqwSG1UVw>? NWHxO3ZscW6qaXLpeJMhTkGNIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNVEhdk1? MoDBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
REF52 M2DPSmtqdmG|ZTDhd5NigQ>? M2G2eJ4yOCEQvF2= MnjNSG1UVw>? NGW5N4JqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKH5zMECgcm0> M1nVOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
PC3 MV3LbY5ie2ViYYPzZZk> M{nh[54yOCEQvF2= M{GxbmROW09? NYfVXpRKcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iBzMECgcm0> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
SKOV-3 Ml60T4lv[XOnIHHzd4F6 NHvUcJR,OTBizszN M2mwd2ROW09? MYnpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFUxKG6P MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
L3.6p1 NVvKN2RtU2mwYYPlJIF{e2G7 Mn7nglExKM7:TR?= NI\ydldFVVOR MVPpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFMxOCCwTR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
F-G NGPyRXpMcW6jc3WgZZN{[Xl? M2n2Rp4yOCEQvF2= NIHP[|BFVVOR M{LifYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOzBibl2= M2TuXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
MDCK M{DTfmtqdmG|ZTDhd5NigQ>? MUT+NVAh|ryP NITZdo1FVVOR NUizdHZOcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB3MECgcm0> NEXHSFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{O5OVU6PCd-MUezPVU2QTR:L3G+
PC3 NVnnOlFoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoDQNVAh|ryP NXXKXZo{TE2VTx?= NYq0bpZZe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> NV\Bbm9mRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVU2QTRpPkG3N|k2PTl2PD;hQi=>
REF52 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnntNVAh|ryP NWnze4NjTE2VTx?= NWLhRoQ1e2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> NYrMd49iRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVU2QTRpPkG3N|k2PTl2PD;hQi=>
MDCK NUnBS|FWSXCxcITvd4l{KGG|c3H5 M3PLXFExKM7:TR?= MU\EUXNQ MXfpcoR2[2W|IHHwc5B1d3Orcx?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
REF52 NWDQS4JMSXCxcITvd4l{KGG|c3H5 MmLiNVAh|ryP NHn1RYFFVVOR MV3pcoR2[2W|IHHwc5B1d3Orcx?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
REF52 NVPVWJpITnWwY4Tpc44h[XO|YYm= M4W5O|ExKM7:TR?= NV3nfWl6TE2VTx?= M4izXoJtd2OtczDz[ZJ2dSCjbnSgSm4ue3SrbYXsZZRm\CCvaXfyZZRqd25? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
platelet MojPSpVv[3Srb36gZZN{[Xl? M3XI[VEh|ryP MUDEUXNQ NVLnWY43cW6qaXLpeJMheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJJNxemWjZHnu[y=> NYDjWHptRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3NVY5ODNpPkG5O|E3QDB|PD;hQi=>
platelet M1jYXGZ2dmO2aX;uJIF{e2G7 M2fUN|Eh|ryP Mn;YSG1UVw>? MUjs[YFleyC2bzDpcohq[mm2aX;uJI9nKFCDSzDhcoQhSUuW NYq0RpR5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3NVY5ODNpPkG5O|E3QDB|PD;hQi=>
platelet MUXGeY5kfGmxbjDhd5NigQ>? NXnwPVN3OSEQvF2= NXPycYJ2TE2VTx?= M4jiRYJtd2OtczDjZYxkcXWvIH3vZoltcXqjdHnvckBidmRiZHXud4Uh\3KjboXs[UB{\WO{ZYTpc44> NX31b|lnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3NVY5ODNpPkG5O|E3QDB|PD;hQi=>
4T1 NUPmW2ViTnWwY4Tpc44h[XO|YYm= MoroSG1UVw>? NXfuSWl7[WKxbHnzbIV{KHSqZTDpcpRmemGldHnvckBj\XS5ZXXuJO6zOyCrboTl[5JqdiCjbnSgWO6zWi2LSR?= M2H5fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{SwOFM{Lz5zOUe0NFQ{OzxxYU6=
MCF7 M4DS[2tqdmG|ZTDhd5NigQ>? NVfafWd1hjFyIN88US=> MmHqSG1UVw>? MnzabY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA1OzBibl2= Ml:wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|NUS3PFAoRjJyM{W0O|gxRC:jPh?=
TamR MVfLbY5ie2ViYYPzZZk> NV\rOlQ{hjFyIN88US=> NHrKcYhFVVOR MmK5bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= M2XycVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{W0O|gxLz5{MEO1OFc5ODxxYU6=
FasR MULLbY5ie2ViYYPzZZk> MYn+NVAh|ryP MXfEUXNQ NUnFOFBscW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iBzM{Cgcm0> MkfHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|NUS3PFAoRjJyM{W0O|gxRC:jPh?=
TamR Mn;0SpVv[3Srb36gZZN{[Xl? MUixJO69VQ>? M2WwcWROW09? NIDPdnBqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MmnjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|NUS3PFAoRjJyM{W0O|gxRC:jPh?=
FasR NVyx[HRnTnWwY4Tpc44h[XO|YYm= MWmxJO69VQ>? MnXMSG1UVw>? M4fP[YlvcGmkaYTzJINmdGxibXnndoF1cW:w M1X0e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{W0O|gxLz5{MEO1OFc5ODxxYU6=
endothelial cell NEnlSIRMcW6jc3WgZZN{[Xl? NVnRXHN2PDBibl2= M1jtd2ROW09? Ml:1bY5pcWKrdIOgTFJQOi2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCIQVu= NF\CU2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKxNlQxOid-MkGyNVI1ODJ:L3G+
endothelial cell NEDhU3dHfW6ldHnvckBie3OjeR?= MUS0NEBvVQ>? NGnqbItFVVOR MnjkbY5pcWKrdIOgTFJQOi2rbnT1Z4VlKHO2cnXzd{BncWKncjDmc5Ju[XSrb36= NF74fVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKxNlQxOid-MkGyNVI1ODJ:L3G+
endothelial cell MXzBdI9xfG:|aYOgZZN{[Xl? MmLROFAhdk1? M2XPV2ROW09? M4P3T4lvcGmkaYTzJIFxd3C2b4Ppdy=> NIiyepM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKxNlQxOid-MkGyNVI1ODJ:L3G+
GH3 MnTaSpVv[3Srb36gZZN{[Xl? NYTzTVZHOyEQvF2= M1\4S2ROW09? MWXpcoNz\WG|ZYOgTWspS2FrIHHtdIxqfHWmZR?= NULpN4FORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NlU2OTJpPkKxPVI2PTF{PD;hQi=>
GH3 MX\GeY5kfGmxbjDhd5NigQ>? M3ryXFMh|ryP MX7EUXNQ NXLZdYpm\W6qYX7j[ZMhSkuFYT3jbIFvdmWuIHHjeIl3cXS7 MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl{NUWxNkc,OjF7MkW1NVI9N2F-
HUVEC NUPRS|lx[3m2b4TvfIlkcXS7IHHzd4F6 MkL3glExKM7:TR?= NHzPOpdFVVOR MVzpcZBicXK|IHXu[I91cGWuaXHsJINmdGxidnnhZoltcXS7 MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5NUC1O{c,OjJyN{WwOVc9N2F-
HUVEC M4nxemtqdmG|ZTDhd5NigQ>? MUC1JO69VQ>? MnvVSG1UVw>? NHixenhqdmirYnn0d{BHSUtia3nuZZNmKGGldHn2bZR6 NEjzTHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3OVA2Pyd-MkKwO|UxPTd:L3G+
HUVEC NF\jVXdHfW6ldHnvckBie3OjeR?= MmT5OUDPxE1? NYjLU4lxTE2VTx?= NGLJUppqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5NUC1O{c,OjJyN{WwOVc9N2F-
HUVEC M3f4NWFxd3C2b4Ppd{Bie3OjeR?= MW[1JO69VQ>? M{PZe2ROW09? M2TueYlv\HWlZYOgZZBweHSxc3nz MonsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{WwOVcoRjJ{MEe1NFU4RC:jPh?=
HUVEC NF;aUXZHfW6ldHnvckBie3OjeR?= NWfYPZkzPSEQvF2= NWD6fWczTE2VTx?= M3jtcolueGWmZYOg[Y5ld3SqZXzpZYwh[2WubDDtbYdz[XSrb36gZY5lKGGudHXyd{B1cGViY3XscJVt[XJiYXP0bY4h[3m2b4Pr[YxmfG:w MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5NUC1O{c,OjJyN{WwOVc9N2F-
HUVEC M37ZWWZ2dmO2aX;uJIF{e2G7 MYG1JO69VQ>? M4raVmROW09? M1v1OoJtd2OtczDIWXZGSyC|cILveZRqdmdib36gZ49tdGGpZX6gTUBo\Wy| NGC2ZWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3OVA2Pyd-MkKwO|UxPTd:L3G+
human peripheral blood T cells M{W1UmtqdmG|ZTDhd5NigQ>? M1PMbp4yOCEQvF2= NUHyc3F2TE2VTx?= M3HsVYlvcGmkaYTzJJNqfGVvc4DlZ4lncWNicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=> NVe1TFVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NlgyQDhpPkKzPVI5OTh6PD;hQi=>
human peripheral blood T cells MortSpVv[3Srb36gZZN{[Xl? NVrP[lBkhjFyIN88US=> NFqwUpNFVVOR NWS2NpdFcW2yYXnyd{BVS1JvaX7keYNm\CCWIHPlcIwhdW:{cHjvcI9ocWOjbDDjbIFv\2W|IHHu[EBidHSncoOgZYN1cX[rdImgc4YhWmixQR?= NUDDbZZiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NlgyQDhpPkKzPVI5OTh6PD;hQi=>
human peripheral blood T cells NIfoOlZHfW6ldHnvckBie3OjeR?= MVz+NVAh|ryP NYKweJVrTE2VTx?= NHHTSZNqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhYkGSLUewJIFv\CCOQWS= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl{OEG4PEc,OjN7MkixPFg9N2F-
human peripheral blood T cells NVXINFU{TnWwY4Tpc44h[XO|YYm= NFfEbHd,OTBizszN NXzmOVVYTE2VTx?= MmrLbY1x[Wm{czDBcpRq\2WwLXTldIVv\GWwdDDUJINmdGxiY3;ubpVo[XSrb36= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl{OEG4PEc,OjN7MkixPFg9N2F-
U-2 OS M3PyNZFJXFNiYYPzZZk> MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhXS1{IF;TJINmdGy| MnHqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 NVfGSW5weUiWUzDhd5NigQ>? M4PqUJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| MmrzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MnHadWhVWyCjc4PhfS=> MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 NH\nRZJyUFSVIHHzd4F6 M2e2fJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD NGjCfY5yUFSVIHHzd4F6 NFe4S|RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH MkH5dWhVWyCjc4PhfS=> MmDCdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= NVfVTFZwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) MYrxTHRUKGG|c3H5 MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NYHqVW1IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 Mm\TdWhVWyCjc4PhfS=> Ml3KdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 NVu5[Go1eUiWUzDhd5NigQ>? NF;JcHByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz NHu0U4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 M1uwd5FJXFNiYYPzZZk> M4LKUJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz MlTxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC MYDxTHRUKGG|c3H5 NHfxdmtyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> MnPRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 MmLudWhVWyCjc4PhfS=> M1TMTpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz Mo\MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 Mo\3dWhVWyCjc4PhfS=> M2WzRpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index 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
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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[2]

  • Animal Models: Ctrl-MT and MFCKO-MT mice
  • Dosages: 5 mg/kg
  • Administration: oral administration

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 491.49
Formula

C22H20F3N5O3S

CAS No. 869288-64-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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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.

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