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 69 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 MlfwT4lv[XOnIHHzd4F6 MmW3glExKM7:TR?= MWjEUXNQ M4fZV4lvcGmkaYTzJGZCUyCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEGxJI5O M1\sVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
REF52 M4[yU2tqdmG|ZTDhd5NigQ>? M4XpS54yOCEQvF2= M3HSeWROW09? MnrVbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kB,OTByIH7N MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7NUW5OEc,OTd|OUW1PVQ9N2F-
PC3 NVfGelBCU2mwYYPlJIF{e2G7 MlPsglExKM7:TR?= NFrnToZFVVOR NVfCd5k1cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iBzMECgcm0> NF\mepg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{O5OVU6PCd-MUezPVU2QTR:L3G+
SKOV-3 M1LkdWtqdmG|ZTDhd5NigQ>? MkXvglExKM7:TR?= M2nnS2ROW09? NIjJXZhqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyIH7N NYXLVnhlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVU2QTRpPkG3N|k2PTl2PD;hQi=>
L3.6p1 MlTVT4lv[XOnIHHzd4F6 NYPJRXVWhjFyIN88US=> MnjGSG1UVw>? MmO2bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA{ODBibl2= M13tRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
F-G MYrLbY5ie2ViYYPzZZk> MV3+NVAh|ryP NGPHeolFVVOR M1z3bolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOzBibl2= MnjiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
MDCK MYPLbY5ie2ViYYPzZZk> M1HIfZ4yOCEQvF2= MkHMSG1UVw>? NHLoR|NqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyMDDuUS=> NFm1SFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{O5OVU6PCd-MUezPVU2QTR:L3G+
PC3 MofQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NY\6U|IyOTBizszN NES0RWZFVVOR NIP5V5J{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> NH;BdmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{O5OVU6PCd-MUezPVU2QTR:L3G+
REF52 NF[3SIZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYfxUlRNOTBizszN NEHFTpVFVVOR NYW1UlNUe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> MmHSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
MDCK M{\lR2Fxd3C2b4Ppd{Bie3OjeR?= Mn3PNVAh|ryP NUjrSYxsTE2VTx?= M2PncYlv\HWlZYOgZZBweHSxc3nz MoTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
REF52 MnvKRZBweHSxc3nzJIF{e2G7 NXXPZ4h1OTBizszN NH;CfllFVVOR NIrLOY9qdmS3Y3XzJIFxd3C2b4Ppdy=> MoSxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVQoRjF5M{m1OVk1RC:jPh?=
REF52 MXfGeY5kfGmxbjDhd5NigQ>? NVXWTppSOTBizszN MXHEUXNQ MXTicI9kc3Nic3XyeY0h[W6mIF\OMZN1cW23bHH0[YQhdWmpcnH0bY9v M1O0PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVk1Lz5zN{O5OVU6PDxxYU6=
platelet M37UNWZ2dmO2aX;uJIF{e2G7 MkPyNUDPxE1? NVL0bHZNTE2VTx?= MXTpcohq[mm2czDwcIF1\WyndDDh[4dz\WejdHnvckBidmRic4Dy[YFlcW6p M1XsWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{G2PFA{Lz5zOUexOlgxOzxxYU6=
platelet M4[5dmZ2dmO2aX;uJIF{e2G7 MYCxJO69VQ>? NXq5NlV5TE2VTx?= MY\s[YFleyC2bzDpcohq[mm2aX;uJI9nKFCDSzDhcoQhSUuW MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTdzNkiwN{c,OTl5MU[4NFM9N2F-
platelet MYnGeY5kfGmxbjDhd5NigQ>? NH7IN3YyKM7:TR?= NY\QPWpETE2VTx?= NX7UXXQ1[myxY3vzJINidGOrdX2gcY9jcWyrenH0bY9vKGGwZDDk[Y5{\SCpcnHueYxmKHOnY4LleIlwdg>? NIfiPWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUexOlgxOyd-MUm3NVY5ODN:L3G+
4T1 NUn6OZB2TnWwY4Tpc44h[XO|YYm= MkDpSG1UVw>? Mk\uZYJwdGm|aHXzJJRp\SCrboTldoFkfGmxbjDi[ZR4\WWwIN8yN{BqdnSnZ4LpckBidmRiVN8yVk1KUQ>? NX7QdoJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3OFA1OzNpPkG5O|QxPDN|PD;hQi=>
MCF7 MormT4lv[XOnIHHzd4F6 MYL+NVAh|ryP NVvxSHRVTE2VTx?= MVrpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFQ{OCCwTR?= NX6yVFhMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzOVQ4QDBpPkKwN|U1PzhyPD;hQi=>
TamR NHGwTpJMcW6jc3WgZZN{[Xl? NVHpR4FLhjFyIN88US=> NXXmVHRpTE2VTx?= NUO2ZppLcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB3MDDuUS=> M1zI[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{W0O|gxLz5{MEO1OFc5ODxxYU6=
FasR M3jYO2tqdmG|ZTDhd5NigQ>? Mm\CglExKM7:TR?= NVvOeWhoTE2VTx?= NFrvSYpqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDF|MDDuUS=> NGrUU2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO1OFc5OCd-MkCzOVQ4QDB:L3G+
TamR M{jVSWZ2dmO2aX;uJIF{e2G7 MVOxJO69VQ>? NW\RWIRDTE2VTx?= M3fNXIlvcGmkaYTzJINmdGxibXnndoF1cW:w MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN3NEe4NEc,OjB|NUS3PFA9N2F-
FasR NF;xbWRHfW6ldHnvckBie3OjeR?= MVexJO69VQ>? NGTJT5FFVVOR NULvW|BjcW6qaXLpeJMh[2WubDDtbYdz[XSrb36= NGL6U2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO1OFc5OCd-MkCzOVQ4QDB:L3G+
endothelial cell M37VWWtqdmG|ZTDhd5NigQ>? Mm\YOFAhdk1? M{\WUGROW09? MVPpcohq[mm2czDINm8zNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKE[DSx?= MlW2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{MUK0NFIoRjJzMkGyOFAzRC:jPh?=
endothelial cell MYfGeY5kfGmxbjDhd5NigQ>? NEnSW|g1OCCwTR?= MWXEUXNQ NGHIUJFqdmirYnn0d{BJOk9{LXnu[JVk\WRic4Ty[ZN{KG[rYnXyJIZwem2jdHnvci=> NHr6e5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKxNlQxOid-MkGyNVI1ODJ:L3G+
endothelial cell NHn0TFNCeG:ydH;zbZMh[XO|YYm= M13GclQxKG6P NXqzToZkTE2VTx?= M1PSZYlvcGmkaYTzJIFxd3C2b4Ppdy=> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJzMkSwNkc,OjF{MUK0NFI9N2F-
GH3 M{TIW2Z2dmO2aX;uJIF{e2G7 Mn[zN{DPxE1? MVvEUXNQ NHu4PHNqdmO{ZXHz[ZMhUUtqQ3GpJIFueGyrdIXk[S=> MlfwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7MkW1NVIoRjJzOUK1OVEzRC:jPh?=
GH3 MYLGeY5kfGmxbjDhd5NigQ>? NFfBTG4{KM7:TR?= NXTBTGNvTE2VTx?= NHrSR2RmdmijbnPld{BDU0OjLXPoZY5v\WxiYXP0bZZqfHl? M4Hr[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUK1OVEzLz5{MUmyOVUyOjxxYU6=
HUVEC NGPuN5NkgXSxdH;4bYNqfHliYYPzZZk> MXj+NVAh|ryP NID5bYpFVVOR MXLpcZBicXK|IHXu[I91cGWuaXHsJINmdGxidnnhZoltcXS7 MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5NUC1O{c,OjJyN{WwOVc9N2F-
HUVEC MXvLbY5ie2ViYYPzZZk> NH\ONlA2KM7:TR?= MnjCSG1UVw>? MVXpcohq[mm2czDGRWshc2mwYYPlJIFkfGm4aYT5 M1XXd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe1NFU4Lz5{MkC3OVA2PzxxYU6=
HUVEC Ml;vSpVv[3Srb36gZZN{[Xl? MlnlOUDPxE1? NFTDTI5FVVOR NVGyTpp{cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M3LhSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe1NFU4Lz5{MkC3OVA2PzxxYU6=
HUVEC NV\Tc2ZsSXCxcITvd4l{KGG|c3H5 NVnzSlBnPSEQvF2= M2TwSGROW09? M2nKV4lv\HWlZYOgZZBweHSxc3nz NV62SW52RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|UxPTdpPkKyNFc2ODV5PD;hQi=>
HUVEC M2O0RmZ2dmO2aX;uJIF{e2G7 NXrGUnNkPSEQvF2= NVfmZpZiTE2VTx?= NYP0TWZpcW2yZXTld{BmdmSxdHjlcIlidCClZXzsJI1q\3KjdHnvckBidmRiYXz0[ZJ{KHSqZTDj[YxtfWyjcjDhZ5RqdiCleYTvd4tmdGW2b36= MknLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{WwOVcoRjJ{MEe1NFU4RC:jPh?=
HUVEC M3;SNWZ2dmO2aX;uJIF{e2G7 NF7WZ2M2KM7:TR?= Ml7VSG1UVw>? MWXicI9kc3NiSGXWSWMhe3C{b4X0bY5oKG:wIHPvcIxi\2WwIFmg[4Vtew>? NIq2fpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3OVA2Pyd-MkKwO|UxPTd:L3G+
human peripheral blood T cells MkPJT4lv[XOnIHHzd4F6 NIDyUVh,OTBizszN NV;KZVhvTE2VTx?= M3HBUIlvcGmkaYTzJJNqfGVvc4DlZ4lncWNicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=> MkHhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MkixPFgoRjJ|OUK4NVg5RC:jPh?=
human peripheral blood T cells NIi4WYlHfW6ldHnvckBie3OjeR?= NF;sc2V,OTBizszN NFi3SpRFVVOR M2HPPIlueGGrcoOgWGNTNWmwZIXj[YQhXCClZXzsJI1wenCqb3zv[4lk[WxiY3jhcodmeyCjbnSgZYx1\XK|IHHjeIl3cXS7IH;mJHJpd0F? NWnvN|Y5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NlgyQDhpPkKzPVI5OTh6PD;hQi=>
human peripheral blood T cells NFX0OHVHfW6ldHnvckBie3OjeR?= M3[0S54yOCEQvF2= NFK0XYxFVVOR MVjpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gXmFRNTdyIHHu[EBNSVR? NYTzUWNERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NlgyQDhpPkKzPVI5OTh6PD;hQi=>
human peripheral blood T cells NWXZe2dqTnWwY4Tpc44h[XO|YYm= Mn3FglExKM7:TR?= NHPNWIpFVVOR MVvpcZBicXK|IFHueIlo\W5vZHXw[Y5l\W62IGSgZ4VtdCClb37qeYdifGmxbh?= M1nNNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUK4NVg5Lz5{M{myPFE5QDxxYU6=
U-2 OS MmrtdWhVWyCjc4PhfS=> NYfWOnpbeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGWtNkBQWyClZXzsdy=> MkTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 NYW5bI4yeUiWUzDhd5NigQ>? M2rRdJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| NFPPPVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 NVf0TZhleUiWUzDhd5NigQ>? M1[wOJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= NEjyTGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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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

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

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

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