PF-562271

For research use only.

Catalog No.S2890 Synonyms: PF-00562271

93 publications

PF-562271 Chemical Structure

CAS No. 717907-75-0

PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

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Selleck's PF-562271 has been cited by 93 publications

Purity & Quality Control

Choose Selective FAK Inhibitors

Biological Activity

Description PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
Targets
FAK [1]
(Cell-free assay)
PYK2 [1]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
CDK3/CyclinE [1]
(Cell-free assay)
CDK1/CyclinB [1]
(Cell-free assay)
1.5 nM 13 nM 30 nM 47 nM 58 nM
In vitro

PF-562271 binds in the ATP-binding cleft of FAK, forming two of the three “canonical” H-bonds between the inhibitor and main-chain atoms in the kinase hinge region. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. PF-562271 (3.3 μM) results in G1 arrest of PC3-M cells. [1] PF-562271 (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. PF-262271 potently blocks blood vessel sprouting without detectable changes in vascular leakage. [2] PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
IST-MES1 M2Tmfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfkTWM2OD12OT64PVQ1KM7:TR?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
EKVX Ml\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXSTWM2OD12OT62O|MyKM7:TR?= NIP5eZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
NCI-H1395 MoPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7J[ZVKSzVyPUS5MlA1QTJizszN MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
LS-1034 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIr0dlZKSzVyPUS4Mlg6PTRizszN MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
RT4 M{njfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVW0S5JCUUN3ME20PE45Ozd5IN88US=> NVfu[nM2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
PSN1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rhfGlEPTB;NEiuNVQxOSEQvF2= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
KY821 M1rDNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\pUpFxUUN3ME20O{43PDN2IN88US=> MnnpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
LC-1F NUnmeVdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfQTWM2OD12Nz62NVA2KM7:TR?= NXuzZ5FURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
Saos-2 NHHCR3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LCbmlEPTB;NEeuN|EzOyEQvF2= MlXHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
BL-70 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f3TGlEPTB;NE[uO|c{PyEQvF2= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
HCC1569 NFXUXpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIf4SnRKSzVyPUS2MlU6OTdizszN Ml;6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
CP66-MEL M2f2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTR4LkK3PFkh|ryP NEL3dpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
NCI-H187 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHu[4FvUUN3ME20Ok4yQDZ7IN88US=> MmPzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NCI-H1703 Mlq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELsbIVKSzVyPUS2MlA2QTJizszN Mkm3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NCI-H2342 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV6xZ|AxUUN3ME20OU4yOTF5IN88US=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
EoL-1-cell MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvOTWM2OD12ND65NVM3KM7:TR?= NYHnRmI{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
MRK-nu-1 MnvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTR2Lke0NVQh|ryP NHXEVYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
SAS NF2zNIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\QTWM2OD12Mz60Nlg5KM7:TR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
LB996-RCC NHXxVZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzyVYFKSzVyPUSyMlgxODhizszN NX;tR|FERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
OAW-42 MlLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jjTWlEPTB;NEKuNlk1OiEQvF2= NFL1cow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
PF-382 M1vK[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjGXXBKSzVyPUSwMlc1QDdizszN MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
COLO-678 NUTFb5dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\4WVZKSzVyPUSwMlU6PSEQvF2= MmTIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NCI-H2170 M2q0UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTN7Lkm5O|ch|ryP NYj1U4JGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
KU-19-19 M4fNcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHxT2lsUUN3ME2zPU43Ojh{IN88US=> M2nTWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
SW756 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXE[ZpKSzVyPUO5MlUxQTFizszN MorUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
Capan-2 M{GxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrUVlNMUUN3ME2zPU4xPTB7IN88US=> NXX6PW04RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
MDA-MB-453 NGn6cZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTN7LkCyNVgh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
TGBC24TKB NXfxe2NlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHCTWM2OD1|OD6wNlM6KM7:TR?= M3TjbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
A375 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jGN2lEPTB;M{euO|Y1PyEQvF2= M{X4UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
RCM-1 MmjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\KTWM2OD1|Nz61N|U5KM7:TR?= MlfZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
KARPAS-422 NX62fIt7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHRWXhKSzVyPUO3MlQ1OzFizszN Mk\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
LNCaP-Clone-FGC MmfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4m3WWlEPTB;M{euNVkxOyEQvF2= M2fBbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
HCC1937 MnLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2m4ZmlEPTB;M{euNFE2PCEQvF2= NYPMWlI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
no-11 M1\5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL6TWM2OD1|Nj64OVM3KM7:TR?= MnXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
KYSE-140 NXLz[XJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIH4cnpKSzVyPUO2MlczQThizszN NEjFUXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
SW1463 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13hXWlEPTB;M{[uOlU3PiEQvF2= NXPM[ZNQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
NEC8 NEnNbmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\WfmlEPTB;M{[uOFkzPCEQvF2= MlG2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
BV-173 M4HOW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTsSYNKSzVyPUO1MlgzPjRizszN MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H1355 NVyw[W5ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnuRW5EUUN3ME2zOU44PzF6IN88US=> M{X6PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
EFE-184 M4TEdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTN3Lk[4Nlkh|ryP MkTjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
HH MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3DTWM2OD1|NT60NVQyKM7:TR?= M1jSWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
HC-1 NY\DeGZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17QV2lEPTB;M{WuOFAzPCEQvF2= NYjwTlh7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
HCC2218 M3Pjbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPBTWM2OD1|NT6yNVg2KM7:TR?= NHPTflY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
NCI-H1417 NV3zSItET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlX1TWM2OD1|Mz65OVg2KM7:TR?= NIjzVWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
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wild type fibroblast cells MXjxTHRUKGG|c3H5 NULG[2U{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IHPvcpRzd2xiSHige4lt\CC2eYDlJIZq[nKxYnzhd5Qh[2WubIO= NHrYXIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 NGn4fGNyUFSVIHHzd4F6 MoXadWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? NYHZVo1[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 NX\yOo5GeUiWUzDhd5NigQ>? NHTzbo5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBCPjd|IHPlcIx{MQ>? NVXI[|hERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 M2focZFJXFNiYYPzZZk> NFK5ZYlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBDXC1zMjDj[Yxtew>? M2TIclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 NVu5[VVjeUiWUzDhd5NigQ>? NH6wbmlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBNSU5vNTDj[Yxtew>? NVzkfWhRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
DAOY NG\KNnFyUFSVIHHzd4F6 M1SxWJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGRCV1liY3XscJM> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 NEi0ZlhyUFSVIHHzd4F6 NGT4VIlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBDXC1|NzDj[Yxtew>? M{PsV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS MlLFdWhVWyCjc4PhfS=> NETvNFZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBWNTJiT2OgZ4VtdHN? NInYZ3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 M1TtN5FJXFNiYYPzZZk> MWXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz NXr3VoFZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 MV\xTHRUKGG|c3H5 M3XLXZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNid3NvMjDj[Yxtew>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 NFPVV|dyUFSVIHHzd4F6 NE\tZmpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBQUFNvNUCgZ4VtdHN? NV3xWHlwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH MXjxTHRUKGG|c3H5 MXfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNVOKIHPlcIx{ NWLHTpBqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-FAK / FAK / p-Talin / Talin ; 

PubMed: 26530902     


Dose response of PF-562271 on the phosphorylation of FAK-Y397 or Talin-S425 in PC3-mm2 cells.

p-Src / Src / p-paxillin / Paxillin / ICAM-1 ; 

PubMed: 29417941     


MDA-MB-231 cells transfected with FAK-specific siRNAs or treated for 12 h with PF-562271 at the indicated concentrations were subjected to immunoblotting with indicated antibodies.

26530902 29417941
Immunofluorescence
p-FAK; 

PubMed: 26530902     


Immunostaining of PC3-mm2 cells showed that phosphorylated FAK is localized at focal adhesions (inset).

26530902
Growth inhibition assay
Cell viability; 

PubMed: 28953264     


MTT assay showed inhibition of cell proliferation and viability in HCT116 (B) and SW480 (D) cell lines treated with resveratrol and/or different concentrations of FAK-Inhibitor (PF-562271: 0.01, 0.1, 1, and 10 µM) cultured in monolayer for 12 h. Data shown are representative of three independent sets of experiments. Values were compared with the control and statistically significant values with p < 0.05 are designated by an asterisk (*) and p < 0.01 are designated by two asterisks (**).

28953264
In vivo PF-562271 (< 33 mg/kg p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in U87MG-bearing mice. PF-562271 (50 mg/kg p.o. bid) results in 86% tumor growth inhibition in BxPc3 xenografts mice and 45% tumor growth inhibition in PC3-M xenografts mice. PF-562271 (25 mg/kg, bid) results in 2-fold greater apoptosis in treated tumors in mice bearing H125 lung xenografts. [1] PF-562271 (33 mg/kg, p.o.) inhibits extensive movement of the tumor cells over 24 hours in mice. PF-562271 (33 mg/kg, p.o.) results in altered E-cadherin dynamics in mice, which correlates with reduced E-cadherin–dependent collective cell movement. [3] PF-562271 (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. [4] PF-562,271 (5 mg/kg, oral) results in significant and similar increases in osteocalcin and cancellous bone parameters and a decrease in tumor growth and signs of bone healing in rats implanted with MDA-MB-231 cells in the tibia. [5]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: Athymic female mice bearing BxPc3 or PC3-M xenografts.
  • Dosages: 50 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (197.04 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+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.
5 mg/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 507.49
Formula

C21H20F3N7O3S

CAS No. 717907-75-0
Storage powder
in solvent
Synonyms PF-00562271
Smiles CN(C1=C(C=CC=N1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)C4)S(=O)(=O)C

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 )

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    C2
    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):
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    C4=C3/X C4: LOG(C4):
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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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FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID