PF-562271

For research use only.

Catalog No.S2890 Synonyms: PF-00562271

97 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 97 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 M4\uS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDxTWM2OD12OT64PVQ1KM7:TR?= NYnQPZY4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
EKVX MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrFTWM2OD12OT62O|MyKM7:TR?= NWnGfGR6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
NCI-H1395 NH3hSGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTR7LkC0PVIh|ryP M1HR[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
LS-1034 MnjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{j2dGlEPTB;NEiuPFk2PCEQvF2= NV:5dJlJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
RT4 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDoc2xKSzVyPUS4Mlg{PzdizszN MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
PSN1 NF3hOGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXqwRoFiUUN3ME20PE4yPDBzIN88US=> NHWwSnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
KY821 MoTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrqTWM2OD12Nz62OFM1KM7:TR?= M3zUTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
LC-1F M{LI[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{ixdGlEPTB;NEeuOlExPSEQvF2= NUi2ZYdMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
Saos-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLyXYlOUUN3ME20O{4{OTJ|IN88US=> M3y2dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
BL-70 M{TxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LYdmlEPTB;NE[uO|c{PyEQvF2= M2fsd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
HCC1569 NF;LfplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTR4LkW5NVch|ryP M17rblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
CP66-MEL MkfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTR4LkK3PFkh|ryP M{XqS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
NCI-H187 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vtOGlEPTB;NE[uNVg3QSEQvF2= MkfyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NCI-H1703 M2PBVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTufmhKSzVyPUS2MlA2QTJizszN MmjzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NCI-H2342 NXG1[4FUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHlcWZKSzVyPUS1MlEyOTdizszN NEfpOGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
EoL-1-cell MnTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTR2LkmxN|Yh|ryP NEe3eZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
MRK-nu-1 M1\GRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3X5XGlEPTB;NESuO|QyPCEQvF2= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
SAS NWnnVVVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTR|LkSyPFgh|ryP MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
LB996-RCC M{nBTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DROmlEPTB;NEKuPFAxQCEQvF2= MonCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
OAW-42 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGSwOZZKSzVyPUSyMlI6PDJizszN MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
PF-382 M{HnbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jVfmlEPTB;NECuO|Q5PyEQvF2= Mn;1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
COLO-678 MmTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TsUmlEPTB;NECuOVk2KM7:TR?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H2170 M2[2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[yWWlEPTB;M{muPVk4PyEQvF2= M2PiR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
KU-19-19 NWm5WIs{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTN7Lk[yPFIh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
SW756 NIP5[3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P3b2lEPTB;M{muOVA6OSEQvF2= NWfJdXYyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
Capan-2 NFfvZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTN7LkC1NFkh|ryP NFXkVoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
MDA-MB-453 M2jUS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTN7LkCyNVgh|ryP NEXCPVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
TGBC24TKB MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TBdWlEPTB;M{iuNFI{QSEQvF2= M3LrUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
A375 MoDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTN5Lke2OFch|ryP Mn\rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
RCM-1 MmnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jXemlEPTB;M{euOVM2QCEQvF2= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
KARPAS-422 MlGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:5SYdKSzVyPUO3MlQ1OzFizszN NXXsV2prRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
LNCaP-Clone-FGC NGPwWm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDFTWM2OD1|Nz6xPVA{KM7:TR?= NVHxZ|FZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
HCC1937 M1fFcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DpZmlEPTB;M{euNFE2PCEQvF2= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
no-11 MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEf6eFBKSzVyPUO2Mlg2OzZizszN MmDBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
KYSE-140 NGTJ[2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTN4LkeyPVgh|ryP Ml7qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
SW1463 MnTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL6TWM2OD1|Nj62OVY3KM7:TR?= M4HubVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
NEC8 Mo\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkC0TWM2OD1|Nj60PVI1KM7:TR?= M2KwOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
BV-173 M37lNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTN3LkiyOlQh|ryP MnnnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NCI-H1355 NW[yU2JKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;mTWM2OD1|NT63O|E5KM7:TR?= MmfvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
EFE-184 NWLSVpgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTN3Lk[4Nlkh|ryP M3j3d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
HH NGnI[2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVGyb2YyUUN3ME2zOU41OTRzIN88US=> NVW0TlAxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
HC-1 NUDDTYduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml6wTWM2OD1|NT60NFI1KM7:TR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
HCC2218 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4SxO2lEPTB;M{WuNlE5PSEQvF2= M{\aTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
NCI-H1417 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTN|Lkm1PFUh|ryP MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
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NCI-H2405 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;mTWM2OD1zNj6yNlE5KM7:TR?= NXjMToI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
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CAL-12T Mn\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLzTWM2OD1zND60N|M3KM7:TR?= NH7JOWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
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VMRC-RCZ NHe5VllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\LeGlEPTB;MUSuNlM3KM7:TR?= MlnjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
CAL-72 NHPRclJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXGTWM2OD1zND6xPVA3KM7:TR?= NH\vTVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
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LB2241-RCC NWnnSJdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LOPWlEPTB;MUOuNVQ3QSEQvF2= Mn:yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
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HCC1806 MkfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn74TWM2OD1zMj62PVUzKM7:TR?= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
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MG 63 (6-TG R) Ml3TdWhVWyCjc4PhfS=> NY[weVZPeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz Mo\uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
wild type fibroblast cells MXzxTHRUKGG|c3H5 NVzObnFWeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IHPvcpRzd2xiSHige4lt\CC2eYDlJIZq[nKxYnzhd5Qh[2WubIO= M{\QU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 MkHOdWhVWyCjc4PhfS=> NFz2dGRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?= NFzsTW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 MWHxTHRUKGG|c3H5 Mn6wdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRVY4OyClZXzsd{k> M4fINlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 MXHxTHRUKGG|c3H5 NXL5fGtteUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? MnqzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 NWLVVoM6eUiWUzDhd5NigQ>? MnzydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUGFPNTViY3XscJM> Mm\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
DAOY NGT3ToZyUFSVIHHzd4F6 MXjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDERW9[KGOnbHzz MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 NYH2NGhLeUiWUzDhd5NigQ>? NW\PN2E5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
U-2 OS MkDodWhVWyCjc4PhfS=> MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDVMVIhV1NiY3XscJM> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh41 NE\2UolyUFSVIHHzd4F6 M3fjepFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpPDFiY3XscJM> NH\VbmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 MX7xTHRUKGG|c3H5 M3vD[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNid3NvMjDj[Yxtew>? NEHKZmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 NVezXGNVeUiWUzDhd5NigQ>? MkO2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgU2hUNTVyIHPlcIx{ MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH MoLodWhVWyCjc4PhfS=> M3fycZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vU1igZ4VtdHN? NH76fo49[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
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
CalculateReset

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
    Concentration
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    Molecular Weight

*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
    V1
    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):
    C3=C2/X C3: LOG(C3):
    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