PF-562271

Catalog No.S2890 Synonyms: PF-00562271

For research use only.

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.

PF-562271 Chemical Structure

CAS No. 717907-75-0

Selleck's PF-562271 has been cited by 101 publications

Purity & Quality Control

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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)
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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 NIH2O5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPBNG94UUN3ME20PU45QTR2IN88US=> NH\vR4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
EKVX M3LsXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTR7Lk[3N|Eh|ryP MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H1395 Mn7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zDXGlEPTB;NEmuNFQ6OiEQvF2= NHjYSZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
LS-1034 MoLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXy3SpppUUN3ME20PE45QTV2IN88US=> M4nwd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
RT4 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTR6LkizO|ch|ryP Ml;QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
PSN1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrWTWg1UUN3ME20PE4yPDBzIN88US=> M4\JPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
KY821 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rXXmlEPTB;NEeuOlQ{PCEQvF2= MlPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
LC-1F NEDMbY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLFTWM2OD12Nz62NVA2KM7:TR?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
Saos-2 MkXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f4WGlEPTB;NEeuN|EzOyEQvF2= M4LPRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
BL-70 NV7JXFkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HGfmlEPTB;NE[uO|c{PyEQvF2= M{D0blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
HCC1569 NUPuOpBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTR4LkW5NVch|ryP NH;LTG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
CP66-MEL NUTWVJZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzTWYlIUUN3ME20Ok4zPzh7IN88US=> NUjyZpE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
NCI-H187 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\STWM2OD12Nj6xPFY6KM7:TR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H1703 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1yydmlEPTB;NE[uNFU6OiEQvF2= NGrkSXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
NCI-H2342 NIH4eppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXQTWM2OD12NT6xNVE4KM7:TR?= NUL0[|hTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
EoL-1-cell NIf5UIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH2TWM2OD12ND65NVM3KM7:TR?= M3;NVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
MRK-nu-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HDd2lEPTB;NESuO|QyPCEQvF2= NUTrdFk2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
SAS NHTQdHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTR|LkSyPFgh|ryP NV3PcG5KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
LB996-RCC NV[zOHZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPuTWM2OD12Mj64NFA5KM7:TR?= NVHBTIN{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
OAW-42 NG\sbo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfrUo1KSzVyPUSyMlI6PDJizszN MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
PF-382 NYruTpk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\xVmlEPTB;NECuO|Q5PyEQvF2= NEnCOII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
COLO-678 NFfDSVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jPUWlEPTB;NECuOVk2KM7:TR?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H2170 NE\FW3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jER2lEPTB;M{muPVk4PyEQvF2= NF;VNmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
KU-19-19 NWj5NZN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\4VGpKSzVyPUO5MlYzQDJizszN MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
SW756 M4nPWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[xTG41UUN3ME2zPU42ODlzIN88US=> MnrqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
Capan-2 NGDP[ohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnTeW9KSzVyPUO5MlA2ODlizszN MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
MDA-MB-453 MlLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fjVmlEPTB;M{muNFIyQCEQvF2= NGLUWlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
TGBC24TKB M2PPfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTN6LkCyN|kh|ryP MlfYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
A375 NF\oPIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DabGlEPTB;M{euO|Y1PyEQvF2= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
RCM-1 NVO2SVRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnDeoRKSzVyPUO3MlU{PThizszN M4LQVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
KARPAS-422 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnCTWM2OD1|Nz60OFMyKM7:TR?= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
LNCaP-Clone-FGC NU\GdWViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVewUZQ1UUN3ME2zO{4yQTB|IN88US=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
HCC1937 Mlv3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2i3fGlEPTB;M{euNFE2PCEQvF2= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
no-11 M3HXW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjUV2VKSzVyPUO2Mlg2OzZizszN NHvWSZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
KYSE-140 M1XabGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTN4LkeyPVgh|ryP M3uxcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
SW1463 Mnz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPycVJKSzVyPUO2MlY2PjZizszN MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NEC8 MkDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{W0TWlEPTB;M{[uOFkzPCEQvF2= NVSySFRLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
BV-173 NX;BXHJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTN3LkiyOlQh|ryP MmfBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NCI-H1355 NHXPOG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{WxVWlEPTB;M{WuO|cyQCEQvF2= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
EFE-184 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P1cWlEPTB;M{WuOlgzQSEQvF2= NH;xVY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
HH NECxPHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17UZmlEPTB;M{WuOFE1OSEQvF2= NH;rOYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
HC-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTN3LkSwNlQh|ryP MoPTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
HCC2218 Ml;hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTN3LkKxPFUh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H1417 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTN|Lkm1PFUh|ryP NVzIfXZmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
IA-LM M1PFVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTN|Lk[3OFYh|ryP MmHhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NCI-H522 NUfrXmc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTN|Lk[1OEDPxE1? NEjtfm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
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wild type fibroblast cells M3nQfJFJXFNiYYPzZZk> MU\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5Ih[2:wdILvcEBJcCC5aXzkJJR6eGViZnnido9jdGG|dDDj[Yxtew>? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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DAOY MYLxTHRUKGG|c3H5 M2\XU5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGRCV1liY3XscJM> M{DKcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 NI\MTlFyUFSVIHHzd4F6 NWDhd3pJeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? M2fxSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS NVLacoNbeUiWUzDhd5NigQ>? M172UZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHUuOiCRUzDj[Yxtew>? Mm\FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 NFnXWG1yUFSVIHHzd4F6 MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz M1Ple|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 MWDxTHRUKGG|c3H5 M3vvb5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNid3NvMjDj[Yxtew>? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 M1X2UZFJXFNiYYPzZZk> MnLsdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgU2hUNTVyIHPlcIx{ MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH NILEWodyUFSVIHHzd4F6 NH3JdIZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLWPIJINmdGy| M2LkTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Assay
Methods Test Index PMID
Western blot p-FAK / FAK / p-Talin / Talin ; p-Src / Src / p-paxillin / Paxillin / ICAM-1 26530902 29417941
Immunofluorescence p-FAK 26530902
Growth inhibition assay Cell viability 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 (from reference)

Animal Research:[1]
  • 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 3 years -20°C powder
2 years -80°C in solvent
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)

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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