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 105 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)
Click to View More Targets
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 MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXT1WZZyUUN3ME20PU45QTR2IN88US=> NUX3UngxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
EKVX NIrUWG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTR7Lk[3N|Eh|ryP NEfqbnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
NCI-H1395 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\TTWM2OD12OT6wOFkzKM7:TR?= NXnNPIJMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
LS-1034 NWj3fYNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HpUGlEPTB;NEiuPFk2PCEQvF2= NUTy[29DRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
RT4 M2q2eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnmzTWM2OD12OD64N|c4KM7:TR?= NUfZO|JmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
PSN1 NIXtVYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fzZmlEPTB;NEiuNVQxOSEQvF2= NUT2PFl5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
KY821 NF7LRopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTR5Lk[0N|Qh|ryP NH\FUJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
LC-1F NVTHbpBUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3yepBoUUN3ME20O{43OTB3IN88US=> MnnzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
Saos-2 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33SdWlEPTB;NEeuN|EzOyEQvF2= M1y3[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
BL-70 NFmzN4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDKTWM2OD12Nj63O|M4KM7:TR?= NYS2SYhqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
HCC1569 NX74PWxGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTR4LkW5NVch|ryP MlvoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
CP66-MEL NYD0Xml2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTR4LkK3PFkh|ryP MlTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NCI-H187 Mnj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH70elNKSzVyPUS2MlE5PjlizszN MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H1703 NEX4R2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzHZZlxUUN3ME20Ok4xPTl{IN88US=> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H2342 MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4exZWlEPTB;NEWuNVEyPyEQvF2= NFzxTJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
EoL-1-cell MnXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlX4TWM2OD12ND65NVM3KM7:TR?= MkDXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
MRK-nu-1 NGLJWXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DtTWlEPTB;NESuO|QyPCEQvF2= M{T0[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
SAS NF25Z4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTR|LkSyPFgh|ryP NUS0dHZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
LB996-RCC M3PxdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHWTWM2OD12Mj64NFA5KM7:TR?= M{jTdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
OAW-42 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzrbIVKSzVyPUSyMlI6PDJizszN NYTLcIIzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
PF-382 M3;O[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjR[lVKSzVyPUSwMlc1QDdizszN NFXPZnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
COLO-678 NVvWRnFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXGNXF4UUN3ME20NE42QTVizszN NULBenlxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
NCI-H2170 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\YVmlEPTB;M{muPVk4PyEQvF2= M{TvWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
KU-19-19 NXyzVWlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTN7Lk[yPFIh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
SW756 M3PNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFj5VVdKSzVyPUO5MlUxQTFizszN M1;WRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
Capan-2 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTN7LkC1NFkh|ryP M3;3[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
MDA-MB-453 NXTscYFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjLTWM2OD1|OT6wNlE5KM7:TR?= NHTkc3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
TGBC24TKB NXnvSGJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHJOJBKSzVyPUO4MlAzOzlizszN Mm\jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
A375 Mnv1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTPTWM2OD1|Nz63OlQ4KM7:TR?= NUjFfllZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
RCM-1 MmnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnyTWM2OD1|Nz61N|U5KM7:TR?= MkXMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
KARPAS-422 NHm2OHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XlPGlEPTB;M{euOFQ{OSEQvF2= MoOyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
LNCaP-Clone-FGC NXT1VZZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF75UpdKSzVyPUO3MlE6ODNizszN NFrMWG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
HCC1937 M4TYc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTN5LkCxOVQh|ryP NIn4eng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
no-11 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTN4Lki1N|Yh|ryP MnvQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
KYSE-140 M{DROWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PL[2lEPTB;M{[uO|I6QCEQvF2= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
SW1463 NYPaWW4{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4j3ZmlEPTB;M{[uOlU3PiEQvF2= NEHjd4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
NEC8 NYrR[YtoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLPXmVrUUN3ME2zOk41QTJ2IN88US=> NGj3RlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
BV-173 NE\zSHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnsdnZKSzVyPUO1MlgzPjRizszN M1nIO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
NCI-H1355 MnLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTN3Lke3NVgh|ryP NHG2cZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
EFE-184 M2LDS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPKOJpKSzVyPUO1MlY5OjlizszN M3fhOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
HH MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rlO2lEPTB;M{WuOFE1OSEQvF2= NGTUZlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
HC-1 NE[zbW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;P[3VKSzVyPUO1MlQxOjRizszN NF70enM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
HCC2218 Mn;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYO5N2FVUUN3ME2zOU4zOTh3IN88US=> NGPPUVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
NCI-H1417 M4DPNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEK0VnNKSzVyPUOzMlk2QDVizszN NF3BSI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
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wild type fibroblast cells M{HzO5FJXFNiYYPzZZk> NEWxVFByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiY3;ueJJwdCCKaDD3bYxlKHS7cHWg[oljem:kbHHzeEBk\Wyucx?= M3HjWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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DAOY NYLrbnJNeUiWUzDhd5NigQ>? MXPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDERW9[KGOnbHzz MmjjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-37 NGHufJlyUFSVIHHzd4F6 NI\GeXVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBDXC1|NzDj[Yxtew>? NULQPHgzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
U-2 OS Mor3dWhVWyCjc4PhfS=> Mo[5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWU0zKE:VIHPlcIx{ M{WwfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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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

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+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.

5 mg/ml

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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