PF-562271

For research use only. Not for use in humans.

Catalog No.S2890

67 publications

PF-562271 Chemical Structure

Molecular Weight(MW): 507.49

PF-562271 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 67 publications

Purity & Quality Control

Choose Selective FAK Inhibitors

Biological Activity

Description PF-562271 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
MV-4-11 NEDiS45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mki3TWM2OD1yLkK3OlYh|ryP MVHTRW5ITVJ?
SW982 M2fXXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\zcmlEPTB;MD6zNlgzKM7:TR?= NETWTGxUSU6JRWK=
KM12 NEG3NINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7VSnBKSzVyPUCuN|g2PTdizszN MXLTRW5ITVJ?
COLO-205 M17nXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmK2TWM2OD1yLkS4OlU5KM7:TR?= NYnYOmZGW0GQR1XS
COLO-829 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\HTWM2OD1yLke1NVc3KM7:TR?= NWrTV4ttW0GQR1XS
MG-63 NVXS[Is4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnX2TWM2OD1yLkiwOlM4KM7:TR?= NVnhNnVkW0GQR1XS
IGROV-1 M{HuPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTBwOEGwN|gh|ryP MojaV2FPT0WU
NCI-H650 NHm4TGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTBwOEOxOVQh|ryP Mm\3V2FPT0WU
RT-112 NYfHVYUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fUfWlEPTB;MD65PFQ3KM7:TR?= Mn7RV2FPT0WU
BCPAP NUnSbYx2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEf0eJpKSzVyPUGuNFEzQDhizszN MUDTRW5ITVJ?
ALL-PO MoT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDlTWM2OD1zLkCxOVg1KM7:TR?= Mn\yV2FPT0WU
KYSE-270 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1L5W2lEPTB;MT6wOFcyPCEQvF2= MXfTRW5ITVJ?
8305C NFvO[VBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjvTWM2OD1zLkC5PVA1KM7:TR?= NGHrW4NUSU6JRWK=
NCI-H810 NXzGTJRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfHcmtKSzVyPUGuNVA4PzZizszN Mn7wV2FPT0WU
CAL-33 M2nGV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTFwMUK5N|gh|ryP M2rUPHNCVkeHUh?=
AN3-CA MnrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M176SWlEPTB;MT6yNVg3PyEQvF2= NXPwZ|BzW0GQR1XS
NKM-1 NXuxVGk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4H2VGlEPTB;MT6yO|UxPiEQvF2= M2nIb3NCVkeHUh?=
BPH-1 M3jUWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlmwTWM2OD1zLkK4O|Y3KM7:TR?= NVP2RZR2W0GQR1XS
MES-SA MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVT0S5E2UUN3ME2xMlMxPjh{IN88US=> Ml;TV2FPT0WU
CAL-62 NXSxOmxlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUf3XoZzUUN3ME2xMlMyQTB7IN88US=> NVnacWtIW0GQR1XS
Detroit562 NHvlelNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXGTWM2OD1zLkO1NlIzKM7:TR?= MYrTRW5ITVJ?
KYSE-150 NWH6b5JzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTFwM{WyN|Yh|ryP MWTTRW5ITVJ?
SK-UT-1 M1Hyfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFwNES2OFch|ryP Ml7nV2FPT0WU
HUTU-80 M4Lofmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTpc|NMUUN3ME2xMlQ1QDh4IN88US=> NGTk[VFUSU6JRWK=
SIG-M5 NVjySndXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zBb2lEPTB;MT60PFM5PyEQvF2= NXPoeWd[W0GQR1XS
AGS NGjPO29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHK1WZJKSzVyPUGuOVIyOjRizszN MmLsV2FPT0WU
ST486 Mo\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XnNWlEPTB;MT61N|I4QCEQvF2= M3i1cnNCVkeHUh?=
HSC-2 MonDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL6PXBkUUN3ME2xMlU{QTVizszN NXPyOpd4W0GQR1XS
LCLC-103H M1i5SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkS0TWM2OD1zLkW1PFE5KM7:TR?= M1XBT3NCVkeHUh?=
BC-1 NHTYO|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTFwNkG2OlQh|ryP NH:5eo5USU6JRWK=
CGTH-W-1 Mo[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHITWM2OD1zLk[xOlc6KM7:TR?= M33wN3NCVkeHUh?=
MZ1-PC NVr6XHFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fWTmlEPTB;MT62NlMyOiEQvF2= MmTSV2FPT0WU
SW1710 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF31VpBKSzVyPUGuOlI3OjhizszN MUHTRW5ITVJ?
EW-13 Ml\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYKxSFZ1UUN3ME2xMlY{PDZ4IN88US=> MmDoV2FPT0WU
TE-11 M3LmVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFwNkO1NlIh|ryP MYTTRW5ITVJ?
BHY Ml3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXrcIlKSzVyPUGuOlU3PjNizszN NEDDPFZUSU6JRWK=
ML-2 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInmR|FKSzVyPUGuOlY5ODJizszN Mlm4V2FPT0WU
MEL-JUSO NHmxRoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPvNlYzUUN3ME2xMlczQDlzIN88US=> NXLRXGxkW0GQR1XS
U251 MmPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnDV2dKSzVyPUGuO|QxOzFizszN NGjueXNUSU6JRWK=
MHH-ES-1 NXjhb|NiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTFwN{m1Olgh|ryP NXP2TGJ3W0GQR1XS
CAL-85-1 NGPqeWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPIT4l1UUN3ME2xMlgxPDlizszN MV;TRW5ITVJ?
D-336MG MoX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXUTWM2OD1zLki1OlE1KM7:TR?= NXrpeINEW0GQR1XS
VA-ES-BJ MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfpNItHUUN3ME2xMlkxOzF3IN88US=> MoP3V2FPT0WU
MDA-MB-468 M33wO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jUNWlEPTB;MT65NVI4OiEQvF2= Mkj6V2FPT0WU
MEL-HO NYi4fIpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1uzV2lEPTB;MT65O|k6OyEQvF2= MVLTRW5ITVJ?
SW954 MmHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfQOW9KSzVyPUKuNFAyPTFizszN MXfTRW5ITVJ?
LB831-BLC M2X4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLKTFlrUUN3ME2yMlAxQTh6IN88US=> NHfxWmZUSU6JRWK=
EW-16 NVzpe5lDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TGW2lEPTB;Mj6wN|k5OyEQvF2= NF7wTnpUSU6JRWK=
NCI-H460 NYrvfZljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzQdHdKSzVyPUKuNFQ5OzlizszN MU\TRW5ITVJ?
CHP-212 NGTUd5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPoVGhKSzVyPUKuNFk2OzlizszN MVHTRW5ITVJ?
MHH-NB-11 NV7CTG83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLVW2tRUUN3ME2yMlEzQDF6IN88US=> NV25OHZ4W0GQR1XS
DU-4475 MnmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3RTWM2OD1{LkG0O|U6KM7:TR?= MUPTRW5ITVJ?
ABC-1 M3LUXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zacGlEPTB;Mj6yOVE6PiEQvF2= MWfTRW5ITVJ?
LOUCY MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;oVIVKSzVyPUKuNlYyOjhizszN NICyTXpUSU6JRWK=
LC-2-ad Mm\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjsTWM2OD1{LkK2PVY3KM7:TR?= M1\GXHNCVkeHUh?=
ETK-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTJwMki0OkDPxE1? NGruUpZUSU6JRWK=
KYSE-180 NGX0UW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;NVVBLUUN3ME2yMlI5QDd2IN88US=> M2TTWnNCVkeHUh?=
HOP-92 NWKyT282T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJwM{C2O|Mh|ryP Mn\OV2FPT0WU
RCC10RGB MlW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jvNGlEPTB;Mj6zNlUxPyEQvF2= NUn0PWtuW0GQR1XS
KASUMI-1 M2\0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3vN2d6UUN3ME2yMlMzQDhizszN MWLTRW5ITVJ?
ACN NWTJd5oyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Hke2lEPTB;Mj6zOFc1PSEQvF2= MW\TRW5ITVJ?
BxPC-3 M{[xemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYS2d4RbUUN3ME2yMlM2PDN4IN88US=> MULTRW5ITVJ?
MONO-MAC-6 MlXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vIT2lEPTB;Mj60NVI1QCEQvF2= M{\4RnNCVkeHUh?=
CAL-39 NXH1U3E{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{D4VmlEPTB;Mj60NVYzQCEQvF2= NF62NlBUSU6JRWK=
CMK NFHYNmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LaXWlEPTB;Mj60NVc6PSEQvF2= MoraV2FPT0WU
MFE-296 NU[zOZY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LuXGlEPTB;Mj60O|c6OiEQvF2= NE\zbYNUSU6JRWK=
DU-145 NYXXTHE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjiOZBKSzVyPUKuOFkyOThizszN MXvTRW5ITVJ?
MDA-MB-231 MnzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrXe4pZUUN3ME2yMlQ6PTd{IN88US=> MV3TRW5ITVJ?
EFO-27 NXfDc3d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\PTWM2OD1{LkWxPFg5KM7:TR?= NH[0TFBUSU6JRWK=
SNU-387 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfoWZhkUUN3ME2yMlUzQDJizszN MmfNV2FPT0WU
KYSE-410 NH\KXXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jFNWlEPTB;Mj61OlUyPyEQvF2= NH3VdZdUSU6JRWK=
NCCIT M3LkTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nQSGlEPTB;Mj61O|I1KM7:TR?= MnjxV2FPT0WU
LXF-289 M4LQc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTETWM2OD1{LkW4Nlc{KM7:TR?= MW\TRW5ITVJ?
HMV-II M1TqVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTCWWxKSzVyPUKuOVg6QTdizszN MlzlV2FPT0WU
MOLT-4 M2DBemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjPd2lKUUN3ME2yMlYxPzF{IN88US=> Ml3DV2FPT0WU
KOSC-2 NVfkPXg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPnXoZKSzVyPUKuOlM5PzlizszN MUTTRW5ITVJ?
TUR MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfrTWM2OD1{Lk[1N|Y6KM7:TR?= MmHoV2FPT0WU
NCI-H2087 NFznd5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTRV3B3UUN3ME2yMlcyPjR4IN88US=> NYLvTVVQW0GQR1XS
SCC-15 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3LUnJKSzVyPUKuO|UzPTJizszN MVrTRW5ITVJ?
HSC-4 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjDPHBxUUN3ME2yMlc5Ozh7IN88US=> Mn[3V2FPT0WU
G-402 MkewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojETWM2OD1{LkixOFQ4KM7:TR?= Mn7yV2FPT0WU
GP5d M1jRSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnufW5NUUN3ME2yMlg{QDJ5IN88US=> NYHz[5hzW0GQR1XS
IGR-1 NEDCfpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\hfFI4UUN3ME2yMlg{QTh5IN88US=> MYfTRW5ITVJ?
SK-PN-DW M4rxR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPMTWM2OD1{Lki2NlA1KM7:TR?= NIfyZZlUSU6JRWK=
OPM-2 MkfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmO0TWM2OD1{Lki5PVc5KM7:TR?= M4rTWXNCVkeHUh?=
5637 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHrTHFKSzVyPUKuPVI1OzlizszN NX7VXlJ6W0GQR1XS
NCI-H2030 NHjwS2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkSzTWM2OD1{Lkm4NFI6KM7:TR?= NWToWVBVW0GQR1XS
SK-LU-1 Mk\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjRfWt1UUN3ME2yMlk5OzN2IN88US=> MlL4V2FPT0WU
EW-18 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfjVmtvUUN3ME2zMlA2OzJizszN M3y3W3NCVkeHUh?=
786-0 NUfWNYpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDiN5ZXUUN3ME2zMlA2Pzh2IN88US=> MnHuV2FPT0WU
NCI-H1963 NFzYUVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTNwMEi4NlUh|ryP MXHTRW5ITVJ?
A2780 NX71RZdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DJOGlEPTB;Mz6xNFM1OSEQvF2= NYDodZZLW0GQR1XS
NCI-H526 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\CcnlKSzVyPUOuNVM6PjFizszN NHn5fHFUSU6JRWK=
BHT-101 NIfRZZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTvVpRRUUN3ME2zMlE2Pzl6IN88US=> MYnTRW5ITVJ?
RPMI-7951 NXHPbFRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXGTWM2OD1|LkKwNVM4KM7:TR?= NUTMRplFW0GQR1XS
HL-60 Mk[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTNwMkGxOEDPxE1? M3L1OnNCVkeHUh?=
CTV-1 MmDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv4TWM2OD1|LkK1N|c4KM7:TR?= NWP0cWZNW0GQR1XS
IST-SL1 NIXzT5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHiTWM2OD1|LkK5OFY2KM7:TR?= NX7Db5dIW0GQR1XS
G-401 NVOzSIdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHziOodKSzVyPUOuNlk5ODhizszN NVrVcYN7W0GQR1XS
OVCAR-5 M1zMSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK4TWM2OD1|LkO2N|UzKM7:TR?= Mk\YV2FPT0WU
EW-1 Mli3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPhTWM2OD1|LkSwOVQ1KM7:TR?= MnnwV2FPT0WU
H4 NXLRcHNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTNwNEe1Olkh|ryP MVTTRW5ITVJ?
EM-2 NIrLUVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzrNY9KSzVyPUOuOFg3PzRizszN NILZXYpUSU6JRWK=
RS4-11 NIj6[plIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXhZpl3UUN3ME2zMlQ5PzF3IN88US=> NHPDS2VUSU6JRWK=
NOMO-1 NFHESWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zQNmlEPTB;Mz60PVIxPCEQvF2= NVr5WJlNW0GQR1XS
HCT-116 NFvV[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7MTWM2OD1|LkWwO|EyKM7:TR?= Mk\kV2FPT0WU
CAL-120 NUPz[YpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo[5TWM2OD1|LkW3N|Uh|ryP NWPLbow5W0GQR1XS
CAL-51 M2j4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXyxTnB3UUN3ME2zMlU4PjF{IN88US=> NXTPfZQ4W0GQR1XS
RVH-421 MkDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTNwNkCzNVEh|ryP M3n5W3NCVkeHUh?=
NCI-H2081 MoPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTNwNkWyPFgh|ryP NFn0dXJUSU6JRWK=
SBC-5 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrRWZNCUUN3ME2zMlY4QDh{IN88US=> NH\6TYFUSU6JRWK=
RL95-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXmUIZmUUN3ME2zMlcyQDZ2IN88US=> MkDvV2FPT0WU
SW872 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nuc2lEPTB;Mz63Olk2QCEQvF2= M{L5SHNCVkeHUh?=
VM-CUB-1 NX;QTYp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LaNWlEPTB;Mz63O|UyKM7:TR?= M4LmOXNCVkeHUh?=
SUP-T1 NUKxb4g3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTNwN{izNkDPxE1? NHS4WG5USU6JRWK=
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NCI-H2342 MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTR3LkGxNVch|ryP Ml7oV2FPT0WU
NCI-H1703 NETod|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTR4LkC1PVIh|ryP NGK4TGxUSU6JRWK=
NCI-H187 NWOwRoVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjJTWM2OD12Nj6xPFY6KM7:TR?= MY\TRW5ITVJ?
CP66-MEL MnPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFq2WJhKSzVyPUS2MlI4QDlizszN NHLHUFBUSU6JRWK=
HCC1569 M4DWdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Prb2lEPTB;NE[uOVkyPyEQvF2= M4HzOHNCVkeHUh?=
BL-70 NFjzPYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfRRmR2UUN3ME20Ok44PzN5IN88US=> M3vtUHNCVkeHUh?=
Saos-2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\qTmZKSzVyPUS3MlMyOjNizszN MkLsV2FPT0WU
LC-1F M{nCZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDDcYlKSzVyPUS3MlYyODVizszN NX32e5pVW0GQR1XS
KY821 M2rV[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG5TWlKSzVyPUS3MlY1OzRizszN NUfFcWhNW0GQR1XS
PSN1 NIjiPYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED0OXZKSzVyPUS4MlE1ODFizszN NXHFZXZUW0GQR1XS
RT4 M3PQUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTETWM2OD12OD64N|c4KM7:TR?= NV20XoE{W0GQR1XS
LS-1034 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rN[GlEPTB;NEiuPFk2PCEQvF2= MljSV2FPT0WU
NCI-H1395 NVP5bHpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTpTWM2OD12OT6wOFkzKM7:TR?= NFfoWYlUSU6JRWK=
EKVX NIXy[|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7WTWM2OD12OT62O|MyKM7:TR?= NVfySJJnW0GQR1XS
IST-MES1 MlW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TJPWlEPTB;NEmuPFk1PCEQvF2= MmTuV2FPT0WU

... 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.
  • Formulation: 5% Gelucire
  • 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 N/A
Smiles CN(C1=C(CNC2=C(C=NC(=N2)NC3=CC=C4NC(=O)CC4=C3)C(F)(F)F)C=CC=N1)[S](C)(=O)=O

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
    Volume
    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):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
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