PF-562271

For research use only.

Catalog No.S2890

83 publications

PF-562271 Chemical Structure

CAS No. 717907-75-0

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 83 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 NWqwSnJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTFeVdkUUN3ME2wMlI4PjZizszN M4LHcXNCVkeHUh?=
SW982 MmP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTnbWUxUUN3ME2wMlMzQDJizszN M2TNT3NCVkeHUh?=
KM12 NF\pZYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DIe2lEPTB;MD6zPFU2PyEQvF2= MmfSV2FPT0WU
COLO-205 MmHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjwV|ZKSzVyPUCuOFg3PThizszN NHLJ[3lUSU6JRWK=
COLO-829 NGmxeFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULZPZd[UUN3ME2wMlc2OTd4IN88US=> NWK0[IFDW0GQR1XS
MG-63 MnzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjrSVFKSzVyPUCuPFA3OzdizszN M4q3fXNCVkeHUh?=
IGROV-1 MkW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfPVnJ4UUN3ME2wMlgyODN6IN88US=> NIfQcHlUSU6JRWK=
NCI-H650 M3\GcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlr2TWM2OD1yLkizNVU1KM7:TR?= M2S1UHNCVkeHUh?=
RT-112 MlLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;yZmVHUUN3ME2wMlk5PDZizszN MV3TRW5ITVJ?
BCPAP NEexS3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojFTWM2OD1zLkCxNlg5KM7:TR?= MXLTRW5ITVJ?
ALL-PO MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXRTmdKSzVyPUGuNFE2QDRizszN MYTTRW5ITVJ?
KYSE-270 NEDJO4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTFwMES3NVQh|ryP MkDQV2FPT0WU
8305C Mo\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPjcmdOUUN3ME2xMlA6QTB2IN88US=> MYXTRW5ITVJ?
NCI-H810 NULG[Y93T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPNTZBvUUN3ME2xMlExPzd4IN88US=> M2O2cXNCVkeHUh?=
CAL-33 MkHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nlb2lEPTB;MT6xNlk{QCEQvF2= NU\LT|VNW0GQR1XS
AN3-CA M2DQNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrMNlc1UUN3ME2xMlIyQDZ5IN88US=> M3PMO3NCVkeHUh?=
NKM-1 NYXpdFVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTFwMke1NFYh|ryP NEP3fGhUSU6JRWK=
BPH-1 NVjMR3N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4izdmlEPTB;MT6yPFc3PiEQvF2= MlP6V2FPT0WU
MES-SA MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTFwM{C2PFIh|ryP NF\PSHVUSU6JRWK=
CAL-62 MoPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\RXJVKSzVyPUGuN|E6ODlizszN NFfxUnJUSU6JRWK=
Detroit562 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XBRWlEPTB;MT6zOVIzOiEQvF2= MlvBV2FPT0WU
KYSE-150 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rXeGlEPTB;MT6zOVI{PiEQvF2= NVXxSWptW0GQR1XS
SK-UT-1 NFm0VZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LFSWlEPTB;MT60OFY1PyEQvF2= M1vHNHNCVkeHUh?=
HUTU-80 NVnFTWF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXBOXczUUN3ME2xMlQ1QDh4IN88US=> M2C2OnNCVkeHUh?=
SIG-M5 NXvzSHR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jYWWlEPTB;MT60PFM5PyEQvF2= MnXYV2FPT0WU
AGS Moe1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HHWGlEPTB;MT61NlEzPCEQvF2= NVfDeHVyW0GQR1XS
ST486 M{TGZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTFwNUOyO|gh|ryP MnzOV2FPT0WU
HSC-2 NFP6WWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVX1RoxFUUN3ME2xMlU{QTVizszN MVvTRW5ITVJ?
LCLC-103H MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LJ[GlEPTB;MT61OVgyQCEQvF2= MlTXV2FPT0WU
BC-1 M1\qRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvzd|lKSzVyPUGuOlE3PjRizszN MVfTRW5ITVJ?
CGTH-W-1 NWnDVVVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTFwNkG2O|kh|ryP MXzTRW5ITVJ?
MZ1-PC NUOyUFhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorHTWM2OD1zLk[yN|EzKM7:TR?= MkHGV2FPT0WU
SW1710 MmL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[xTWM2OD1zLk[yOlI5KM7:TR?= MnTQV2FPT0WU
EW-13 MkPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLITWM2OD1zLk[zOFY3KM7:TR?= NVjzenh{W0GQR1XS
TE-11 NF7NSXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfBN3c4UUN3ME2xMlY{PTJ{IN88US=> M4jaN3NCVkeHUh?=
BHY M2\KWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTrTWM2OD1zLk[1OlY{KM7:TR?= MV;TRW5ITVJ?
ML-2 Mm\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfwTWM2OD1zLk[2PFAzKM7:TR?= NFHmSGpUSU6JRWK=
MEL-JUSO NYf5eIxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFwN{K4PVEh|ryP MlrUV2FPT0WU
U251 M3fobGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjzOHZKSzVyPUGuO|QxOzFizszN NVXyZ5V7W0GQR1XS
MHH-ES-1 NEjweZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NISwfHZKSzVyPUGuO|k2PjhizszN M{ftdHNCVkeHUh?=
CAL-85-1 NVrDbJZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH31eWxKSzVyPUGuPFA1QSEQvF2= NUDwXZE2W0GQR1XS
D-336MG NIPUXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nTWmlEPTB;MT64OVYyPCEQvF2= MWHTRW5ITVJ?
VA-ES-BJ NX\6VXRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUS5bHFZUUN3ME2xMlkxOzF3IN88US=> NGjmS3hUSU6JRWK=
MDA-MB-468 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnmyTWM2OD1zLkmxNlczKM7:TR?= MVXTRW5ITVJ?
MEL-HO Mo\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTFwOUe5PVMh|ryP NF\PXJdUSU6JRWK=
SW954 M2XTVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILXfZhKSzVyPUKuNFAyPTFizszN NIjUW3FUSU6JRWK=
LB831-BLC MmCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn36TWM2OD1{LkCwPVg5KM7:TR?= NW\rfop[W0GQR1XS
EW-16 NX3yUYN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PJZWlEPTB;Mj6wN|k5OyEQvF2= Ml7jV2FPT0WU
NCI-H460 NH7aVW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\0NWlEPTB;Mj6wOFg{QSEQvF2= MYHTRW5ITVJ?
CHP-212 MmXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3Qe3hrUUN3ME2yMlA6PTN7IN88US=> NH7JXFBUSU6JRWK=
MHH-NB-11 NFfaZmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zOR2lEPTB;Mj6xNlgyQCEQvF2= MnSxV2FPT0WU
DU-4475 M{PPfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLHcIdNUUN3ME2yMlE1PzV7IN88US=> NHntRmhUSU6JRWK=
ABC-1 M{n5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTJwMkWxPVYh|ryP MlXqV2FPT0WU
LOUCY MkXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTJwMk[xNlgh|ryP M{WyNHNCVkeHUh?=
LC-2-ad NEj3XXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;Dfm9KSzVyPUKuNlY6PjZizszN NV3MUWVDW0GQR1XS
ETK-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\W[2lEPTB;Mj6yPFQ3KM7:TR?= MlP0V2FPT0WU
KYSE-180 NH7Y[lBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXuTWM2OD1{LkK4PFc1KM7:TR?= MX;TRW5ITVJ?
HOP-92 M37ydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJwM{C2O|Mh|ryP NHm4cG1USU6JRWK=
RCC10RGB MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjZV4J1UUN3ME2yMlMzPTB5IN88US=> M2\sV3NCVkeHUh?=
KASUMI-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TqNmlEPTB;Mj6zNlg5KM7:TR?= NHn5fm9USU6JRWK=
ACN NInMV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rkVWlEPTB;Mj6zOFc1PSEQvF2= NVTR[GNEW0GQR1XS
BxPC-3 NHSzTnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXKcFFKSzVyPUKuN|U1OzZizszN M1vtSXNCVkeHUh?=
MONO-MAC-6 NXz3[IF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJwNEGyOFgh|ryP MlP1V2FPT0WU
CAL-39 NGjnU5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTJwNEG2Nlgh|ryP NGW5cHZUSU6JRWK=
CMK NF\lVHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJwNEG3PVUh|ryP NHfqemhUSU6JRWK=
MFE-296 Mn7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2i4cmlEPTB;Mj60O|c6OiEQvF2= MUjTRW5ITVJ?
DU-145 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTJwNEmxNVgh|ryP NYOz[oUzW0GQR1XS
MDA-MB-231 M1[1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnyflVKSzVyPUKuOFk2PzJizszN NVPRZmRYW0GQR1XS
EFO-27 M2TtdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJwNUG4PFgh|ryP MWHTRW5ITVJ?
SNU-387 Mo\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHGXnVKSzVyPUKuOVI5OiEQvF2= M1TUc3NCVkeHUh?=
KYSE-410 NFTuNINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PPUGlEPTB;Mj61OlUyPyEQvF2= MWDTRW5ITVJ?
NCCIT M2fUOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTJwNUeyOEDPxE1? NEXPTZJUSU6JRWK=
LXF-289 M3vXWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XZNWlEPTB;Mj61PFI4OyEQvF2= NYO3UVdHW0GQR1XS
HMV-II MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXq3c3BuUUN3ME2yMlU5QTl5IN88US=> M3LWbnNCVkeHUh?=
MOLT-4 NXfUfVNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2KxVmlEPTB;Mj62NFcyOiEQvF2= NF[zdHZUSU6JRWK=
KOSC-2 MmmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWL0RplvUUN3ME2yMlY{QDd7IN88US=> M4fnenNCVkeHUh?=
TUR MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTJwNkWzOlkh|ryP NXH0[IR2W0GQR1XS
NCI-H2087 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJwN{G2OFYh|ryP MkXlV2FPT0WU
SCC-15 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPUTWM2OD1{Lke1NlUzKM7:TR?= M4X4VHNCVkeHUh?=
HSC-4 NIPaPGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnO3TWM2OD1{Lke4N|g6KM7:TR?= Mm[3V2FPT0WU
G-402 M2j4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTJwOEG0OFch|ryP NYWyZ49JW0GQR1XS
GP5d MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2f1[mlEPTB;Mj64N|gzPyEQvF2= M{HQZXNCVkeHUh?=
IGR-1 NGLpd3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnLc3VKSzVyPUKuPFM6QDdizszN NX;TU|VjW0GQR1XS
SK-PN-DW NVPQOYRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTKNGVHUUN3ME2yMlg3OjB2IN88US=> Ml\VV2FPT0WU
OPM-2 M3\NR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnZTWM2OD1{Lki5PVc5KM7:TR?= MV7TRW5ITVJ?
5637 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PlW2lEPTB;Mj65NlQ{QSEQvF2= NHHDVWZUSU6JRWK=
NCI-H2030 NGPmcFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTJwOUiwNlkh|ryP NVjpU5NDW0GQR1XS
SK-LU-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnQfmZCUUN3ME2yMlk5OzN2IN88US=> NXHOOVRLW0GQR1XS
EW-18 NIDSNWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT2TWM2OD1|LkC1N|Ih|ryP MkTxV2FPT0WU
786-0 NYXlNGZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rWN2lEPTB;Mz6wOVc5PCEQvF2= NFP4[mhUSU6JRWK=
NCI-H1963 MnPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HDSmlEPTB;Mz6wPFgzPSEQvF2= MnHQV2FPT0WU
A2780 NYf1OIs3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HE[WlEPTB;Mz6xNFM1OSEQvF2= NELJbmVUSU6JRWK=
NCI-H526 MoD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mme3TWM2OD1|LkGzPVYyKM7:TR?= NHXCbm9USU6JRWK=
BHT-101 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTNwMUW3PVgh|ryP MnXMV2FPT0WU
RPMI-7951 MlqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGniVXVKSzVyPUOuNlAyOzdizszN NVTifFBuW0GQR1XS
HL-60 MlfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTNwMkGxOEDPxE1? MoXSV2FPT0WU
CTV-1 NGHM[GxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTNwMkWzO|ch|ryP NI\TU3dUSU6JRWK=
IST-SL1 M2rQdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjFRo5DUUN3ME2zMlI6PDZ3IN88US=> M3HKe3NCVkeHUh?=
G-401 NFu5eJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XkW2lEPTB;Mz6yPVgxQCEQvF2= M3T3VnNCVkeHUh?=
OVCAR-5 NYSxUpFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTNwM{[zOVIh|ryP NHnNS45USU6JRWK=
EW-1 M1zQdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfjXGtYUUN3ME2zMlQxPTR2IN88US=> NYXIU4VYW0GQR1XS
H4 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrOT21SUUN3ME2zMlQ4PTZ7IN88US=> MYLTRW5ITVJ?
EM-2 NYnmSYRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj0Tm5{UUN3ME2zMlQ5Pjd2IN88US=> NE\SXWdUSU6JRWK=
RS4-11 M4TXfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGruXZZKSzVyPUOuOFg4OTVizszN MUjTRW5ITVJ?
NOMO-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrKb2xKSzVyPUOuOFkzODRizszN NVnWTJNOW0GQR1XS
HCT-116 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jEZ2lEPTB;Mz61NFcyOSEQvF2= MXLTRW5ITVJ?
CAL-120 Mn7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLWTWM2OD1|LkW3N|Uh|ryP MX3TRW5ITVJ?
CAL-51 Mn3oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDTTWM2OD1|LkW3OlEzKM7:TR?= NXTvcHhlW0GQR1XS
RVH-421 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTNwNkCzNVEh|ryP M2jNNXNCVkeHUh?=
NCI-H2081 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXMb49KSzVyPUOuOlUzQDhizszN NYX0boRGW0GQR1XS
SBC-5 Ml;BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTNwNke4PFIh|ryP NXX1[3VHW0GQR1XS
RL95-2 M2jrRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHVTWM2OD1|LkexPFY1KM7:TR?= MoLFV2FPT0WU
SW872 MknqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTNwN{[5OVgh|ryP NVvPcmp{W0GQR1XS
VM-CUB-1 MnTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj6TWM2OD1|Lke3OVEh|ryP M{XCR3NCVkeHUh?=
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NCI-H2342 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4faRmlEPTB;NEWuNVEyPyEQvF2= MUfTRW5ITVJ?
NCI-H1703 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLjTWM2OD12Nj6wOVkzKM7:TR?= Mmf2V2FPT0WU
NCI-H187 NW[3SFFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjDRpY2UUN3ME20Ok4yQDZ7IN88US=> MWXTRW5ITVJ?
CP66-MEL NHTub4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTR4LkK3PFkh|ryP MWXTRW5ITVJ?
HCC1569 NIHYPFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\xTWM2OD12Nj61PVE4KM7:TR?= MYPTRW5ITVJ?
BL-70 MoS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzrfXRKSzVyPUS2Mlc4OzdizszN NXvpV|VXW0GQR1XS
Saos-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTR5LkOxNlMh|ryP M37CNHNCVkeHUh?=
LC-1F MmTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTR5Lk[xNFUh|ryP Mn3sV2FPT0WU
KY821 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LhUWlEPTB;NEeuOlQ{PCEQvF2= MmPqV2FPT0WU
PSN1 NEfYUpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLITWM2OD12OD6xOFAyKM7:TR?= NFXNbW9USU6JRWK=
RT4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTR6LkizO|ch|ryP NHq5N2FUSU6JRWK=
LS-1034 M3:4W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnCd5R6UUN3ME20PE45QTV2IN88US=> NUnaelNQW0GQR1XS
NCI-H1395 NXu2ZYhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIn0flhKSzVyPUS5MlA1QTJizszN M2S1fHNCVkeHUh?=
EKVX NVLvdYNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HrVGlEPTB;NEmuOlc{OSEQvF2= M3fkcXNCVkeHUh?=
IST-MES1 M3rUeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PZRmlEPTB;NEmuPFk1PCEQvF2= MmfoV2FPT0WU

... 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 N/A
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
    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