PF-562271

For research use only.

Catalog No.S2890

78 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 78 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 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXXTWM2OD1yLkK3OlYh|ryP MUfTRW5ITVJ?
SW982 NWmxXXB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEP2[IhKSzVyPUCuN|I5OiEQvF2= M3;lO3NCVkeHUh?=
KM12 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDVRXVKSzVyPUCuN|g2PTdizszN NVvPN4FZW0GQR1XS
COLO-205 NWH1XYhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNEi2OVgh|ryP MnnWV2FPT0WU
COLO-829 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTzXpFKSzVyPUCuO|UyPzZizszN NUPNOHR4W0GQR1XS
MG-63 NWjVco9UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVq1VJlqUUN3ME2wMlgxPjN5IN88US=> MkPuV2FPT0WU
IGROV-1 NFfBWHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTQUXVKSzVyPUCuPFExOzhizszN MmLHV2FPT0WU
NCI-H650 NYrXdmROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\6Z2JKSzVyPUCuPFMyPTRizszN Mn3TV2FPT0WU
RT-112 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\kTWM2OD1yLkm4OFYh|ryP NFqxfnRUSU6JRWK=
BCPAP NITQR3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\LTWM2OD1zLkCxNlg5KM7:TR?= MnHxV2FPT0WU
ALL-PO MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIW1dFBKSzVyPUGuNFE2QDRizszN MVPTRW5ITVJ?
KYSE-270 NWHIPIlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mli3TWM2OD1zLkC0O|E1KM7:TR?= M3XPbHNCVkeHUh?=
8305C MkizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFwMEm5NFQh|ryP MoHUV2FPT0WU
NCI-H810 NILJVIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXBTWM2OD1zLkGwO|c3KM7:TR?= MXrTRW5ITVJ?
CAL-33 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v0N2lEPTB;MT6xNlk{QCEQvF2= NGnIfZpUSU6JRWK=
AN3-CA NFPFUpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnzc4JIUUN3ME2xMlIyQDZ5IN88US=> NEHHfoZUSU6JRWK=
NKM-1 MnjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nxWGlEPTB;MT6yO|UxPiEQvF2= NEXUSlJUSU6JRWK=
BPH-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnRTWM2OD1zLkK4O|Y3KM7:TR?= Mme0V2FPT0WU
MES-SA NGHjR|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPoTWM2OD1zLkOwOlgzKM7:TR?= NVXVSZpuW0GQR1XS
CAL-62 M3zGcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfjd5ZZUUN3ME2xMlMyQTB7IN88US=> MVHTRW5ITVJ?
Detroit562 NYfr[ZlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfTUW1EUUN3ME2xMlM2OjJ{IN88US=> MmjnV2FPT0WU
KYSE-150 M4XsUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TrfWlEPTB;MT6zOVI{PiEQvF2= NYrPUowyW0GQR1XS
SK-UT-1 M4DsPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XSZWlEPTB;MT60OFY1PyEQvF2= NVnLRVZPW0GQR1XS
HUTU-80 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTFwNES4PFYh|ryP MWjTRW5ITVJ?
SIG-M5 M{\1TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH6wN4lKSzVyPUGuOFg{QDdizszN MkjDV2FPT0WU
AGS M1zPSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTFwNUKxNlQh|ryP M1SwW3NCVkeHUh?=
ST486 MkC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrERYJrUUN3ME2xMlU{Ojd6IN88US=> M1fUZXNCVkeHUh?=
HSC-2 NYri[XJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFO3ZlVKSzVyPUGuOVM6PSEQvF2= NWq1VGlnW0GQR1XS
LCLC-103H NEXRcG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvVN2FKSzVyPUGuOVU5OThizszN MonvV2FPT0WU
BC-1 NWr1eWI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jUfmlEPTB;MT62NVY3PCEQvF2= NETOS5BUSU6JRWK=
CGTH-W-1 NEj4RXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XWeGlEPTB;MT62NVY4QSEQvF2= MYXTRW5ITVJ?
MZ1-PC M{KxZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHyTWM2OD1zLk[yN|EzKM7:TR?= NXXIVJFWW0GQR1XS
SW1710 MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DuZmlEPTB;MT62NlYzQCEQvF2= MWnTRW5ITVJ?
EW-13 NWPqZotWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTFwNkO0OlYh|ryP M3rje3NCVkeHUh?=
TE-11 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnn0TWM2OD1zLk[zOVIzKM7:TR?= NHfFVG5USU6JRWK=
BHY NH2yO5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTFwNkW2OlMh|ryP MkLNV2FPT0WU
ML-2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3k[3VKUUN3ME2xMlY3QDB{IN88US=> NGPaeHpUSU6JRWK=
MEL-JUSO NVTjU3VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfYPXF6UUN3ME2xMlczQDlzIN88US=> NYXs[|EzW0GQR1XS
U251 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTPWGpXUUN3ME2xMlc1ODNzIN88US=> NWjhOI5{W0GQR1XS
MHH-ES-1 NFnYVXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK1U4I1UUN3ME2xMlc6PTZ6IN88US=> MYPTRW5ITVJ?
CAL-85-1 MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFqzRm1KSzVyPUGuPFA1QSEQvF2= NWrxd5RoW0GQR1XS
D-336MG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzOWlVRUUN3ME2xMlg2PjF2IN88US=> NFq3fnRUSU6JRWK=
VA-ES-BJ Mnf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T0N2lEPTB;MT65NFMyPSEQvF2= M{T4R3NCVkeHUh?=
MDA-MB-468 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTFwOUGyO|Ih|ryP NHrCTIZUSU6JRWK=
MEL-HO MnHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTFwOUe5PVMh|ryP MnKzV2FPT0WU
SW954 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P6[GlEPTB;Mj6wNFE2OSEQvF2= NF3Jdm5USU6JRWK=
LB831-BLC NEnoTZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUiwSI1XUUN3ME2yMlAxQTh6IN88US=> MXTTRW5ITVJ?
EW-16 NEXFSo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX[1ZYxnUUN3ME2yMlA{QTh|IN88US=> NHTEXGxUSU6JRWK=
NCI-H460 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HOSGlEPTB;Mj6wOFg{QSEQvF2= NFe1eI5USU6JRWK=
CHP-212 MmXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\TSWlEPTB;Mj6wPVU{QSEQvF2= MWnTRW5ITVJ?
MHH-NB-11 NFLJbYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJwMUK4NVgh|ryP MoTuV2FPT0WU
DU-4475 NWPoeWV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH0[4lDUUN3ME2yMlE1PzV7IN88US=> MX;TRW5ITVJ?
ABC-1 NYPldItnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PRfWlEPTB;Mj6yOVE6PiEQvF2= NE\teFFUSU6JRWK=
LOUCY NXTubJBjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXYc2xKSzVyPUKuNlYyOjhizszN MUDTRW5ITVJ?
LC-2-ad NF\KfGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzwVVVKSzVyPUKuNlY6PjZizszN MVnTRW5ITVJ?
ETK-1 M{nOdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHrUHU4UUN3ME2yMlI5PDZizszN M3PEW3NCVkeHUh?=
KYSE-180 M3nwcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnJeW1KSzVyPUKuNlg5PzRizszN NUO1U3BDW0GQR1XS
HOP-92 NEe2R4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVi2U3l2UUN3ME2yMlMxPjd|IN88US=> NIrxWplUSU6JRWK=
RCC10RGB NIPLfWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzzTWM2OD1{LkOyOVA4KM7:TR?= NXHLe|RTW0GQR1XS
KASUMI-1 NHPaS2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTJwM{K4PEDPxE1? NHPSUnZUSU6JRWK=
ACN MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvz[mNKSzVyPUKuN|Q4PDVizszN NV3rToM6W0GQR1XS
BxPC-3 M2nKTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJwM{W0N|Yh|ryP Mlv4V2FPT0WU
MONO-MAC-6 NFzIOnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYD1bG0yUUN3ME2yMlQyOjR6IN88US=> NY\sTnRSW0GQR1XS
CAL-39 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;vTWM2OD1{LkSxOlI5KM7:TR?= MmnmV2FPT0WU
CMK M1zoZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T1[mlEPTB;Mj60NVc6PSEQvF2= MV\TRW5ITVJ?
MFE-296 M2TzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHiWGtGUUN3ME2yMlQ4Pzl{IN88US=> NGL3Zm5USU6JRWK=
DU-145 NInVfoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTJwNEmxNVgh|ryP MW\TRW5ITVJ?
MDA-MB-231 M33Zc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPtTItMUUN3ME2yMlQ6PTd{IN88US=> MmXXV2FPT0WU
EFO-27 NIXhZ|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\qPZFxUUN3ME2yMlUyQDh6IN88US=> NWfC[FlKW0GQR1XS
SNU-387 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDzTWM2OD1{LkWyPFIh|ryP MXrTRW5ITVJ?
KYSE-410 Mn3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJwNU[1NVch|ryP M2fSPHNCVkeHUh?=
NCCIT Mny3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFP0VVZKSzVyPUKuOVczPCEQvF2= M{PkbHNCVkeHUh?=
LXF-289 M1ywTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HxR2lEPTB;Mj61PFI4OyEQvF2= NX3yPFB1W0GQR1XS
HMV-II MmD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJwNUi5PVch|ryP NXj3V2YzW0GQR1XS
MOLT-4 NWDzOG9wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVr2fZZ1UUN3ME2yMlYxPzF{IN88US=> MWXTRW5ITVJ?
KOSC-2 MlvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{OySmlEPTB;Mj62N|g4QSEQvF2= NXXnRmNFW0GQR1XS
TUR M13aXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFj1T2VKSzVyPUKuOlU{PjlizszN NYC2ZohpW0GQR1XS
NCI-H2087 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVO1W|hbUUN3ME2yMlcyPjR4IN88US=> NX;oSmViW0GQR1XS
SCC-15 M1;memdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTJwN{WyOVIh|ryP MULTRW5ITVJ?
HSC-4 M1LTNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTJwN{izPFkh|ryP NIDlZnZUSU6JRWK=
G-402 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDQTWM2OD1{LkixOFQ4KM7:TR?= M{jhV3NCVkeHUh?=
GP5d NGHZdVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[1XmtKSzVyPUKuPFM5OjdizszN NEDsb25USU6JRWK=
IGR-1 M1;3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vUPGlEPTB;Mj64N|k5PyEQvF2= NWH4RnhiW0GQR1XS
SK-PN-DW NGr5[mRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PuZmlEPTB;Mj64OlIxPCEQvF2= NWjnOVE2W0GQR1XS
OPM-2 MmXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnjTWM2OD1{Lki5PVc5KM7:TR?= MVzTRW5ITVJ?
5637 MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jSbGlEPTB;Mj65NlQ{QSEQvF2= MYnTRW5ITVJ?
NCI-H2030 M{XjRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTJwOUiwNlkh|ryP M4rQc3NCVkeHUh?=
SK-LU-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfCfZVMUUN3ME2yMlk5OzN2IN88US=> NF7WZmFUSU6JRWK=
EW-18 M2[xVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHVZZBKSzVyPUOuNFU{OiEQvF2= MnPRV2FPT0WU
786-0 NFrKTYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHw[HI6UUN3ME2zMlA2Pzh2IN88US=> MnvmV2FPT0WU
NCI-H1963 MnzaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPHTWM2OD1|LkC4PFI2KM7:TR?= MWDTRW5ITVJ?
A2780 NEDXXlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTNwMUCzOFEh|ryP NFzKUXdUSU6JRWK=
NCI-H526 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXX0N2lEUUN3ME2zMlE{QTZzIN88US=> NWPo[FBWW0GQR1XS
BHT-101 NHHpR4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTNwMUW3PVgh|ryP M1vuVnNCVkeHUh?=
RPMI-7951 NHvLcFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnriTWM2OD1|LkKwNVM4KM7:TR?= NFXucHlUSU6JRWK=
HL-60 NXi4fWJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfVTWM2OD1|LkKxNVQh|ryP NU\BVZVFW0GQR1XS
CTV-1 NF3MSlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHuxNJJKSzVyPUOuNlU{PzdizszN Mlz2V2FPT0WU
IST-SL1 Ml;uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTNwMkm0OlUh|ryP NFm0WJNUSU6JRWK=
G-401 NVj5dm9uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnPW4pjUUN3ME2zMlI6QDB6IN88US=> NEPlOYdUSU6JRWK=
OVCAR-5 NFmyVYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPsdZkzUUN3ME2zMlM3OzV{IN88US=> MlvOV2FPT0WU
EW-1 MkDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojiTWM2OD1|LkSwOVQ1KM7:TR?= NXrUVlB6W0GQR1XS
H4 NYnZZVNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LiWmlEPTB;Mz60O|U3QSEQvF2= M4\udHNCVkeHUh?=
EM-2 M{PhS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\lTWM2OD1|LkS4Olc1KM7:TR?= NGGwR2VUSU6JRWK=
RS4-11 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\pT3JKSzVyPUOuOFg4OTVizszN MWXTRW5ITVJ?
NOMO-1 M3zhUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULY[IZOUUN3ME2zMlQ6OjB2IN88US=> NH2yRYdUSU6JRWK=
HCT-116 NXr6SlZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfZVoFKSzVyPUOuOVA4OTFizszN NVP2cFFQW0GQR1XS
CAL-120 NEjxRpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PkZ2lEPTB;Mz61O|M2KM7:TR?= NFO5VIxUSU6JRWK=
CAL-51 M2\3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmewTWM2OD1|LkW3OlEzKM7:TR?= NXPzRpd5W0GQR1XS
RVH-421 MnnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\IfopKSzVyPUOuOlA{OTFizszN NEDUbJdUSU6JRWK=
NCI-H2081 Ml;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XCNWlEPTB;Mz62OVI5QCEQvF2= MYHTRW5ITVJ?
SBC-5 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPl[HltUUN3ME2zMlY4QDh{IN88US=> NEn3UJFUSU6JRWK=
RL95-2 NX\ld2Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFP4VVdKSzVyPUOuO|E5PjRizszN NVTqeFRqW0GQR1XS
SW872 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TTUmlEPTB;Mz63Olk2QCEQvF2= NVy5NXU2W0GQR1XS
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SUP-T1 M2Du[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTNwN{izNkDPxE1? NVvBUotxW0GQR1XS
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NCI-H2342 NGnrTJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjmO5RKSzVyPUS1MlEyOTdizszN MkKxV2FPT0WU
NCI-H1703 NHzod3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{e4eGlEPTB;NE[uNFU6OiEQvF2= MYPTRW5ITVJ?
NCI-H187 M{\zeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrGTWM2OD12Nj6xPFY6KM7:TR?= NFHmXJNUSU6JRWK=
CP66-MEL NF\kN3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLqTWM2OD12Nj6yO|g6KM7:TR?= M4PmdXNCVkeHUh?=
HCC1569 M4C5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTR4LkW5NVch|ryP NWnNNGpvW0GQR1XS
BL-70 M3jvR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTR4Lke3N|ch|ryP NHzyTotUSU6JRWK=
Saos-2 MmPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LrWGlEPTB;NEeuN|EzOyEQvF2= M3W2PHNCVkeHUh?=
LC-1F NHPVcndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFq4TnNKSzVyPUS3MlYyODVizszN MoD0V2FPT0WU
KY821 MnT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fMZWlEPTB;NEeuOlQ{PCEQvF2= NYj1XY1sW0GQR1XS
PSN1 M4D6XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT2WIRKSzVyPUS4MlE1ODFizszN NWTIWlBJW0GQR1XS
RT4 MmKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jHSmlEPTB;NEiuPFM4PyEQvF2= NH\W[ldUSU6JRWK=
LS-1034 NXfWWFIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\kRXdKSzVyPUS4Mlg6PTRizszN NVP4ZVhCW0GQR1XS
NCI-H1395 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonuTWM2OD12OT6wOFkzKM7:TR?= MkHmV2FPT0WU
EKVX MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjmTWM2OD12OT62O|MyKM7:TR?= NFvBZmFUSU6JRWK=
IST-MES1 M4XiOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXSxO|VsUUN3ME20PU45QTR2IN88US=> MmThV2FPT0WU

... 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):
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    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