PF-562271

Catalog No.S2890

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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In DMSO USD 350 In stock
USD 170 In stock
USD 270 In stock
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USD 970 In stock
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Cited by 66 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 NUXxcWVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDZcGRKSzVyPUCuNlc3PiEQvF2= MU\TRW5ITVJ?
SW982 MnLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUWyO|dkUUN3ME2wMlMzQDJizszN M4e1RnNCVkeHUh?=
KM12 M3zqN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjjZZRKSzVyPUCuN|g2PTdizszN M2S3U3NCVkeHUh?=
COLO-205 M{[yTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnkWZVyUUN3ME2wMlQ5PjV6IN88US=> NHfJeoVUSU6JRWK=
COLO-829 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTBwN{WxO|Yh|ryP M1[1RXNCVkeHUh?=
MG-63 NWjHVGJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjmXIlUUUN3ME2wMlgxPjN5IN88US=> M{DSeXNCVkeHUh?=
IGROV-1 NGTzcHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnld3BKSzVyPUCuPFExOzhizszN M{TNdnNCVkeHUh?=
NCI-H650 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILoNoNKSzVyPUCuPFMyPTRizszN M1;sXHNCVkeHUh?=
RT-112 NGjMPWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGq1c4JKSzVyPUCuPVg1PiEQvF2= MX;TRW5ITVJ?
BCPAP MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLPSHlKSzVyPUGuNFEzQDhizszN NFHZcIRUSU6JRWK=
ALL-PO MoLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYThbZZ5UUN3ME2xMlAyPTh2IN88US=> NH24S5lUSU6JRWK=
KYSE-270 M4LEdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnFcHhKSzVyPUGuNFQ4OTRizszN MkPwV2FPT0WU
8305C MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\4SpV2UUN3ME2xMlA6QTB2IN88US=> M2rST3NCVkeHUh?=
NCI-H810 NXzWe5BnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2KyemlEPTB;MT6xNFc4PiEQvF2= M3;KU3NCVkeHUh?=
CAL-33 M1L5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXzcZh4UUN3ME2xMlEzQTN6IN88US=> M1jtSXNCVkeHUh?=
AN3-CA M1fFXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfoTWM2OD1zLkKxPFY4KM7:TR?= M1zxXnNCVkeHUh?=
NKM-1 NFfSe2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[yfG9KSzVyPUGuNlc2ODZizszN MUPTRW5ITVJ?
BPH-1 NEjYOldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTFwMki3OlYh|ryP NULuTFE2W0GQR1XS
MES-SA MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFwM{C2PFIh|ryP M1f1SXNCVkeHUh?=
CAL-62 NGHrcJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPXTWM2OD1zLkOxPVA6KM7:TR?= MXPTRW5ITVJ?
Detroit562 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzGTWM2OD1zLkO1NlIzKM7:TR?= MWrTRW5ITVJ?
KYSE-150 NVzRZm1vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvYZXhKSzVyPUGuN|UzOzZizszN NHnRU2NUSU6JRWK=
SK-UT-1 M{[yNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXYeWRKSzVyPUGuOFQ3PDdizszN NHS1TJNUSU6JRWK=
HUTU-80 MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTFwNES4PFYh|ryP NVfLSWhzW0GQR1XS
SIG-M5 NFjtN5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfDTGtiUUN3ME2xMlQ5Ozh5IN88US=> M2C4NXNCVkeHUh?=
AGS MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3z1SGlEPTB;MT61NlEzPCEQvF2= M125PHNCVkeHUh?=
ST486 M{XiOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGO0S2hKSzVyPUGuOVMzPzhizszN M2KwUnNCVkeHUh?=
HSC-2 NWntXpJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;WTWM2OD1zLkWzPVUh|ryP MnHqV2FPT0WU
LCLC-103H MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTFwNUW4NVgh|ryP NEntdW1USU6JRWK=
BC-1 NI\sXnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmW5TWM2OD1zLk[xOlY1KM7:TR?= MnX0V2FPT0WU
CGTH-W-1 NUXJXVZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTFwNkG2O|kh|ryP NIrEd5NUSU6JRWK=
MZ1-PC MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37vSGlEPTB;MT62NlMyOiEQvF2= NH7BXI9USU6JRWK=
SW1710 NVvpbIZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLBTWM2OD1zLk[yOlI5KM7:TR?= MWfTRW5ITVJ?
EW-13 M4XXeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7hO|BKSzVyPUGuOlM1PjZizszN MnfkV2FPT0WU
TE-11 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPjT|JiUUN3ME2xMlY{PTJ{IN88US=> NYHhe2JYW0GQR1XS
BHY NFe2OlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHSwcJdKSzVyPUGuOlU3PjNizszN MlzwV2FPT0WU
ML-2 M1nRR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTFwNk[4NFIh|ryP M{nXSHNCVkeHUh?=
MEL-JUSO M2HWOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;lTWM2OD1zLkeyPFkyKM7:TR?= M4i0dHNCVkeHUh?=
U251 NUX6SW9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mli2TWM2OD1zLke0NFMyKM7:TR?= M1fXd3NCVkeHUh?=
MHH-ES-1 NWLM[WMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:0XXpKSzVyPUGuO|k2PjhizszN Ml:0V2FPT0WU
CAL-85-1 NHzST3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zkV2lEPTB;MT64NFQ6KM7:TR?= MkG3V2FPT0WU
D-336MG M{DzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjaR4lKSzVyPUGuPFU3OTRizszN M2jONnNCVkeHUh?=
VA-ES-BJ Mn7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rRW2lEPTB;MT65NFMyPSEQvF2= MYjTRW5ITVJ?
MDA-MB-468 NWfkXlFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\STmlEPTB;MT65NVI4OiEQvF2= MnzwV2FPT0WU
MEL-HO M{f4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYW1[pRbUUN3ME2xMlk4QTl|IN88US=> NU\xTVlQW0GQR1XS
SW954 NGK4[o9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjIb45KSzVyPUKuNFAyPTFizszN NILQW41USU6JRWK=
LB831-BLC Mn\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HSRWlEPTB;Mj6wNFk5QCEQvF2= NV3ZV|dqW0GQR1XS
EW-16 M2fGVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTJwMEO5PFMh|ryP NHjsPGtUSU6JRWK=
NCI-H460 NFfycHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LBVmlEPTB;Mj6wOFg{QSEQvF2= MnHvV2FPT0WU
CHP-212 NWD0dYJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fRcWlEPTB;Mj6wPVU{QSEQvF2= MmTCV2FPT0WU
MHH-NB-11 NV;EXGNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[xTZhwUUN3ME2yMlEzQDF6IN88US=> MY\TRW5ITVJ?
DU-4475 NFLLO41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTJwMUS3OVkh|ryP M4HGNXNCVkeHUh?=
ABC-1 NYf5Om5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDxTWM2OD1{LkK1NVk3KM7:TR?= MnLIV2FPT0WU
LOUCY M17FdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\mdGVPUUN3ME2yMlI3OTJ6IN88US=> MkW4V2FPT0WU
LC-2-ad M{W0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTJwMk[5OlYh|ryP M33iNHNCVkeHUh?=
ETK-1 M1rqO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnXTJdKSzVyPUKuNlg1PiEQvF2= NGPTXWNUSU6JRWK=
KYSE-180 M4myc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTSNGhKSzVyPUKuNlg5PzRizszN NWq4OpZ{W0GQR1XS
HOP-92 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHTTWM2OD1{LkOwOlc{KM7:TR?= MlPJV2FPT0WU
RCC10RGB MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjWT3JKSzVyPUKuN|I2ODdizszN MYTTRW5ITVJ?
KASUMI-1 NVvmbXpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEe0[GhKSzVyPUKuN|I5QCEQvF2= NIWzTFNUSU6JRWK=
ACN NWHVS4hyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYL4e|FCUUN3ME2yMlM1PzR3IN88US=> Mmf6V2FPT0WU
BxPC-3 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zKVmlEPTB;Mj6zOVQ{PiEQvF2= MnyxV2FPT0WU
MONO-MAC-6 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzDdZZKSzVyPUKuOFEzPDhizszN M17WZ3NCVkeHUh?=
CAL-39 NWC0SJFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvsNlZPUUN3ME2yMlQyPjJ6IN88US=> MWHTRW5ITVJ?
CMK M3rpemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLUTWM2OD1{LkSxO|k2KM7:TR?= M3fEcXNCVkeHUh?=
MFE-296 MnKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\PPWtyUUN3ME2yMlQ4Pzl{IN88US=> MmiyV2FPT0WU
DU-145 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofTTWM2OD1{LkS5NVE5KM7:TR?= MYnTRW5ITVJ?
MDA-MB-231 NXW2XHBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2K2NWlEPTB;Mj60PVU4OiEQvF2= MWnTRW5ITVJ?
EFO-27 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHK5PG5KSzVyPUKuOVE5QDhizszN NYf1bGFSW0GQR1XS
SNU-387 MoPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTJwNUK4NkDPxE1? Ml\hV2FPT0WU
KYSE-410 NFnZN2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLlcFFxUUN3ME2yMlU3PTF5IN88US=> NYfkeJViW0GQR1XS
NCCIT M1fkRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LHUGlEPTB;Mj61O|I1KM7:TR?= MX3TRW5ITVJ?
LXF-289 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTJwNUiyO|Mh|ryP NV35b2M4W0GQR1XS
HMV-II NXnZV3VHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETmbnRKSzVyPUKuOVg6QTdizszN MkWzV2FPT0WU
MOLT-4 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJwNkC3NVIh|ryP NHnSOHlUSU6JRWK=
KOSC-2 M{L4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTJwNkO4O|kh|ryP M3;RcHNCVkeHUh?=
TUR NEfxT5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\0TWM2OD1{Lk[1N|Y6KM7:TR?= NIHN[29USU6JRWK=
NCI-H2087 MnPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkf0TWM2OD1{LkexOlQ3KM7:TR?= MlXFV2FPT0WU
SCC-15 M4jpdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\BeoxUUUN3ME2yMlc2OjV{IN88US=> NYK4eJdzW0GQR1XS
HSC-4 M3W3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrPSIo6UUN3ME2yMlc5Ozh7IN88US=> NUnEeYk3W0GQR1XS
G-402 M3GyPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTJwOEG0OFch|ryP M2Hje3NCVkeHUh?=
GP5d M2\wUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkL2TWM2OD1{LkizPFI4KM7:TR?= MWnTRW5ITVJ?
IGR-1 NFnXbIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILsb5FKSzVyPUKuPFM6QDdizszN MkHaV2FPT0WU
SK-PN-DW NEfZUXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjBSJdPUUN3ME2yMlg3OjB2IN88US=> M3nMSXNCVkeHUh?=
OPM-2 MoHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLkTWM2OD1{Lki5PVc5KM7:TR?= NFzhT3BUSU6JRWK=
5637 M2GxNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJwOUK0N|kh|ryP NGf3bYZUSU6JRWK=
NCI-H2030 M{TtOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjXeJpKSzVyPUKuPVgxOjlizszN MUnTRW5ITVJ?
SK-LU-1 NXHyWoZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljqTWM2OD1{Lkm4N|M1KM7:TR?= MmPUV2FPT0WU
EW-18 NFv2bINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13COmlEPTB;Mz6wOVMzKM7:TR?= MUHTRW5ITVJ?
786-0 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTNwMEW3PFQh|ryP NWDmb|ZqW0GQR1XS
NCI-H1963 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTNwMEi4NlUh|ryP M1\sbXNCVkeHUh?=
A2780 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVf6dYpWUUN3ME2zMlExOzRzIN88US=> M3q4R3NCVkeHUh?=
NCI-H526 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTNwMUO5OlEh|ryP M3f3SXNCVkeHUh?=
BHT-101 NY\iTJNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfITWM2OD1|LkG1O|k5KM7:TR?= MYLTRW5ITVJ?
RPMI-7951 NFraW|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDYdmlUUUN3ME2zMlIxOTN5IN88US=> NFL0eodUSU6JRWK=
HL-60 NFrYTHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPnTWM2OD1|LkKxNVQh|ryP MoryV2FPT0WU
CTV-1 MnTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfJUpFVUUN3ME2zMlI2Ozd5IN88US=> M2niTXNCVkeHUh?=
IST-SL1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUewOWp1UUN3ME2zMlI6PDZ3IN88US=> MUnTRW5ITVJ?
G-401 NFTkcYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTNwMkm4NFgh|ryP MWTTRW5ITVJ?
OVCAR-5 M2\hXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfhTWM2OD1|LkO2N|UzKM7:TR?= NUDZfmZWW0GQR1XS
EW-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHNSmpGUUN3ME2zMlQxPTR2IN88US=> M{LiZnNCVkeHUh?=
H4 NGPBWGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfxUm9KSzVyPUOuOFc2PjlizszN NVrrNpZ1W0GQR1XS
EM-2 NX7McIk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37jZ2lEPTB;Mz60PFY4PCEQvF2= Mmn4V2FPT0WU
RS4-11 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\3R2lEPTB;Mz60PFcyPSEQvF2= NVHMfmZxW0GQR1XS
NOMO-1 NVjtd2MxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLtUWhKSzVyPUOuOFkzODRizszN M2LT[nNCVkeHUh?=
HCT-116 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjI[ndZUUN3ME2zMlUxPzFzIN88US=> MkPMV2FPT0WU
CAL-120 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTkc|hKSzVyPUOuOVc{PSEQvF2= MYDTRW5ITVJ?
CAL-51 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrmU3ZrUUN3ME2zMlU4PjF{IN88US=> NInuV4VUSU6JRWK=
RVH-421 M1Hre2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3uxUmlEPTB;Mz62NFMyOSEQvF2= MnPVV2FPT0WU
NCI-H2081 NEjKcGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTNwNkWyPFgh|ryP NYrPXnZbW0GQR1XS
SBC-5 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVSxRlY4UUN3ME2zMlY4QDh{IN88US=> M3zkenNCVkeHUh?=
RL95-2 NGPjcplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI[wRWFKSzVyPUOuO|E5PjRizszN M1TpRXNCVkeHUh?=
SW872 M1zaWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nmcmlEPTB;Mz63Olk2QCEQvF2= NHHBWFlUSU6JRWK=
VM-CUB-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nQ[GlEPTB;Mz63O|UyKM7:TR?= MorWV2FPT0WU
SUP-T1 MoTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{joTmlEPTB;Mz63PFMzKM7:TR?= MYjTRW5ITVJ?
697 MlHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TpZmlEPTB;Mz64NVY2PyEQvF2= NULnfnBzW0GQR1XS
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NCI-H187 M1Ptd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXoco9KSzVyPUS2MlE5PjlizszN NH35U|lUSU6JRWK=
CP66-MEL M4Xldmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTR4LkK3PFkh|ryP M3zVeHNCVkeHUh?=
HCC1569 NFPlWVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHu0cHRKSzVyPUS2MlU6OTdizszN NVzTTW44W0GQR1XS
BL-70 M1jwR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHyUHNUUUN3ME20Ok44PzN5IN88US=> M1LBbnNCVkeHUh?=
Saos-2 NV;Cb|BtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3:3fmlEPTB;NEeuN|EzOyEQvF2= MYXTRW5ITVJ?
LC-1F NGfGboRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTs[4FKSzVyPUS3MlYyODVizszN MX7TRW5ITVJ?
KY821 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\ZSmlEPTB;NEeuOlQ{PCEQvF2= NYrEWVlKW0GQR1XS
PSN1 M2XTRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHn4bIZKSzVyPUS4MlE1ODFizszN MofmV2FPT0WU
RT4 M2[1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoOzTWM2OD12OD64N|c4KM7:TR?= MkPDV2FPT0WU
LS-1034 NWGyNYxxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFuwcndKSzVyPUS4Mlg6PTRizszN M2rUUnNCVkeHUh?=
NCI-H1395 NWPRSZRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTR7LkC0PVIh|ryP MVTTRW5ITVJ?
EKVX NYXD[Jk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWT3PIpNUUN3ME20PU43PzNzIN88US=> MlfTV2FPT0WU
IST-MES1 NGXGNVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7mUVRKSzVyPUS5Mlg6PDRizszN MXvTRW5ITVJ?

... 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

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