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PF-562271 (VS-6062) inhibiteur de FAK/Pyk2

N° Cat.S2890

Le PF-562271 (PF-00562271) est un inhibiteur puissant, ATP-compétitif et réversible de FAK avec un IC50 de 1,5 nM dans les essais sans cellules, environ 10 fois moins puissant pour Pyk2 que FAK et une sélectivité >100 fois supérieure contre les autres protéines kinases, à l'exception de certaines CDKs.
PF-562271 (VS-6062) FAK inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 507.49

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Contrôle qualité

Lot : Pureté : 99.95%
99.95

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires Type dessai Concentration Temps dincubation Formulation Description de lactivité PMID
IST-MES1 Growth Inhibition Assay IC50=49.8944 μM SANGER
EKVX Growth Inhibition Assay IC50=49.6731 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=49.0492 μM SANGER
LS-1034 Growth Inhibition Assay IC50=48.8954 μM SANGER
RT4 Growth Inhibition Assay IC50=48.8377 μM SANGER
PSN1 Growth Inhibition Assay IC50=48.1401 μM SANGER
KY821 Growth Inhibition Assay IC50=47.6434 μM SANGER
LC-1F Growth Inhibition Assay IC50=47.6105 μM SANGER
Saos-2 Growth Inhibition Assay IC50=47.3123 μM SANGER
BL-70 Growth Inhibition Assay IC50=46.7737 μM SANGER
HCC1569 Growth Inhibition Assay IC50=46.5917 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=46.2789 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=46.1869 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=46.0592 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=45.1117 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=44.9136 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=44.7414 μM SANGER
SAS Growth Inhibition Assay IC50=43.4288 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=42.8008 μM SANGER
OAW-42 Growth Inhibition Assay IC50=42.2942 μM SANGER
PF-382 Growth Inhibition Assay IC50=40.7487 μM SANGER
COLO-678 Growth Inhibition Assay IC50=40.595 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=39.9977 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=39.6282 μM SANGER
SW756 Growth Inhibition Assay IC50=39.5091 μM SANGER
Capan-2 Growth Inhibition Assay IC50=39.0509 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=39.0218 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=38.0239 μM SANGER
A375 Growth Inhibition Assay IC50=37.7647 μM SANGER
RCM-1 Growth Inhibition Assay IC50=37.5358 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=37.4431 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=37.1903 μM SANGER
HCC1937 Growth Inhibition Assay IC50=37.0154 μM SANGER
no-11 Growth Inhibition Assay IC50=36.8536 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=36.7298 μM SANGER
SW1463 Growth Inhibition Assay IC50=36.6566 μM SANGER
NEC8 Growth Inhibition Assay IC50=36.4924 μM SANGER
BV-173 Growth Inhibition Assay IC50=35.8264 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=35.7718 μM SANGER
EFE-184 Growth Inhibition Assay IC50=35.6829 μM SANGER
HH Growth Inhibition Assay IC50=35.4141 μM SANGER
HC-1 Growth Inhibition Assay IC50=35.4024 μM SANGER
HCC2218 Growth Inhibition Assay IC50=35.2185 μM SANGER
NCI-H1417 Growth Inhibition Assay IC50=33.9585 μM SANGER
IA-LM Growth Inhibition Assay IC50=33.6746 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=33.654 μM SANGER
MC-IXC Growth Inhibition Assay IC50=33.5655 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=33.3679 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=33.2235 μM SANGER
EHEB Growth Inhibition Assay IC50=33.0494 μM SANGER
LU-165 Growth Inhibition Assay IC50=33.008 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=32.6163 μM SANGER
SW48 Growth Inhibition Assay IC50=32.3825 μM SANGER
DJM-1 Growth Inhibition Assay IC50=32.1386 μM SANGER
KM-H2 Growth Inhibition Assay IC50=31.7306 μM SANGER
SW620 Growth Inhibition Assay IC50=31.6283 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=31.5625 μM SANGER
LAN-6 Growth Inhibition Assay IC50=31.4992 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=31.3008 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=31.112 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=31.0621 μM SANGER
D-263MG Growth Inhibition Assay IC50=31.0424 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=30.8953 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=30.6794 μM SANGER
SW962 Growth Inhibition Assay IC50=30.2477 μM SANGER
LS-411N Growth Inhibition Assay IC50=30.1475 μM SANGER
HEC-1 Growth Inhibition Assay IC50=30.0053 μM SANGER
A673 Growth Inhibition Assay IC50=29.732 μM SANGER
CAL-54 Growth Inhibition Assay IC50=29.6046 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=29.5466 μM SANGER
TE-1 Growth Inhibition Assay IC50=29.2167 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=29.012 μM SANGER
KLE Growth Inhibition Assay IC50=28.9906 μM SANGER
D-283MED Growth Inhibition Assay IC50=28.8708 μM SANGER
NY Growth Inhibition Assay IC50=28.6579 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=28.3171 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=28.2592 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=28.2459 μM SANGER
T-24 Growth Inhibition Assay IC50=28.1925 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=28.0495 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=27.6975 μM SANGER
SNU-C1 Growth Inhibition Assay IC50=27.6491 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=27.5548 μM SANGER
T98G Growth Inhibition Assay IC50=27.1973 μM SANGER
LU-99A Growth Inhibition Assay IC50=27.1754 μM SANGER
U-2-OS Growth Inhibition Assay IC50=27.0271 μM SANGER
HuH-7 Growth Inhibition Assay IC50=26.9086 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=26.5553 μM SANGER
DSH1 Growth Inhibition Assay IC50=26.5406 μM SANGER
U-87-MG Growth Inhibition Assay IC50=26.5305 μM SANGER
Daudi Growth Inhibition Assay IC50=26.5158 μM SANGER
FADU Growth Inhibition Assay IC50=26.5152 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=25.9901 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=25.7501 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=25.7459 μM SANGER
D-247MG Growth Inhibition Assay IC50=25.4743 μM SANGER
CaR-1 Growth Inhibition Assay IC50=25.357 μM SANGER
TGW Growth Inhibition Assay IC50=25.2337 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=24.9237 μM SANGER
SW684 Growth Inhibition Assay IC50=24.7624 μM SANGER
SW1990 Growth Inhibition Assay IC50=24.5883 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=24.5217 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=24.4977 μM SANGER
EFM-19 Growth Inhibition Assay IC50=24.1844 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=23.7461 μM SANGER
PC-14 Growth Inhibition Assay IC50=23.6623 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=23.6093 μM SANGER
MC-CAR Growth Inhibition Assay IC50=23.5183 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=23.3546 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=23.2511 μM SANGER
SW1573 Growth Inhibition Assay IC50=23.0646 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=22.8836 μM SANGER
A498 Growth Inhibition Assay IC50=22.8177 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=22.6746 μM SANGER
IMR-5 Growth Inhibition Assay IC50=22.287 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=22.1677 μM SANGER
LS-513 Growth Inhibition Assay IC50=22.0367 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=21.9863 μM SANGER
OCUB-M Growth Inhibition Assay IC50=21.9688 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=21.8631 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=21.8596 μM SANGER
DOK Growth Inhibition Assay IC50=21.7687 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=21.6837 μM SANGER
COLO-792 Growth Inhibition Assay IC50=21.5827 μM SANGER
HCE-T Growth Inhibition Assay IC50=21.5094 μM SANGER
K-562 Growth Inhibition Assay IC50=21.4971 μM SANGER
NCI-H64 Growth Inhibition Assay IC50=21.4756 μM SANGER
K5 Growth Inhibition Assay IC50=21.3893 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=21.3288 μM SANGER
RKO Growth Inhibition Assay IC50=21.3202 μM SANGER
MFE-280 Growth Inhibition Assay IC50=21.3188 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=20.5814 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=20.4613 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=20.3953 μM SANGER
Raji Growth Inhibition Assay IC50=20.2568 μM SANGER
EW-7 Growth Inhibition Assay IC50=20.1628 μM SANGER
NOS-1 Growth Inhibition Assay IC50=20.1577 μM SANGER
NB10 Growth Inhibition Assay IC50=19.6268 μM SANGER
KU812 Growth Inhibition Assay IC50=19.5944 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=19.5725 μM SANGER
U031 Growth Inhibition Assay IC50=19.2219 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=19.2155 μM SANGER
HT-1376 Growth Inhibition Assay IC50=19.2029 μM SANGER
HCC1187 Growth Inhibition Assay IC50=19.1796 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=19.1754 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=18.8918 μM SANGER
NCI-H748 Growth Inhibition Assay IC50=18.8585 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=18.8299 μM SANGER
UACC-257 Growth Inhibition Assay IC50=18.2062 μM SANGER
TE-8 Growth Inhibition Assay IC50=18.0669 μM SANGER
EW-11 Growth Inhibition Assay IC50=17.9958 μM SANGER
CESS Growth Inhibition Assay IC50=17.9326 μM SANGER
A253 Growth Inhibition Assay IC50=17.825 μM SANGER
MN-60 Growth Inhibition Assay IC50=17.7936 μM SANGER
EB2 Growth Inhibition Assay IC50=17.7426 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=16.9219 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=16.6138 μM SANGER
THP-1 Growth Inhibition Assay IC50=16.4665 μM SANGER
TK10 Growth Inhibition Assay IC50=16.3742 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=16.2218 μM SANGER
HT-144 Growth Inhibition Assay IC50=15.9497 μM SANGER
Becker Growth Inhibition Assay IC50=15.8926 μM SANGER
DB Growth Inhibition Assay IC50=15.6941 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=15.4163 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=15.2868 μM SANGER
LK-2 Growth Inhibition Assay IC50=15.0862 μM SANGER
LS-123 Growth Inhibition Assay IC50=15.0165 μM SANGER
KALS-1 Growth Inhibition Assay IC50=15.0158 μM SANGER
BT-20 Growth Inhibition Assay IC50=14.9384 μM SANGER
GAMG Growth Inhibition Assay IC50=14.5577 μM SANGER
CAL-12T Growth Inhibition Assay IC50=14.4336 μM SANGER
ES5 Growth Inhibition Assay IC50=14.2599 μM SANGER
YAPC Growth Inhibition Assay IC50=14.2407 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=14.236 μM SANGER
CAL-72 Growth Inhibition Assay IC50=14.1906 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=13.7453 μM SANGER
NB5 Growth Inhibition Assay IC50=13.5503 μM SANGER
DEL Growth Inhibition Assay IC50=13.5503 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=13.5031 μM SANGER
CCF-STTG1 Growth Inhibition Assay IC50=13.4039 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=13.1469 μM SANGER
SW948 Growth Inhibition Assay IC50=13.013 μM SANGER
ES4 Growth Inhibition Assay IC50=12.9487 μM SANGER
OE33 Growth Inhibition Assay IC50=12.9456 μM SANGER
HT Growth Inhibition Assay IC50=12.9437 μM SANGER
LU-134-A Growth Inhibition Assay IC50=12.93 μM SANGER
HCC1806 Growth Inhibition Assay IC50=12.6952 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=12.658 μM SANGER
HAL-01 Growth Inhibition Assay IC50=12.6174 μM SANGER
8505C Growth Inhibition Assay IC50=12.612 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=12.4087 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=12.3851 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=12.3421 μM SANGER
REH Growth Inhibition Assay IC50=12.1573 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=12.1447 μM SANGER
CAL-27 Growth Inhibition Assay IC50=12.1369 μM SANGER
A172 Growth Inhibition Assay IC50=12.1207 μM SANGER
769-P Growth Inhibition Assay IC50=12.019 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=12.0139 μM SANGER
L-540 Growth Inhibition Assay IC50=11.899 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=11.8519 μM SANGER
GB-1 Growth Inhibition Assay IC50=11.7619 μM SANGER
BL-41 Growth Inhibition Assay IC50=11.7173 μM SANGER
GR-ST Growth Inhibition Assay IC50=11.6181 μM SANGER
SNU-449 Growth Inhibition Assay IC50=11.6072 μM SANGER
ES6 Growth Inhibition Assay IC50=11.576 μM SANGER
COR-L105 Growth Inhibition Assay IC50=11.3237 μM SANGER
SW626 Growth Inhibition Assay IC50=11.2889 μM SANGER
HLE Growth Inhibition Assay IC50=11.2119 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=11.1389 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=11.1209 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=11.0892 μM SANGER
EGI-1 Growth Inhibition Assay IC50=10.9455 μM SANGER
UMC-11 Growth Inhibition Assay IC50=10.9373 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=10.7068 μM SANGER
SW13 Growth Inhibition Assay IC50=10.6374 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=10.6181 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=10.5105 μM SANGER
CAS-1 Growth Inhibition Assay IC50=10.4608 μM SANGER
COLO-679 Growth Inhibition Assay IC50=10.4285 μM SANGER
YT Growth Inhibition Assay IC50=10.4001 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=10.3227 μM SANGER
LU-65 Growth Inhibition Assay IC50=10.2943 μM SANGER
SJRH30 Growth Inhibition Assay IC50=10.1844 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=10.1776 μM SANGER
RXF393 Growth Inhibition Assay IC50=10.1392 μM SANGER
EFO-21 Growth Inhibition Assay IC50=10.0093 μM SANGER
U-698-M Growth Inhibition Assay IC50=9.997 μM SANGER
NCI-H716 Growth Inhibition Assay IC50=9.93322 μM SANGER
CHP-126 Growth Inhibition Assay IC50=9.9329 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=9.84828 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=9.77984 μM SANGER
SN12C Growth Inhibition Assay IC50=9.76806 μM SANGER
SK-CO-1 Growth Inhibition Assay IC50=9.76235 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=9.75535 μM SANGER
KNS-42 Growth Inhibition Assay IC50=9.43407 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=9.39652 μM SANGER
UACC-62 Growth Inhibition Assay IC50=9.37297 μM SANGER
MFH-ino Growth Inhibition Assay IC50=9.29007 μM SANGER
HCC70 Growth Inhibition Assay IC50=9.27309 μM SANGER
Daoy Growth Inhibition Assay IC50=9.24143 μM SANGER
SF539 Growth Inhibition Assay IC50=9.21098 μM SANGER
NCI-H719 Growth Inhibition Assay IC50=9.18391 μM SANGER
DMS-273 Growth Inhibition Assay IC50=9.125 μM SANGER
HT-29 Growth Inhibition Assay IC50=9.12373 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=9.06012 μM SANGER
NH-12 Growth Inhibition Assay IC50=9.02542 μM SANGER
MKN45 Growth Inhibition Assay IC50=8.96063 μM SANGER
LoVo Growth Inhibition Assay IC50=8.95566 μM SANGER
AM-38 Growth Inhibition Assay IC50=8.80439 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=8.79772 μM SANGER
C3A Growth Inhibition Assay IC50=8.76561 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=8.73107 μM SANGER
TE-5 Growth Inhibition Assay IC50=8.70296 μM SANGER
PA-1 Growth Inhibition Assay IC50=8.66694 μM SANGER
C-33-A Growth Inhibition Assay IC50=8.61529 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=8.48595 μM SANGER
KP-4 Growth Inhibition Assay IC50=8.41853 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=8.3692 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=8.35723 μM SANGER
J82 Growth Inhibition Assay IC50=8.34124 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=8.29308 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=8.29185 μM SANGER
IPC-298 Growth Inhibition Assay IC50=8.27709 μM SANGER
MKN28 Growth Inhibition Assay IC50=8.24598 μM SANGER
GCIY Growth Inhibition Assay IC50=8.23713 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=8.06521 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=7.94553 μM SANGER
COLO-800 Growth Inhibition Assay IC50=7.90685 μM SANGER
SF268 Growth Inhibition Assay IC50=7.8356 μM SANGER
HT-1080 Growth Inhibition Assay IC50=7.78555 μM SANGER
ECC12 Growth Inhibition Assay IC50=7.72901 μM SANGER
ONS-76 Growth Inhibition Assay IC50=7.69416 μM SANGER
22RV1 Growth Inhibition Assay IC50=7.67975 μM SANGER
MLMA Growth Inhibition Assay IC50=7.54689 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=7.52272 μM SANGER
HuO9 Growth Inhibition Assay IC50=7.48794 μM SANGER
HCC1143 Growth Inhibition Assay IC50=7.37898 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=7.24024 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=7.21273 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=7.18038 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=7.16906 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=7.09791 μM SANGER
HT-3 Growth Inhibition Assay IC50=7.0349 μM SANGER
YKG-1 Growth Inhibition Assay IC50=7.02678 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=6.96315 μM SANGER
MS-1 Growth Inhibition Assay IC50=6.95192 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=6.94715 μM SANGER
GI-1 Growth Inhibition Assay IC50=6.94348 μM SANGER
MEG-01 Growth Inhibition Assay IC50=6.93546 μM SANGER
23132-87 Growth Inhibition Assay IC50=6.90901 μM SANGER
C-4-II Growth Inhibition Assay IC50=6.83117 μM SANGER
ESS-1 Growth Inhibition Assay IC50=6.76072 μM SANGER
639-V Growth Inhibition Assay IC50=6.75127 μM SANGER
TE-12 Growth Inhibition Assay IC50=6.72377 μM SANGER
Calu-6 Growth Inhibition Assay IC50=6.65435 μM SANGER
M059J Growth Inhibition Assay IC50=6.55625 μM SANGER
NCI-H838 Growth Inhibition Assay IC50=6.51703 μM SANGER
no-10 Growth Inhibition Assay IC50=6.4784 μM SANGER
SF295 Growth Inhibition Assay IC50=6.4498 μM SANGER
SCC-25 Growth Inhibition Assay IC50=6.42493 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=6.4036 μM SANGER
COLO-680N Growth Inhibition Assay IC50=6.37638 μM SANGER
COLO-824 Growth Inhibition Assay IC50=6.27868 μM SANGER
HSC-3 Growth Inhibition Assay IC50=6.17396 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=6.1516 μM SANGER
Calu-3 Growth Inhibition Assay IC50=6.14689 μM SANGER
PC-3 Growth Inhibition Assay IC50=6.13072 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=6.12497 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=6.03787 μM SANGER
HEL Growth Inhibition Assay IC50=6.02188 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=5.90148 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=5.88206 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=5.85891 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=5.79581 μM SANGER
KG-1 Growth Inhibition Assay IC50=5.74005 μM SANGER
647-V Growth Inhibition Assay IC50=5.62042 μM SANGER
TE-9 Growth Inhibition Assay IC50=5.61788 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=5.60421 μM SANGER
TE-15 Growth Inhibition Assay IC50=5.57779 μM SANGER
HCC2157 Growth Inhibition Assay IC50=5.56896 μM SANGER
HOP-62 Growth Inhibition Assay IC50=5.56887 μM SANGER
SR Growth Inhibition Assay IC50=5.53645 μM SANGER
TE-6 Growth Inhibition Assay IC50=5.44569 μM SANGER
GDM-1 Growth Inhibition Assay IC50=5.41781 μM SANGER
SF126 Growth Inhibition Assay IC50=5.41465 μM SANGER
ES8 Growth Inhibition Assay IC50=5.41409 μM SANGER
A101D Growth Inhibition Assay IC50=5.39689 μM SANGER
LC4-1 Growth Inhibition Assay IC50=5.39303 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=5.37077 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=5.30538 μM SANGER
A2058 Growth Inhibition Assay IC50=5.30438 μM SANGER
RD Growth Inhibition Assay IC50=5.29771 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=5.29218 μM SANGER
COLO-684 Growth Inhibition Assay IC50=5.25371 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=5.09139 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=5.02834 μM SANGER
U-266 Growth Inhibition Assay IC50=4.94919 μM SANGER
GOTO Growth Inhibition Assay IC50=4.79293 μM SANGER
SW780 Growth Inhibition Assay IC50=4.76849 μM SANGER
SNB75 Growth Inhibition Assay IC50=4.7466 μM SANGER
SH-4 Growth Inhibition Assay IC50=4.72633 μM SANGER
MKN1 Growth Inhibition Assay IC50=4.70665 μM SANGER
A431 Growth Inhibition Assay IC50=4.68228 μM SANGER
COR-L23 Growth Inhibition Assay IC50=4.6728 μM SANGER
OE19 Growth Inhibition Assay IC50=4.63145 μM SANGER
Calu-1 Growth Inhibition Assay IC50=4.58707 μM SANGER
L-363 Growth Inhibition Assay IC50=4.55996 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=4.55516 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=4.49701 μM SANGER
GT3TKB Growth Inhibition Assay IC50=4.48822 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=4.48532 μM SANGER
C8166 Growth Inhibition Assay IC50=4.47753 μM SANGER
SCC-9 Growth Inhibition Assay IC50=4.44299 μM SANGER
BC-3 Growth Inhibition Assay IC50=4.43477 μM SANGER
SNU-423 Growth Inhibition Assay IC50=4.42685 μM SANGER
KS-1 Growth Inhibition Assay IC50=4.42459 μM SANGER
HOS Growth Inhibition Assay IC50=4.38567 μM SANGER
A3-KAW Growth Inhibition Assay IC50=4.35552 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=4.33723 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=4.31016 μM SANGER
DV-90 Growth Inhibition Assay IC50=4.29397 μM SANGER
NCI-H1734 Growth Inhibition Assay IC50=4.26695 μM SANGER
TE-10 Growth Inhibition Assay IC50=4.22887 μM SANGER
CHL-1 Growth Inhibition Assay IC50=4.18961 μM SANGER
CA46 Growth Inhibition Assay IC50=4.16104 μM SANGER
SIMA Growth Inhibition Assay IC50=4.144 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=4.12975 μM SANGER
ATN-1 Growth Inhibition Assay IC50=4.10777 μM SANGER
HGC-27 Growth Inhibition Assay IC50=4.09549 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=4.09429 μM SANGER
G-361 Growth Inhibition Assay IC50=4.0906 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=4.08674 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=4.07861 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=4.0773 μM SANGER
NB1 Growth Inhibition Assay IC50=4.06644 μM SANGER
ACHN Growth Inhibition Assay IC50=4.0237 μM SANGER
SCC-4 Growth Inhibition Assay IC50=3.95782 μM SANGER
HCC2998 Growth Inhibition Assay IC50=3.94843 μM SANGER
A204 Growth Inhibition Assay IC50=3.90956 μM SANGER
TE-441-T Growth Inhibition Assay IC50=3.8293 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=3.81676 μM SANGER
697 Growth Inhibition Assay IC50=3.81657 μM SANGER
SUP-T1 Growth Inhibition Assay IC50=3.7832 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=3.7751 μM SANGER
SW872 Growth Inhibition Assay IC50=3.76958 μM SANGER
RL95-2 Growth Inhibition Assay IC50=3.71864 μM SANGER
SBC-5 Growth Inhibition Assay IC50=3.67882 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=3.65288 μM SANGER
RVH-421 Growth Inhibition Assay IC50=3.60311 μM SANGER
CAL-51 Growth Inhibition Assay IC50=3.57612 μM SANGER
CAL-120 Growth Inhibition Assay IC50=3.5735 μM SANGER
HCT-116 Growth Inhibition Assay IC50=3.50711 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=3.49204 μM SANGER
RS4-11 Growth Inhibition Assay IC50=3.48715 μM SANGER
EM-2 Growth Inhibition Assay IC50=3.48674 μM SANGER
H4 Growth Inhibition Assay IC50=3.47569 μM SANGER
EW-1 Growth Inhibition Assay IC50=3.40544 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=3.36352 μM SANGER
G-401 Growth Inhibition Assay IC50=3.29808 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=3.29465 μM SANGER
CTV-1 Growth Inhibition Assay IC50=3.25377 μM SANGER
HL-60 Growth Inhibition Assay IC50=3.2114 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=3.20137 μM SANGER
BHT-101 Growth Inhibition Assay IC50=3.15798 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=3.13961 μM SANGER
A2780 Growth Inhibition Assay IC50=3.10341 μM SANGER
NCI-H1963 Growth Inhibition Assay IC50=3.08825 μM SANGER
786-0 Growth Inhibition Assay IC50=3.05784 μM SANGER
EW-18 Growth Inhibition Assay IC50=3.0532 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=2.98334 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=2.98029 μM SANGER
5637 Growth Inhibition Assay IC50=2.92439 μM SANGER
OPM-2 Growth Inhibition Assay IC50=2.89978 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=2.86204 μM SANGER
IGR-1 Growth Inhibition Assay IC50=2.83987 μM SANGER
GP5d Growth Inhibition Assay IC50=2.83827 μM SANGER
G-402 Growth Inhibition Assay IC50=2.81447 μM SANGER
HSC-4 Growth Inhibition Assay IC50=2.78389 μM SANGER
SCC-15 Growth Inhibition Assay IC50=2.75252 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=2.71646 μM SANGER
TUR Growth Inhibition Assay IC50=2.65369 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=2.63879 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=2.60712 μM SANGER
HMV-II Growth Inhibition Assay IC50=2.58997 μM SANGER
LXF-289 Growth Inhibition Assay IC50=2.58273 μM SANGER
NCCIT Growth Inhibition Assay IC50=2.5724 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=2.56517 μM SANGER
SNU-387 Growth Inhibition Assay IC50=2.5282 μM SANGER
EFO-27 Growth Inhibition Assay IC50=2.51888 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=2.49572 μM SANGER
DU-145 Growth Inhibition Assay IC50=2.49118 μM SANGER
MFE-296 Growth Inhibition Assay IC50=2.47792 μM SANGER
CMK Growth Inhibition Assay IC50=2.41795 μM SANGER
CAL-39 Growth Inhibition Assay IC50=2.41628 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=2.41248 μM SANGER
BxPC-3 Growth Inhibition Assay IC50=2.35436 μM SANGER
ACN Growth Inhibition Assay IC50=2.34745 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=2.3288 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=2.32507 μM SANGER
HOP-92 Growth Inhibition Assay IC50=2.30673 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=2.28874 μM SANGER
ETK-1 Growth Inhibition Assay IC50=2.2846 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=2.26966 μM SANGER
LOUCY Growth Inhibition Assay IC50=2.26128 μM SANGER
ABC-1 Growth Inhibition Assay IC50=2.25196 μM SANGER
DU-4475 Growth Inhibition Assay IC50=2.14759 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=2.12818 μM SANGER
CHP-212 Growth Inhibition Assay IC50=2.09539 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=2.04839 μM SANGER
EW-16 Growth Inhibition Assay IC50=2.03983 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=2.00988 μM SANGER
SW954 Growth Inhibition Assay IC50=2.00151 μM SANGER
MEL-HO Growth Inhibition Assay IC50=1.97993 μM SANGER
MDA-MB-468 Growth Inhibition Assay IC50=1.91272 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=1.90315 μM SANGER
D-336MG Growth Inhibition Assay IC50=1.85614 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=1.8049 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=1.79568 μM SANGER
U251 Growth Inhibition Assay IC50=1.74031 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=1.72891 μM SANGER
ML-2 Growth Inhibition Assay IC50=1.66802 μM SANGER
BHY Growth Inhibition Assay IC50=1.65663 μM SANGER
TE-11 Growth Inhibition Assay IC50=1.63522 μM SANGER
EW-13 Growth Inhibition Assay IC50=1.63466 μM SANGER
SW1710 Growth Inhibition Assay IC50=1.62628 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=1.62312 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=1.61679 μM SANGER
BC-1 Growth Inhibition Assay IC50=1.61664 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=1.55818 μM SANGER
HSC-2 Growth Inhibition Assay IC50=1.5395 μM SANGER
ST486 Growth Inhibition Assay IC50=1.53278 μM SANGER
AGS Growth Inhibition Assay IC50=1.52124 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=1.48387 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=1.44886 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=1.44647 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=1.35236 μM SANGER
Detroit562 Growth Inhibition Assay IC50=1.35222 μM SANGER
CAL-62 Growth Inhibition Assay IC50=1.31909 μM SANGER
MES-SA Growth Inhibition Assay IC50=1.30682 μM SANGER
BPH-1 Growth Inhibition Assay IC50=1.28766 μM SANGER
NKM-1 Growth Inhibition Assay IC50=1.27506 μM SANGER
AN3-CA Growth Inhibition Assay IC50=1.21867 μM SANGER
CAL-33 Growth Inhibition Assay IC50=1.12938 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=1.10776 μM SANGER
8305C Growth Inhibition Assay IC50=1.09904 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=1.04714 μM SANGER
ALL-PO Growth Inhibition Assay IC50=1.01584 μM SANGER
BCPAP Growth Inhibition Assay IC50=1.01288 μM SANGER
RT-112 Growth Inhibition Assay IC50=0.9846 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=0.83154 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=0.81038 μM SANGER
MG-63 Growth Inhibition Assay IC50=0.80637 μM SANGER
COLO-829 Growth Inhibition Assay IC50=0.75176 μM SANGER
COLO-205 Growth Inhibition Assay IC50=0.48658 μM SANGER
KM12 Growth Inhibition Assay IC50=0.38557 μM SANGER
SW982 Growth Inhibition Assay IC50=0.3282 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=0.2766 μM SANGER
sf9 Function assay Reversible/competitive inhibition of NH2-terminal His6-tagged FAK kinase domain (410 to 689 residues) (unknown origin) expressed in baculovirus infected sf9 cells using p(Glu/Tyr) as substrate in presence of ATP, IC50 = 0.0015 μM. 27876318
sf21 Function assay Inhibition of full length recombinant human N-terminal His6-tagged PYK2 expressed in baculovirus infected sf21 cells, IC50 = 0.013 μM. 27876318
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
wild type fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
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Informations chimiques, stockage et stabilité

Poids moléculaire 507.49 Formule

C21H20F3N7O3S

Stockage (À partir de la date de réception)
N° CAS 717907-75-0 Télécharger le SDF Stockage des solutions mères

Synonymes PF-00562271 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

Solubilité

In vitro
Lot:

DMSO : 100 mg/mL (197.04 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL

Calculateur de molarité

Masse Concentration Volume Poids moléculaire
Calculateur de dilution Calculateur de poids moléculaire

In vivo
Lot:

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

mg/kg g μL

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH2O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC50/Ki
FAK
(Cell-free assay)
1.5 nM
PYK2
(Cell-free assay)
13 nM
CDK2/CyclinE
(Cell-free assay)
30 nM
CDK3/CyclinE
(Cell-free assay)
47 nM
CDK1/CyclinB
(Cell-free assay)
58 nM
CDK7/CyclinH/MAT1
(Cell-free assay)
97 nM
FLT3
(Cell-free assay)
97 nM
GSK-3α
(Cell-free assay)
101 nM
CDK5/p35
(Cell-free assay)
120 nM
GSK-3β
(Cell-free assay)
133 nM
Aurora A
(Cell-free assay)
145 nM
In vitro

Le PF-562271 se lie dans la fente de liaison à l'ATP de FAK, formant deux des trois liaisons H "canoniques" entre l'inhibiteur et les atomes de la chaîne principale dans la région de la charnière de la kinase. Ce composé est puissant dans un essai basé sur des cellules inductibles mesurant le phospho-FAK avec un IC50 de 5 nM. Il (3,3 A.M.) entraîne un arrêt en G1 des cellules PC3-M.

Ce produit chimique (1 nM) bloque l'angiogenèse des vaisseaux sanguins stimulée par le bFGF, telle que réalisée dans des essais sur membrane chorioallantoïque de poulet. Il bloque puissamment la germination des vaisseaux sanguins sans changements détectables de la fuite vasculaire.

Il (250 nM) entraîne une inhibition complète de l'invasion collective des cellules A431 dans les gels de collagène.

Kinase Assay
Essai kinase recombinant
Le domaine kinase FAK purifié-activé (410-689 aa) est mis à réagir avec 50 A.M. d'ATP et 10 A.G. par puits d'un polymère peptidique aléatoire de Glu et Tyr, p(Glu/Tyr), dans un tampon kinase [50 A.M. HEPES (pH 7,5), 125 A.M. NaCl, et 48 A.M. MgCl2 pendant 15 min. La phosphorylation de p(Glu/Tyr) est contestée avec un composé dilué en série à des concentrations de 1/2-Log en commençant par une concentration maximale de 1 A.M. Chaque concentration est testée en triple. La phosphorylation de p(Glu/Tyr) est détectée avec un anticorps antiphospho-tyrosine général (PY20) suivi d'un anticorps de chèvre anti-souris IgG conjugué à la peroxydase de raifort (HRP). Le substrat HRP est ajouté, et les lectures d'absorbance à 450 nm sont obtenues après l'ajout d'une solution d'arrêt (2 mol/L H2SO4). Les valeurs d'IC50 sont déterminées à l'aide du modèle Hill-Slope.
In vivo

Le PF-562271 (< 33 mg/kg p.o.) inhibe la phosphorylation de FAK dans les tumeurs de manière dose- et temps-dépendante chez des souris porteuses de tumeurs U87MG. Ce composé (50 mg/kg p.o. bid) entraîne 86 % d'inhibition de la croissance tumorale chez des souris xénogreffées BxPc3 et 45 % d'inhibition de la croissance tumorale chez des souris xénogreffées PC3-M. Il (25 mg/kg, bid) entraîne une apoptose 2 fois plus importante dans les tumeurs traitées chez des souris porteuses de xénogreffes pulmonaires H125.

Ce produit chimique (33 mg/kg, p.o.) inhibe le mouvement étendu des cellules tumorales pendant 24 heures chez des souris. Il (33 mg/kg, p.o.) entraîne des dynamiques altérées de la E-cadhérine chez des souris, ce qui est corrélé à un mouvement collectif des cellules dépendant de la E-cadhérine réduit.

Ce composé (25 mg/kg, p.o. bid) entraîne 62 % d'inhibition de la croissance tumorale dans le modèle murin de xénogreffe par implant local sous-cutané PC3M-luc-C6.

Il (5 mg/kg, oral) entraîne des augmentations significatives et similaires de l'ostéocalcine et des paramètres de l'os spongieux et une diminution de la croissance tumorale et des signes de guérison osseuse chez des rats implantés avec des cellules MDA-MB-231 dans le tibia.

Références
  • [4] https://pubmed.ncbi.nlm.nih.gov/20495381/
  • [5] https://pubmed.ncbi.nlm.nih.gov/18348298/

Applications

Méthodes Biomarqueurs Images PMID
Western blot p-FAK / FAK / p-Talin / Talin p-Src / Src / p-paxillin / Paxillin / ICAM-1
S2890-WB1
26530902
Immunofluorescence p-FAK
S2890-IF1
26530902
Growth inhibition assay Cell viability
S2890-viability1
28953264

Support technique

Instructions de manipulation

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