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PF-562271 (VS-6062) FAK/Pyk2 억제제

제품 번호S2890

PF-562271 (PF-00562271)은 세포 자유 분석에서 1.5 nM의 IC50을 갖는 FAK의 강력한 ATP 경쟁적, 가역적 억제제이며, Pyk2에 대해서는 FAK보다 약 10배 덜 강력하고 일부 CDKs를 제외한 다른 단백질 키나제에 대해서는 100배 이상의 선택성을 보입니다.
PF-562271 (VS-6062) FAK 억제제 Chemical Structure

화학 구조

분자량: 507.49

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품질 관리

배치: 순도: 99.95%
99.95

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 507.49 화학식

C21H20F3N7O3S

보관 (수령일로부터)
CAS 번호 717907-75-0 SDF 다운로드 원액 보관

동의어 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

용해도

In vitro
배치:

DMSO : 100 mg/mL (197.04 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

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
시험관 내(In vitro)

PF-562271은 FAK의 ATP 결합 틈새에 결합하여 억제제와 키나제 힌지 영역의 주쇄 원자 사이에 세 개의 "정규" 수소 결합 중 두 개를 형성합니다. 이 화합물은 포스포-FAK를 5 nM의 IC50으로 측정하는 유도 가능한 세포 기반 분석에서 강력합니다. 이 화합물(3.3 µM)은 PC3-M 세포의 G1기 정지를 유발합니다.

이 화학물질(1 nM)은 닭 코리오알란토막 분석에서 수행된 bFGF-자극 혈관 Angiogenesis를 차단합니다. 이는 혈관 누출의 감지 가능한 변화 없이 강력하게 혈관 맹출을 차단합니다.

이 화합물(250 nM)은 콜라겐 겔로의 A431 세포 집단 침윤을 완전히 억제합니다.

키나아제 분석
재조합 키나제 분석
정제된 활성 FAK 키나제 도메인(410–689 aa)을 50 μM ATP와 10 μg/웰의 Glu 및 Tyr 무작위 펩타이드 중합체, p(Glu/Tyr)과 함께 키나제 버퍼 [50 mM HEPES (pH 7.5), 125 mM NaCl, 48 mM MgCl2]에서 15분 동안 반응시켰습니다. p(Glu/Tyr)의 인산화는 1 μM의 최고 농도부터 시작하여 1/2-Log 농도로 연속 희석된 화합물로 도전되었습니다. 각 농도는 삼중으로 테스트되었습니다. p(Glu/Tyr)의 인산화는 일반적인 항포스포-티로신(PY20) 항체와 이어서 고추냉이 과산화효소(HRP) 접합 염소 항마우스 IgG 항체를 사용하여 검출되었습니다. HRP 기질을 첨가하고 정지 용액(2 mol/L H2SO4) 첨가 후 450 nm에서 흡광도 측정을 얻었습니다. IC50 값은 Hill-Slope 모델을 사용하여 결정되었습니다.
생체 내(In vivo)

PF-562271 (< 33 mg/kg p.o.)은 U87MG를 이식한 쥐에서 용량 및 시간 의존적으로 종양 내 FAK 인산화를 억제합니다. 이 화합물(50 mg/kg p.o. bid)은 BxPc3 이종이식 쥐에서 86%의 종양 성장 억제를, PC3-M 이종이식 쥐에서는 45%의 종양 성장 억제를 유발합니다. 이 화합물(25 mg/kg, bid)은 H125 폐 이종이식을 이식한 쥐의 치료된 종양에서 2배 더 많은 세포자멸사를 유발합니다.

이 화학물질(33 mg/kg, p.o.)은 쥐에서 24시간 동안 종양 세포의 광범위한 이동을 억제합니다. 이 화합물(33 mg/kg, p.o.)은 쥐에서 E-카드헤린 역학의 변화를 유발하며, 이는 E-카드헤린 의존적 집단 세포 이동 감소와 상관관계가 있습니다.

이 화합물(25 mg/kg, p.o. bid)은 PC3M-luc-C6 피하 국소 이식 이종이식 쥐 모델에서 62%의 종양 성장 억제를 유발합니다.

이 화합물(5 mg/kg, 경구)은 정강이에 MDA-MB-231 세포를 이식한 쥐에서 오스테오칼신과 해면골 매개변수의 유의미하고 유사한 증가와 종양 성장 감소 및 뼈 치유 징후를 유발합니다.

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

적용 분야

방법 바이오마커 이미지 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

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