- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- 化合物ライブラリー
- 抗体
- 新製品
- お問い合わせ
PF-562271
別名：PF-00562271
PF-562271 (PF-00562271) 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.
CAS No. 717907-75-0
文献中Selleckの製品使用例（120）
製品安全説明書
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純度：
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PF-562271関連製品
シグナル伝達経路
FAK阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| A172 | Growth Inhibition Assay | IC50=12.1207 μM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=12.1369 μM | SANGER | ||
| NCI-H1437 | Growth Inhibition Assay | IC50=12.1447 μM | SANGER | ||
| REH | Growth Inhibition Assay | IC50=12.1573 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=12.3421 μM | SANGER | ||
| NCI-H1792 | Growth Inhibition Assay | IC50=12.3851 μM | SANGER | ||
| SK-MM-2 | Growth Inhibition Assay | IC50=12.4087 μM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=12.612 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=12.6174 μM | SANGER | ||
| NCI-H2141 | Growth Inhibition Assay | IC50=12.658 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=12.6952 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=12.93 μM | SANGER | ||
| HT | Growth Inhibition Assay | IC50=12.9437 μM | SANGER | ||
| OE33 | Growth Inhibition Assay | IC50=12.9456 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=12.9487 μM | SANGER | ||
| SW948 | Growth Inhibition Assay | IC50=13.013 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=13.1469 μM | SANGER | ||
| CCF-STTG1 | Growth Inhibition Assay | IC50=13.4039 μM | SANGER | ||
| RPMI-8402 | Growth Inhibition Assay | IC50=13.5031 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=13.5503 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=13.5503 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=13.7453 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=14.1906 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=14.236 μM | SANGER | ||
| YAPC | Growth Inhibition Assay | IC50=14.2407 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=14.2599 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=14.4336 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=14.5577 μM | SANGER | ||
| BT-20 | Growth Inhibition Assay | IC50=14.9384 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=15.0158 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=15.0165 μM | SANGER | ||
| LK-2 | Growth Inhibition Assay | IC50=15.0862 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=15.2868 μM | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=15.4163 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=15.6941 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=15.8926 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=15.9497 μM | SANGER | ||
| NCI-H2405 | Growth Inhibition Assay | IC50=16.2218 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=16.3742 μM | SANGER | ||
| THP-1 | Growth Inhibition Assay | IC50=16.4665 μM | SANGER | ||
| LB373-MEL-D | Growth Inhibition Assay | IC50=16.6138 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=16.9219 μM | SANGER | ||
| EB2 | Growth Inhibition Assay | IC50=17.7426 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=17.7936 μM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=17.825 μM | SANGER | ||
| CESS | Growth Inhibition Assay | IC50=17.9326 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=17.9958 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=18.0669 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=18.2062 μM | SANGER | ||
| NCI-H226 | Growth Inhibition Assay | IC50=18.8299 μM | SANGER | ||
| NCI-H748 | Growth Inhibition Assay | IC50=18.8585 μM | SANGER | ||
| NCI-H1299 | Growth Inhibition Assay | IC50=18.8918 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=19.1754 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=19.1796 μM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=19.2029 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=19.2155 μM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=19.2219 μM | SANGER | ||
| NCI-H524 | Growth Inhibition Assay | IC50=19.5725 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=19.5944 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=19.6268 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=20.1577 μM | SANGER | ||
| EW-7 | Growth Inhibition Assay | IC50=20.1628 μM | SANGER | ||
| Raji | Growth Inhibition Assay | IC50=20.2568 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=20.3953 μM | SANGER | ||
| PANC-10-05 | Growth Inhibition Assay | IC50=20.4613 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=20.5814 μM | SANGER | ||
| MFE-280 | Growth Inhibition Assay | IC50=21.3188 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=21.3202 μM | SANGER | ||
| KMOE-2 | Growth Inhibition Assay | IC50=21.3288 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=21.3893 μM | SANGER | ||
| NCI-H64 | Growth Inhibition Assay | IC50=21.4756 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=21.4971 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=21.5094 μM | SANGER | ||
| COLO-792 | Growth Inhibition Assay | IC50=21.5827 μM | SANGER | ||
| PFSK-1 | Growth Inhibition Assay | IC50=21.6837 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=21.7687 μM | SANGER | ||
| NCI-H1882 | Growth Inhibition Assay | IC50=21.8596 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=21.8631 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=21.9688 μM | SANGER | ||
| NCI-H1694 | Growth Inhibition Assay | IC50=21.9863 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=22.0367 μM | SANGER | ||
| NCI-H2122 | Growth Inhibition Assay | IC50=22.1677 μM | SANGER | ||
| IMR-5 | Growth Inhibition Assay | IC50=22.287 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=22.6746 μM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=22.8177 μM | SANGER | ||
| NCI-H727 | Growth Inhibition Assay | IC50=22.8836 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=23.0646 μM | SANGER | ||
| RO82-W-1 | Growth Inhibition Assay | IC50=23.2511 μM | SANGER | ||
| SKG-IIIa | Growth Inhibition Assay | IC50=23.3546 μM | SANGER | ||
| MC-CAR | Growth Inhibition Assay | IC50=23.5183 μM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=23.6093 μM | SANGER | ||
| PC-14 | Growth Inhibition Assay | IC50=23.6623 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=23.7461 μM | SANGER | ||
| EFM-19 | Growth Inhibition Assay | IC50=24.1844 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=24.4977 μM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=24.5217 μM | SANGER | ||
| SW1990 | Growth Inhibition Assay | IC50=24.5883 μM | SANGER | ||
| SW684 | Growth Inhibition Assay | IC50=24.7624 μM | SANGER | ||
| Ca-Ski | Growth Inhibition Assay | IC50=24.9237 μM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=25.2337 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=25.357 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=25.4743 μM | SANGER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=25.7459 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition Assay | IC50=25.7501 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=25.9901 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=26.5152 μM | SANGER | ||
| Daudi | Growth Inhibition Assay | IC50=26.5158 μM | SANGER | ||
| U-87-MG | Growth Inhibition Assay | IC50=26.5305 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=26.5406 μM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=26.5553 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=26.9086 μM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=27.0271 μM | SANGER | ||
| LU-99A | Growth Inhibition Assay | IC50=27.1754 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=27.1973 μM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=27.5548 μM | SANGER | ||
| SNU-C1 | Growth Inhibition Assay | IC50=27.6491 μM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=27.6975 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=28.0495 μM | SANGER | ||
| T-24 | Growth Inhibition Assay | IC50=28.1925 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=28.2459 μM | SANGER | ||
| NCI-H1651 | Growth Inhibition Assay | IC50=28.2592 μM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=28.3171 μM | SANGER | ||
| NY | Growth Inhibition Assay | IC50=28.6579 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=28.8708 μM | SANGER | ||
| KLE | Growth Inhibition Assay | IC50=28.9906 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=29.012 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=29.2167 μM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=29.5466 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=29.6046 μM | SANGER | ||
| A673 | Growth Inhibition Assay | IC50=29.732 μM | SANGER | ||
| HEC-1 | Growth Inhibition Assay | IC50=30.0053 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=30.1475 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=30.2477 μM | SANGER | ||
| OVCAR-8 | Growth Inhibition Assay | IC50=30.6794 μM | SANGER | ||
| NCI-H630 | Growth Inhibition Assay | IC50=30.8953 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=31.0424 μM | SANGER | ||
| NCI-H596 | Growth Inhibition Assay | IC50=31.0621 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=31.112 μM | SANGER | ||
| KYSE-70 | Growth Inhibition Assay | IC50=31.3008 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=31.4992 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=31.5625 μM | SANGER | ||
| SW620 | Growth Inhibition Assay | IC50=31.6283 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=31.7306 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=32.1386 μM | SANGER | ||
| SW48 | Growth Inhibition Assay | IC50=32.3825 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=32.6163 μM | SANGER | ||
| LU-165 | Growth Inhibition Assay | IC50=33.008 μM | SANGER | ||
| EHEB | Growth Inhibition Assay | IC50=33.0494 μM | SANGER | ||
| NCI-H441 | Growth Inhibition Assay | IC50=33.2235 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=33.3679 μM | SANGER | ||
| MC-IXC | Growth Inhibition Assay | IC50=33.5655 μM | SANGER | ||
| NCI-H522 | Growth Inhibition Assay | IC50=33.654 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=33.6746 μM | SANGER | ||
| NCI-H1417 | Growth Inhibition Assay | IC50=33.9585 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=35.2185 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=35.4024 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=35.4141 μM | SANGER | ||
| EFE-184 | Growth Inhibition Assay | IC50=35.6829 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=35.7718 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=35.8264 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=36.4924 μM | SANGER | ||
| SW1463 | Growth Inhibition Assay | IC50=36.6566 μM | SANGER | ||
| KYSE-140 | Growth Inhibition Assay | IC50=36.7298 μM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=36.8536 μM | SANGER | ||
| HCC1937 | Growth Inhibition Assay | IC50=37.0154 μM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=37.1903 μM | SANGER | ||
| KARPAS-422 | Growth Inhibition Assay | IC50=37.4431 μM | SANGER | ||
| RCM-1 | Growth Inhibition Assay | IC50=37.5358 μM | SANGER | ||
| A375 | Growth Inhibition Assay | IC50=37.7647 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=38.0239 μM | SANGER | ||
| MDA-MB-453 | Growth Inhibition Assay | IC50=39.0218 μM | SANGER | ||
| Capan-2 | Growth Inhibition Assay | IC50=39.0509 μM | SANGER | ||
| SW756 | Growth Inhibition Assay | IC50=39.5091 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=39.6282 μM | SANGER | ||
| NCI-H2170 | Growth Inhibition Assay | IC50=39.9977 μM | SANGER | ||
| COLO-678 | Growth Inhibition Assay | IC50=40.595 μM | SANGER | ||
| PF-382 | Growth Inhibition Assay | IC50=40.7487 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=42.2942 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=42.8008 μM | SANGER | ||
| SAS | Growth Inhibition Assay | IC50=43.4288 μM | SANGER | ||
| MRK-nu-1 | Growth Inhibition Assay | IC50=44.7414 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=44.9136 μM | SANGER | ||
| NCI-H2342 | Growth Inhibition Assay | IC50=45.1117 μM | SANGER | ||
| NCI-H1703 | Growth Inhibition Assay | IC50=46.0592 μM | SANGER | ||
| NCI-H187 | Growth Inhibition Assay | IC50=46.1869 μM | SANGER | ||
| CP66-MEL | Growth Inhibition Assay | IC50=46.2789 μM | SANGER | ||
| HCC1569 | Growth Inhibition Assay | IC50=46.5917 μM | SANGER | ||
| BL-70 | Growth Inhibition Assay | IC50=46.7737 μM | SANGER | ||
| Saos-2 | Growth Inhibition Assay | IC50=47.3123 μM | SANGER | ||
| LC-1F | Growth Inhibition Assay | IC50=47.6105 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=47.6434 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=48.1401 μM | SANGER | ||
| RT4 | Growth Inhibition Assay | IC50=48.8377 μM | SANGER | ||
| LS-1034 | Growth Inhibition Assay | IC50=48.8954 μM | SANGER | ||
| NCI-H1395 | Growth Inhibition Assay | IC50=49.0492 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=49.6731 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=49.8944 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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生物活性
| 製品説明 | PF-562271 (PF-00562271) 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 |
|
| In Vitro | ||||
| 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] |
|||
|---|---|---|---|---|
| Kinase Assay | Recombinant kinase assay | |||
| Purified-activated FAK kinase domain (410–689 aa) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl2 for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2 mol/L H2SO4). IC50 values are determined using the Hill-Slope Model. | ||||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | p-Src / Src / p-paxillin / Paxillin / ICAM-1 p-FAK / FAK / p-Talin / Talin |
|
29417941 | |
| Immunofluorescence | p-FAK |
|
26530902 | |
| Growth inhibition assay | Cell viability |
|
28953264 | |
| In Vivo | ||
| 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] |
|
|---|---|---|
| 動物実験 | 動物モデル | Athymic female mice bearing BxPc3 or PC3-M xenografts. |
| 投与量 | 50 mg/kg | |
| 投与経路 | Oral gavage | |
化学情報
| 分子量 | 507.49 | 化学式 | C21H20F3N7O3S |
| CAS No. | 717907-75-0 | SDF | Download PF-562271 SDFをダウンロードする |
| 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 | ||
| 保管 | |||
|
In vitro |
DMSO : 100 mg/mL ( (197.04 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : ˂1 mg/mL Ethanol : ˂1 mg/mL |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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