endast för forskning
Kat.nr.: S7565
Kemisk struktur
| Relaterade mål | EGFR VEGFR JAK FGFR PDGFR HIF HER2 FLT3 FLT Bcr-Abl |
|---|---|
| Övrigt Src Inhibitorer | Saracatinib (AZD0530) PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 UM-164 Tolimidone (MLR-1023) 1-Naphthyl PP1(1-NA-PP1) RK 24466 eCF506 |
| Cellinjer | Analystyp | Koncentration | Inkubationstid | Formulering | Aktivitetsbeskrivning | PMID |
|---|---|---|---|---|---|---|
| EM-2 | Growth inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay, IC50=0μM | SANGER | |||
| LAMA-84 | Growth inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=0.0000038μM | SANGER | |||
| EoL-1-cell | Growth inhibition assay | Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=0.0000095μM | SANGER | |||
| MEG-01 | Growth inhibition assay | Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=0.0000163μM | SANGER | |||
| CTV-1 | Growth inhibition assay | Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=0.0000318μM | SANGER | |||
| BL-70 | Growth inhibition assay | Inhibition of human BL-70 cell growth in a cell viability assay, IC50=0.0000472μM | SANGER | |||
| K-562 | Growth inhibition assay | Inhibition of human K-562 cell growth in a cell viability assay, IC50=0.0001617μM | SANGER | |||
| BV-173 | Growth inhibition assay | Inhibition of human BV-173 cell growth in a cell viability assay, IC50=0.0005143μM | SANGER | |||
| DOHH-2 | Growth inhibition assay | Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=0.0005969μM | SANGER | |||
| A704 | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay, IC50=0.001268μM | SANGER | |||
| NCI-SNU-16 | Growth inhibition assay | Inhibition of human NCI-SNU-16 cell growth in a cell viability assay, IC50=0.01572μM | SANGER | |||
| LC-2-ad | Growth inhibition assay | Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=0.02033μM | SANGER | |||
| LB2518-MEL | Growth inhibition assay | Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=0.04667μM | SANGER | |||
| D-336MG | Growth inhibition assay | Inhibition of human D-336MG cell growth in a cell viability assay, IC50=0.04681μM | SANGER | |||
| LB996-RCC | Growth inhibition assay | Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=0.05668μM | SANGER | |||
| Becker | Growth inhibition assay | Inhibition of human Becker cell growth in a cell viability assay, IC50=0.06381μM | SANGER | |||
| LB1047-RCC | Growth inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=0.07592μM | SANGER | |||
| KS-1 | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay, IC50=0.07758μM | SANGER | |||
| MPP-89 | Growth inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=0.08229μM | SANGER | |||
| RXF393 | Growth inhibition assay | Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.10633μM | SANGER | |||
| LB831-BLC | Growth inhibition assay | Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=0.12715μM | SANGER | |||
| HUTU-80 | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=0.17529μM | SANGER | |||
| A498 | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50=0.18945μM | SANGER | |||
| MZ1-PC | Growth inhibition assay | Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=0.22716μM | SANGER | |||
| TE-8 | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay, IC50=0.23924μM | SANGER | |||
| MFH-ino | Growth inhibition assay | Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=0.23925μM | SANGER | |||
| TE-15 | Growth inhibition assay | Inhibition of human TE-15 cell growth in a cell viability assay, IC50=0.24276μM | SANGER | |||
| NTERA-S-cl-D1 | Growth inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=0.28855μM | SANGER | |||
| COLO-829 | Growth inhibition assay | Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=0.31212μM | SANGER | |||
| SW684 | Growth inhibition assay | Inhibition of human SW684 cell growth in a cell viability assay, IC50=0.32588μM | SANGER | |||
| OS-RC-2 | Growth inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=0.35011μM | SANGER | |||
| IST-MES1 | Growth inhibition assay | Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50=0.35723μM | SANGER | |||
| SNB75 | Growth inhibition assay | Inhibition of human SNB75 cell growth in a cell viability assay, IC50=0.35774μM | SANGER | |||
| SW954 | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50=0.37163μM | SANGER | |||
| RCC10RGB | Growth inhibition assay | Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=0.42631μM | SANGER | |||
| VA-ES-BJ | Growth inhibition assay | Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=0.46261μM | SANGER | |||
| NCI-H1648 | Growth inhibition assay | Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.51582μM | SANGER | |||
| PF-382 | Growth inhibition assay | Inhibition of human PF-382 cell growth in a cell viability assay, IC50=0.70763μM | SANGER | |||
| Daudi | Growth inhibition assay | Inhibition of human Daudi cell growth in a cell viability assay, IC50=0.71411μM | SANGER | |||
| SW982 | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.85819μM | SANGER | |||
| SW872 | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay, IC50=0.86458μM | SANGER | |||
| TE-12 | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay, IC50=0.88831μM | SANGER | |||
| HOP-62 | Growth inhibition assay | Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.91599μM | SANGER | |||
| NOS-1 | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=0.95045μM | SANGER | |||
| BL-41 | Growth inhibition assay | Inhibition of human BL-41 cell growth in a cell viability assay, IC50=1.00013μM | SANGER | |||
| TGBC24TKB | Growth inhibition assay | Inhibition of human TGBC24TKB cell growth in a cell viability assay, IC50=1.03831μM | SANGER | |||
| KGN | Growth inhibition assay | Inhibition of human KGN cell growth in a cell viability assay, IC50=1.0521μM | SANGER | |||
| TK10 | Growth inhibition assay | Inhibition of human TK10 cell growth in a cell viability assay, IC50=1.08418μM | SANGER | |||
| GB-1 | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay, IC50=1.16064μM | SANGER | |||
| GCIY | Growth inhibition assay | Inhibition of human GCIY cell growth in a cell viability assay, IC50=1.2301μM | SANGER | |||
| LXF-289 | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.27256μM | SANGER | |||
| RL95-2 | Growth inhibition assay | Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=1.32436μM | SANGER | |||
| SW962 | Growth inhibition assay | Inhibition of human SW962 cell growth in a cell viability assay, IC50=1.33742μM | SANGER | |||
| HT-144 | Growth inhibition assay | Inhibition of human HT-144 cell growth in a cell viability assay, IC50=1.44517μM | SANGER | |||
| IST-SL2 | Growth inhibition assay | Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=1.47421μM | SANGER | |||
| NB6 | Growth inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay, IC50=1.69698μM | SANGER | |||
| SF126 | Growth inhibition assay | Inhibition of human SF126 cell growth in a cell viability assay, IC50=1.73178μM | SANGER | |||
| BOKU | Growth inhibition assay | Inhibition of human BOKU cell growth in a cell viability assay, IC50=1.80527μM | SANGER | |||
| BB30-HNC | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=1.85472μM | SANGER | |||
| KLE | Growth inhibition assay | Inhibition of human KLE cell growth in a cell viability assay, IC50=1.86232μM | SANGER | |||
| MLMA | Growth inhibition assay | Inhibition of human MLMA cell growth in a cell viability assay, IC50=1.9231μM | SANGER | |||
| KINGS-1 | Growth inhibition assay | Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50=1.96897μM | SANGER | |||
| ES6 | Growth inhibition assay | Inhibition of human ES6 cell growth in a cell viability assay, IC50=2.05401μM | SANGER | |||
| SH-4 | Growth inhibition assay | Inhibition of human SH-4 cell growth in a cell viability assay, IC50=2.12055μM | SANGER | |||
| EB-3 | Growth inhibition assay | Inhibition of human EB-3 cell growth in a cell viability assay, IC50=2.15824μM | SANGER | |||
| KURAMOCHI | Growth inhibition assay | Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=2.24236μM | SANGER | |||
| D-263MG | Growth inhibition assay | Inhibition of human D-263MG cell growth in a cell viability assay, IC50=2.28853μM | SANGER | |||
| SF268 | Growth inhibition assay | Inhibition of human SF268 cell growth in a cell viability assay, IC50=2.48682μM | SANGER | |||
| NB17 | Growth inhibition assay | Inhibition of human NB17 cell growth in a cell viability assay, IC50=2.62875μM | SANGER | |||
| DMS-114 | Growth inhibition assay | Inhibition of human DMS-114 cell growth in a cell viability assay, IC50=2.79022μM | SANGER | |||
| MC116 | Growth inhibition assay | Inhibition of human MC116 cell growth in a cell viability assay, IC50=2.85704μM | SANGER | |||
| MZ2-MEL | Growth inhibition assay | Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=3.08643μM | SANGER | |||
| GI-ME-N | Growth inhibition assay | Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=3.25166μM | SANGER | |||
| 697 | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay, IC50=3.39644μM | SANGER | |||
| ACN | Growth inhibition assay | Inhibition of human ACN cell growth in a cell viability assay, IC50=4.22607μM | SANGER | |||
| TE-10 | Growth inhibition assay | Inhibition of human TE-10 cell growth in a cell viability assay, IC50=4.2795μM | SANGER | |||
| LS-123 | Growth inhibition assay | Inhibition of human LS-123 cell growth in a cell viability assay, IC50=4.35584μM | SANGER | |||
| TE-9 | Growth inhibition assay | Inhibition of human TE-9 cell growth in a cell viability assay, IC50=4.39183μM | SANGER | |||
| CAS-1 | Growth inhibition assay | Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=4.4023μM | SANGER | |||
| BB65-RCC | Growth inhibition assay | Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=4.69952μM | SANGER | |||
| MRK-nu-1 | Growth inhibition assay | Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=4.71792μM | SANGER | |||
| NCI-H1355 | Growth inhibition assay | Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=4.87685μM | SANGER | |||
| KP-N-YS | Growth inhibition assay | Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50=4.92086μM | SANGER | |||
| MZ7-mel | Growth inhibition assay | Inhibition of human MZ7-mel cell growth in a cell viability assay, IC50=5.09269μM | SANGER | |||
| NCI-H747 | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=5.74159μM | SANGER | |||
| C2BBe1 | Growth inhibition assay | Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50=5.78469μM | SANGER | |||
| RPMI-6666 | Growth inhibition assay | Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=5.9621μM | SANGER | |||
| PSN1 | Growth inhibition assay | Inhibition of human PSN1 cell growth in a cell viability assay, IC50=6.16376μM | SANGER | |||
| TE-1 | Growth inhibition assay | Inhibition of human TE-1 cell growth in a cell viability assay, IC50=6.71768μM | SANGER | |||
| ETK-1 | Growth inhibition assay | Inhibition of human ETK-1 cell growth in a cell viability assay, IC50=7.6356μM | SANGER | |||
| ST486 | Growth inhibition assay | Inhibition of human ST486 cell growth in a cell viability assay, IC50=8.27227μM | SANGER | |||
| KU812 | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay, IC50=8.38738μM | SANGER | |||
| EHEB | Growth inhibition assay | Inhibition of human EHEB cell growth in a cell viability assay, IC50=9.0509μM | SANGER | |||
| IMR-5 | Growth inhibition assay | Inhibition of human IMR-5 cell growth in a cell viability assay, IC50=9.28459μM | SANGER | |||
| BB49-HNC | Growth inhibition assay | Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=9.96548μM | SANGER | |||
| NCI-H1581 | Growth inhibition assay | Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=10.3373μM | SANGER | |||
| CP66-MEL | Growth inhibition assay | Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=10.6469μM | SANGER | |||
| NMC-G1 | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=11.0324μM | SANGER | |||
| SIMA | Growth inhibition assay | Inhibition of human SIMA cell growth in a cell viability assay, IC50=11.2916μM | SANGER | |||
| A101D | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay, IC50=11.8487μM | SANGER | |||
| IST-MEL1 | Growth inhibition assay | Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=12.5986μM | SANGER | |||
| no-10 | Growth inhibition assay | Inhibition of human no-10 cell growth in a cell viability assay, IC50=13.1434μM | SANGER | |||
| KALS-1 | Growth inhibition assay | Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=13.16μM | SANGER | |||
| GI-1 | Growth inhibition assay | Inhibition of human GI-1 cell growth in a cell viability assay, IC50=13.2491μM | SANGER | |||
| ONS-76 | Growth inhibition assay | Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=13.3728μM | SANGER | |||
| D-247MG | Growth inhibition assay | Inhibition of human D-247MG cell growth in a cell viability assay, IC50=13.7709μM | SANGER | |||
| NCI-H446 | Growth inhibition assay | Inhibition of human NCI-H446 cell growth in a cell viability assay, IC50=14.1409μM | SANGER | |||
| NALM-6 | Growth inhibition assay | Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=14.2358μM | SANGER | |||
| SK-N-DZ | Growth inhibition assay | Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=14.442μM | SANGER | |||
| QIMR-WIL | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=14.5247μM | SANGER | |||
| MHH-NB-11 | Growth inhibition assay | Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50=14.6569μM | SANGER | |||
| A388 | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay, IC50=14.6758μM | SANGER | |||
| EVSA-T | Growth inhibition assay | Inhibition of human EVSA-T cell growth in a cell viability assay, IC50=15.2484μM | SANGER | |||
| JVM-2 | Growth inhibition assay | Inhibition of human JVM-2 cell growth in a cell viability assay, IC50=16.4704μM | SANGER | |||
| EW-16 | Growth inhibition assay | Inhibition of human EW-16 cell growth in a cell viability assay, IC50=17.7718μM | SANGER | |||
| CP67-MEL | Growth inhibition assay | Inhibition of human CP67-MEL cell growth in a cell viability assay, IC50=18.5863μM | SANGER | |||
| NB13 | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay, IC50=19.0437μM | SANGER | |||
| NCCIT | Growth inhibition assay | Inhibition of human NCCIT cell growth in a cell viability assay, IC50=20.0093μM | SANGER | |||
| SNU-C2B | Growth inhibition assay | Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=20.5124μM | SANGER | |||
| SK-NEP-1 | Growth inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=22.2335μM | SANGER | |||
| TE-6 | Growth inhibition assay | Inhibition of human TE-6 cell growth in a cell viability assay, IC50=22.3864μM | SANGER | |||
| HCE-4 | Growth inhibition assay | Inhibition of human HCE-4 cell growth in a cell viability assay, IC50=22.927μM | SANGER | |||
| TGBC1TKB | Growth inhibition assay | Inhibition of human TGBC1TKB cell growth in a cell viability assay, IC50=23.3177μM | SANGER | |||
| L-540 | Growth inhibition assay | Inhibition of human L-540 cell growth in a cell viability assay, IC50=23.3231μM | SANGER | |||
| 8-MG-BA | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=23.9588μM | SANGER | |||
| OPM-2 | Growth inhibition assay | Inhibition of human OPM-2 cell growth in a cell viability assay, IC50=25.106μM | SANGER | |||
| MHH-PREB-1 | Growth inhibition assay | Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=26.2134μM | SANGER | |||
| ALL-PO | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=26.6132μM | SANGER | |||
| LB771-HNC | Growth inhibition assay | Inhibition of human LB771-HNC cell growth in a cell viability assay, IC50=27.8393μM | SANGER | |||
| NEC8 | Growth inhibition assay | Inhibition of human NEC8 cell growth in a cell viability assay, IC50=29.0389μM | SANGER | |||
| MSTO-211H | Growth inhibition assay | Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50=29.059μM | SANGER | |||
| ATN-1 | Growth inhibition assay | Inhibition of human ATN-1 cell growth in a cell viability assay, IC50=29.7028μM | SANGER | |||
| LB373-MEL-D | Growth inhibition assay | Inhibition of human LB373-MEL-D cell growth in a cell viability assay, IC50=29.7129μM | SANGER | |||
| NB69 | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay, IC50=30.374μM | SANGER | |||
| LOXIMVI | Growth inhibition assay | Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=30.8334μM | SANGER | |||
| HC-1 | Growth inhibition assay | Inhibition of human HC-1 cell growth in a cell viability assay, IC50=32.8423μM | SANGER | |||
| SK-UT-1 | Growth inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=32.9447μM | SANGER | |||
| KARPAS-422 | Growth inhibition assay | Inhibition of human KARPAS-422 cell growth in a cell viability assay, IC50=33.2528μM | SANGER | |||
| KP-N-RT-BM-1 | Growth inhibition assay | Inhibition of human KP-N-RT-BM-1 cell growth in a cell viability assay, IC50=33.8198μM | SANGER | |||
| SIG-M5 | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=34.6805μM | SANGER | |||
| TE-11 | Growth inhibition assay | Inhibition of human TE-11 cell growth in a cell viability assay, IC50=38.0936μM | SANGER | |||
| RKO | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=38.4067μM | SANGER | |||
| LS-411N | Growth inhibition assay | Inhibition of human LS-411N cell growth in a cell viability assay, IC50=38.8809μM | SANGER | |||
| OCUB-M | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=40.2533μM | SANGER | |||
| OVCAR-4 | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=40.5786μM | SANGER | |||
| JiyoyeP-2003 | Growth inhibition assay | Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50=41.2672μM | SANGER | |||
| no-11 | Growth inhibition assay | Inhibition of human no-11 cell growth in a cell viability assay, IC50=41.8283μM | SANGER | |||
| NCI-H1694 | Growth inhibition assay | Inhibition of human NCI-H1694 cell growth in a cell viability assay, IC50=43.3351μM | SANGER | |||
| IST-SL1 | Growth inhibition assay | Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=46.6838μM | SANGER | |||
| T cells | Function assay | Inhibition of anti-CD3/CD28-induced IL2 secretion in human T cells, IC50=1.9μM | 16884310 | |||
| 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 | |||
| 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 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 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 | |||
| Klicka för att visa mer experimentella data för cellinjer | ||||||
| Molekylvikt | 568.67 | Formel | C32H36N6O4 |
Lagring (från mottagningsdatumet) | |
|---|---|---|---|---|---|
| CAS-nr | 837422-57-8 | Ladda ner SDF | Lagring av stamlösningar |
|
|
| Synonymer | KIN001-112, KIN112, Dual LCK/SRC inhibitor | Smiles | CC1=C(C(=CC=C1)C)OC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC(=NC=C3)NC4=CC=C(C=C4)N5CCN(CC5)C | ||
|
In vitro |
DMSO
: 12 mg/mL
(21.1 mM)
Ethanol : 6 mg/mL Water : Insoluble |
|
In vivo |
|||||
Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)
Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)
Beräkningsresultat:
Arbetskoncentration: mg/ml;
Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )
Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH2O, blanda och klarna.
Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.
Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.
| Targets/IC50/Ki |
Lck
(Cell-free assay) 2 nM
Src
(Cell-free assay) 6 nM
|
|---|---|
| In vitro |
WH-4-023 shows little activity on p38 and KDR. |
| Kinasanalys |
Lck-kinasanalys
|
|
Lck HTRF-kinasanalysen innefattar ATP-beroende fosforylering av ett biotinylerat gastrin-substratpeptid i närvaro eller frånvaro av hämmarsubstans. Slutkoncentrationen av gastrin är 1,2 μM. Slutkoncentrationen av ATP är 0,5 μM (Km app = 0,6 ± 0,1 μM), och slutkoncentrationen av Lck (en GST-kinasdomänfusion (AA 225−509)) är 250 pM. Buffertförhållandena är som följer: 50 mM HEPES pH = 7,5, 50 mM NaCl, 20 mM MgCl2, 5 mM MnCl, 2 mM DTT, 0,05% BSA. Analysen avbryts och stoppas med 160 μL detektionsreagens. Detektionsreagenserna är som följer: Buffert gjord av 50 mM Tris, pH = 7,5, 100 mM NaCl, 3 mM EDTA, 0,05% BSA, 0,1% Tween20. Innan avläsning tillsätts Streptavidin allofycocyanin (SA-APC) till en slutkoncentration i analysen på 0,0004 mg/mL, tillsammans med europiummärkt anti-fosfotyrosin-antikropp (Eu-anti-PY) till en slutkoncentration på 0,025 nM. Analysplattan avläses i en Discovery-fluorescensplattläsare med excitation vid 320 nm och emission vid 615 och 655 nm. Analyser för andra kinaser utförs på ett liknande sätt som beskrivs ovan, med variationer i koncentrationerna av enzym, peptidsubstrat och ATP som tillsätts till reaktionen, beroende på kinasens specifika aktivitet och uppmätta Km-värden för substraten.
|
Referenser |
|