pour la recherche uniquement
Linsitinib (OSI-906) inhibiteur de IGF-1R/Insulin Receptor
Réf. CatalogueS1091
Structure chimique
Poids moléculaire: 421.49
Aller à
Contrôle Qualité
Lot :
Pureté :
99.99%
99.99
| Cibles apparentées | EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 |
|---|---|
| Autre IGF-1R Inhibiteurs | BMS-536924 NVP-AEW541 BMS-754807 Picropodophyllin (AXL1717) GSK1904529A AG-1024 NVP-ADW742 NT157 PQ 401 MSDC-0160 |
Culture cellulaire, traitement et concentration de travail
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| A4-Fuk | Growth Inhibition Assay | IC50=0.02806 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=0.03835 μM | SANGER | |||
| TE-11 | Growth Inhibition Assay | IC50=0.07822 μM | SANGER | |||
| EW-1 | Growth Inhibition Assay | IC50=0.08585 μM | SANGER | |||
| HMV-II | Growth Inhibition Assay | IC50=0.08846 μM | SANGER | |||
| COLO-205 | Growth Inhibition Assay | IC50=0.10454 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=0.10696 μM | SANGER | |||
| GDM-1 | Growth Inhibition Assay | IC50=0.13672 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=0.15896 μM | SANGER | |||
| Saos-2 | Growth Inhibition Assay | IC50=0.16526 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=0.18135 μM | SANGER | |||
| G-401 | Growth Inhibition Assay | IC50=0.1823 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=0.18777 μM | SANGER | |||
| EW-7 | Growth Inhibition Assay | IC50=0.18881 μM | SANGER | |||
| NCI-H727 | Growth Inhibition Assay | IC50=0.19794 μM | SANGER | |||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=0.20955 μM | SANGER | |||
| NCI-H650 | Growth Inhibition Assay | IC50=0.21384 μM | SANGER | |||
| NCI-H2122 | Growth Inhibition Assay | IC50=0.23299 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=0.23698 μM | SANGER | |||
| HT-29 | Growth Inhibition Assay | IC50=0.24248 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=0.25915 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=0.26191 μM | SANGER | |||
| LAN-6 | Growth Inhibition Assay | IC50=0.26348 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=0.27001 μM | SANGER | |||
| LS-1034 | Growth Inhibition Assay | IC50=0.27132 μM | SANGER | |||
| EW-11 | Growth Inhibition Assay | IC50=0.28432 μM | SANGER | |||
| SNU-C1 | Growth Inhibition Assay | IC50=0.29313 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=0.33758 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=0.41038 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=0.41368 μM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=0.45437 μM | SANGER | |||
| BFTC-905 | Growth Inhibition Assay | IC50=0.46758 μM | SANGER | |||
| A375 | Growth Inhibition Assay | IC50=0.47617 μM | SANGER | |||
| SJRH30 | Growth Inhibition Assay | IC50=0.50822 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=0.52267 μM | SANGER | |||
| SIG-M5 | Growth Inhibition Assay | IC50=0.53557 μM | SANGER | |||
| DOK | Growth Inhibition Assay | IC50=0.556 μM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=0.58257 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.60236 μM | SANGER | |||
| SK-MM-2 | Growth Inhibition Assay | IC50=0.65491 μM | SANGER | |||
| NCI-H358 | Growth Inhibition Assay | IC50=0.67082 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=0.74859 μM | SANGER | |||
| NH-12 | Growth Inhibition Assay | IC50=0.76046 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=0.76486 μM | SANGER | |||
| COLO-668 | Growth Inhibition Assay | IC50=0.84666 μM | SANGER | |||
| PANC-08-13 | Growth Inhibition Assay | IC50=0.86377 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=0.88263 μM | SANGER | |||
| ABC-1 | Growth Inhibition Assay | IC50=0.90352 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=0.91066 μM | SANGER | |||
| SNU-387 | Growth Inhibition Assay | IC50=0.99393 μM | SANGER | |||
| CMK | Growth Inhibition Assay | IC50=0.99929 μM | SANGER | |||
| SJSA-1 | Growth Inhibition Assay | IC50=1.03653 μM | SANGER | |||
| SIMA | Growth Inhibition Assay | IC50=1.06825 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=1.12297 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=1.15444 μM | SANGER | |||
| MEL-JUSO | Growth Inhibition Assay | IC50=1.15759 μM | SANGER | |||
| T84 | Growth Inhibition Assay | IC50=1.20914 μM | SANGER | |||
| CAL-85-1 | Growth Inhibition Assay | IC50=1.23138 μM | SANGER | |||
| RD | Growth Inhibition Assay | IC50=1.26455 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=1.31462 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=1.34208 μM | SANGER | |||
| EKVX | Growth Inhibition Assay | IC50=1.34568 μM | SANGER | |||
| SK-MEL-3 | Growth Inhibition Assay | IC50=1.48556 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=1.50193 μM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=1.51113 μM | SANGER | |||
| HuH-7 | Growth Inhibition Assay | IC50=1.60098 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=1.66928 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=1.70945 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=1.73887 μM | SANGER | |||
| LB647-SCLC | Growth Inhibition Assay | IC50=1.76583 μM | SANGER | |||
| NCI-H2171 | Growth Inhibition Assay | IC50=1.77716 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=1.91298 μM | SANGER | |||
| MC-IXC | Growth Inhibition Assay | IC50=1.9898 μM | SANGER | |||
| LS-513 | Growth Inhibition Assay | IC50=2.05305 μM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=2.09844 μM | SANGER | |||
| OPM-2 | Growth Inhibition Assay | IC50=2.102 μM | SANGER | |||
| LP-1 | Growth Inhibition Assay | IC50=2.25807 μM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=2.277 μM | SANGER | |||
| CP66-MEL | Growth Inhibition Assay | IC50=2.29014 μM | SANGER | |||
| HCC1143 | Growth Inhibition Assay | IC50=2.45368 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=2.6021 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=2.70838 μM | SANGER | |||
| NCI-H1882 | Growth Inhibition Assay | IC50=2.75227 μM | SANGER | |||
| CHP-126 | Growth Inhibition Assay | IC50=2.76317 μM | SANGER | |||
| NCI-H1623 | Growth Inhibition Assay | IC50=2.92024 μM | SANGER | |||
| GB-1 | Growth Inhibition Assay | IC50=2.93404 μM | SANGER | |||
| RCC10RGB | Growth Inhibition Assay | IC50=2.95281 μM | SANGER | |||
| NCI-H2141 | Growth Inhibition Assay | IC50=2.96896 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=3.00565 μM | SANGER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=3.04085 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=3.04992 μM | SANGER | |||
| SNU-423 | Growth Inhibition Assay | IC50=3.20313 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=3.25699 μM | SANGER | |||
| CAL-12T | Growth Inhibition Assay | IC50=3.40713 μM | SANGER | |||
| LU-99A | Growth Inhibition Assay | IC50=3.47105 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=3.53429 μM | SANGER | |||
| SK-LU-1 | Growth Inhibition Assay | IC50=3.76295 μM | SANGER | |||
| SW837 | Growth Inhibition Assay | IC50=3.76333 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=3.83877 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=3.92086 μM | SANGER | |||
| TGW | Growth Inhibition Assay | IC50=4.01311 μM | SANGER | |||
| GP5d | Growth Inhibition Assay | IC50=4.05362 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=4.15213 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=4.26887 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=4.28615 μM | SANGER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=4.29819 μM | SANGER | |||
| LCLC-103H | Growth Inhibition Assay | IC50=4.32195 μM | SANGER | |||
| LS-411N | Growth Inhibition Assay | IC50=4.44885 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=4.45687 μM | SANGER | |||
| PANC-10-05 | Growth Inhibition Assay | IC50=4.6984 μM | SANGER | |||
| DK-MG | Growth Inhibition Assay | IC50=4.80933 μM | SANGER | |||
| OVCAR-5 | Growth Inhibition Assay | IC50=4.81226 μM | SANGER | |||
| CAL-39 | Growth Inhibition Assay | IC50=4.8767 μM | SANGER | |||
| TE-441-T | Growth Inhibition Assay | IC50=4.90537 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=4.95253 μM | SANGER | |||
| MCF7 | Growth Inhibition Assay | IC50=5.14517 μM | SANGER | |||
| CAPAN-1 | Growth Inhibition Assay | IC50=5.25707 μM | SANGER | |||
| PSN1 | Growth Inhibition Assay | IC50=5.27235 μM | SANGER | |||
| NCI-H292 | Growth Inhibition Assay | IC50=5.30044 μM | SANGER | |||
| CPC-N | Growth Inhibition Assay | IC50=5.39419 μM | SANGER | |||
| DoTc2-4510 | Growth Inhibition Assay | IC50=5.45371 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=5.55933 μM | SANGER | |||
| MHH-ES-1 | Growth Inhibition Assay | IC50=5.59907 μM | SANGER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=5.70227 μM | SANGER | |||
| SW1710 | Growth Inhibition Assay | IC50=5.74751 μM | SANGER | |||
| YAPC | Growth Inhibition Assay | IC50=5.76201 μM | SANGER | |||
| 22RV1 | Growth Inhibition Assay | IC50=5.80019 μM | SANGER | |||
| COLO-679 | Growth Inhibition Assay | IC50=5.88948 μM | SANGER | |||
| TCCSUP | Growth Inhibition Assay | IC50=5.93259 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=5.9397 μM | SANGER | |||
| TE-15 | Growth Inhibition Assay | IC50=6.06605 μM | SANGER | |||
| SCLC-21H | Growth Inhibition Assay | IC50=6.10843 μM | SANGER | |||
| EoL-1-cell | Growth Inhibition Assay | IC50=6.16563 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=6.1671 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=6.27428 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=6.29622 μM | SANGER | |||
| NALM-6 | Growth Inhibition Assay | IC50=6.3323 μM | SANGER | |||
| NCI-H522 | Growth Inhibition Assay | IC50=6.33306 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=6.37079 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=6.38667 μM | SANGER | |||
| NCI-H1417 | Growth Inhibition Assay | IC50=6.40847 μM | SANGER | |||
| HT-1197 | Growth Inhibition Assay | IC50=6.57122 μM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=6.6277 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=6.71916 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=6.75405 μM | SANGER | |||
| HCC2157 | Growth Inhibition Assay | IC50=6.77475 μM | SANGER | |||
| NCI-H838 | Growth Inhibition Assay | IC50=6.9649 μM | SANGER | |||
| NCI-H1299 | Growth Inhibition Assay | IC50=6.9709 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=7.20068 μM | SANGER | |||
| NCI-H441 | Growth Inhibition Assay | IC50=7.34065 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=7.48373 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=7.65929 μM | SANGER | |||
| CAL-54 | Growth Inhibition Assay | IC50=7.82977 μM | SANGER | |||
| KYSE-180 | Growth Inhibition Assay | IC50=7.88941 μM | SANGER | |||
| NCI-H187 | Growth Inhibition Assay | IC50=7.95947 μM | SANGER | |||
| RT-112 | Growth Inhibition Assay | IC50=8.09677 μM | SANGER | |||
| NCI-H1437 | Growth Inhibition Assay | IC50=8.09795 μM | SANGER | |||
| SNU-449 | Growth Inhibition Assay | IC50=8.28272 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=8.29391 μM | SANGER | |||
| NCI-H2030 | Growth Inhibition Assay | IC50=8.37714 μM | SANGER | |||
| HuO-3N1 | Growth Inhibition Assay | IC50=8.37844 μM | SANGER | |||
| COLO-792 | Growth Inhibition Assay | IC50=8.41527 μM | SANGER | |||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=8.85508 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=9.0425 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=9.09751 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=9.10469 μM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=9.29974 μM | SANGER | |||
| NCI-H1993 | Growth Inhibition Assay | IC50=9.44261 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=9.4712 μM | SANGER | |||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=9.51583 μM | SANGER | |||
| NCCIT | Growth Inhibition Assay | IC50=9.53169 μM | SANGER | |||
| SAS | Growth Inhibition Assay | IC50=10.248 μM | SANGER | |||
| A673 | Growth Inhibition Assay | IC50=10.3704 μM | SANGER | |||
| NCI-H1522 | Growth Inhibition Assay | IC50=10.3707 μM | SANGER | |||
| NCI-H810 | Growth Inhibition Assay | IC50=10.3907 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=10.4564 μM | SANGER | |||
| GR-ST | Growth Inhibition Assay | IC50=10.5024 μM | SANGER | |||
| SUP-T1 | Growth Inhibition Assay | IC50=10.7317 μM | SANGER | |||
| NB5 | Growth Inhibition Assay | IC50=10.9022 μM | SANGER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=10.9571 μM | SANGER | |||
| SK-CO-1 | Growth Inhibition Assay | IC50=10.9931 μM | SANGER | |||
| Capan-2 | Growth Inhibition Assay | IC50=11.3198 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=11.6757 μM | SANGER | |||
| REH | Growth Inhibition Assay | IC50=11.7451 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=11.8615 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=12.0916 μM | SANGER | |||
| NCI-H1651 | Growth Inhibition Assay | IC50=12.2478 μM | SANGER | |||
| NCI-H1618 | Growth Inhibition Assay | IC50=12.3976 μM | SANGER | |||
| NCI-H2081 | Growth Inhibition Assay | IC50=12.6141 μM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=12.7213 μM | SANGER | |||
| NY | Growth Inhibition Assay | IC50=13.0643 μM | SANGER | |||
| PANC-03-27 | Growth Inhibition Assay | IC50=13.0807 μM | SANGER | |||
| BHY | Growth Inhibition Assay | IC50=13.2121 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=13.3763 μM | SANGER | |||
| 5637 | Growth Inhibition Assay | IC50=13.7759 μM | SANGER | |||
| LC-1F | Growth Inhibition Assay | IC50=14.0356 μM | SANGER | |||
| SNB75 | Growth Inhibition Assay | IC50=14.0383 μM | SANGER | |||
| CHP-212 | Growth Inhibition Assay | IC50=14.0464 μM | SANGER | |||
| HT-1376 | Growth Inhibition Assay | IC50=14.1126 μM | SANGER | |||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=14.1502 μM | SANGER | |||
| CA46 | Growth Inhibition Assay | IC50=14.1827 μM | SANGER | |||
| SCC-15 | Growth Inhibition Assay | IC50=14.5583 μM | SANGER | |||
| ATN-1 | Growth Inhibition Assay | IC50=14.6627 μM | SANGER | |||
| NCI-H2405 | Growth Inhibition Assay | IC50=14.8157 μM | SANGER | |||
| NCI-H716 | Growth Inhibition Assay | IC50=14.8493 μM | SANGER | |||
| SW620 | Growth Inhibition Assay | IC50=14.9014 μM | SANGER | |||
| NCI-H226 | Growth Inhibition Assay | IC50=14.9085 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=14.9432 μM | SANGER | |||
| KYSE-150 | Growth Inhibition Assay | IC50=14.955 μM | SANGER | |||
| OCUB-M | Growth Inhibition Assay | IC50=14.9883 μM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=15.0984 μM | SANGER | |||
| SW1463 | Growth Inhibition Assay | IC50=15.4223 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=15.5346 μM | SANGER | |||
| MKN28 | Growth Inhibition Assay | IC50=15.5479 μM | SANGER | |||
| SW13 | Growth Inhibition Assay | IC50=15.618 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=15.9697 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=15.9768 μM | SANGER | |||
| Calu-1 | Growth Inhibition Assay | IC50=16.0368 μM | SANGER | |||
| ST486 | Growth Inhibition Assay | IC50=16.0431 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=16.1246 μM | SANGER | |||
| EGI-1 | Growth Inhibition Assay | IC50=16.446 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=16.4731 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=17.2297 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=17.2459 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=17.4139 μM | SANGER | |||
| Daoy | Growth Inhibition Assay | IC50=17.4695 μM | SANGER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=17.4771 μM | SANGER | |||
| NCI-H1563 | Growth Inhibition Assay | IC50=17.4917 μM | SANGER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=17.6648 μM | SANGER | |||
| 786-0 | Growth Inhibition Assay | IC50=17.8353 μM | SANGER | |||
| AM-38 | Growth Inhibition Assay | IC50=17.9306 μM | SANGER | |||
| COLO-824 | Growth Inhibition Assay | IC50=18.4436 μM | SANGER | |||
| SK-MEL-30 | Growth Inhibition Assay | IC50=18.5082 μM | SANGER | |||
| CESS | Growth Inhibition Assay | IC50=18.7609 μM | SANGER | |||
| BL-70 | Growth Inhibition Assay | IC50=18.8156 μM | SANGER | |||
| NCI-H2170 | Growth Inhibition Assay | IC50=18.9179 μM | SANGER | |||
| HT-3 | Growth Inhibition Assay | IC50=18.983 μM | SANGER | |||
| BOKU | Growth Inhibition Assay | IC50=19.0381 μM | SANGER | |||
| HPAF-II | Growth Inhibition Assay | IC50=19.3015 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=19.4765 μM | SANGER | |||
| MC-CAR | Growth Inhibition Assay | IC50=19.6313 μM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=19.777 μM | SANGER | |||
| SW1783 | Growth Inhibition Assay | IC50=19.7806 μM | SANGER | |||
| KP-N-YN | Growth Inhibition Assay | IC50=20.0262 μM | SANGER | |||
| LU-165 | Growth Inhibition Assay | IC50=20.5571 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=20.6451 μM | SANGER | |||
| EFM-19 | Growth Inhibition Assay | IC50=21.0716 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=21.1054 μM | SANGER | |||
| HEL | Growth Inhibition Assay | IC50=21.4216 μM | SANGER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=21.426 μM | SANGER | |||
| ECC4 | Growth Inhibition Assay | IC50=21.707 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=21.8368 μM | SANGER | |||
| KMOE-2 | Growth Inhibition Assay | IC50=21.8921 μM | SANGER | |||
| NCI-H524 | Growth Inhibition Assay | IC50=22.0808 μM | SANGER | |||
| WSU-NHL | Growth Inhibition Assay | IC50=22.1577 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=22.2469 μM | SANGER | |||
| HOP-92 | Growth Inhibition Assay | IC50=22.3167 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=22.4677 μM | SANGER | |||
| KYSE-270 | Growth Inhibition Assay | IC50=22.9357 μM | SANGER | |||
| SK-MEL-24 | Growth Inhibition Assay | IC50=23.187 μM | SANGER | |||
| Calu-3 | Growth Inhibition Assay | IC50=23.2128 μM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=23.2367 μM | SANGER | |||
| SW1573 | Growth Inhibition Assay | IC50=23.7415 μM | SANGER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=24.0194 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=24.5013 μM | SANGER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=24.6064 μM | SANGER | |||
| KALS-1 | Growth Inhibition Assay | IC50=24.7327 μM | SANGER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=25.8032 μM | SANGER | |||
| HuP-T3 | Growth Inhibition Assay | IC50=26.1674 μM | SANGER | |||
| OE19 | Growth Inhibition Assay | IC50=26.2153 μM | SANGER | |||
| J82 | Growth Inhibition Assay | IC50=26.2471 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=26.3819 μM | SANGER | |||
| DMS-53 | Growth Inhibition Assay | IC50=26.5138 μM | SANGER | |||
| COLO-741 | Growth Inhibition Assay | IC50=26.8344 μM | SANGER | |||
| SW48 | Growth Inhibition Assay | IC50=26.882 μM | SANGER | |||
| IGR-1 | Growth Inhibition Assay | IC50=26.9334 μM | SANGER | |||
| 639-V | Growth Inhibition Assay | IC50=27.0245 μM | SANGER | |||
| LK-2 | Growth Inhibition Assay | IC50=27.4141 μM | SANGER | |||
| NCI-H2347 | Growth Inhibition Assay | IC50=27.9699 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition Assay | IC50=28.0905 μM | SANGER | |||
| LS-123 | Growth Inhibition Assay | IC50=28.1262 μM | SANGER | |||
| U031 | Growth Inhibition Assay | IC50=28.252 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition Assay | IC50=28.4721 μM | SANGER | |||
| NCI-H2087 | Growth Inhibition Assay | IC50=28.7552 μM | SANGER | |||
| NCI-H2342 | Growth Inhibition Assay | IC50=29.5208 μM | SANGER | |||
| SW626 | Growth Inhibition Assay | IC50=29.756 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=29.815 μM | SANGER | |||
| RXF393 | Growth Inhibition Assay | IC50=30.0952 μM | SANGER | |||
| LC4-1 | Growth Inhibition Assay | IC50=30.3092 μM | SANGER | |||
| NCI-H1694 | Growth Inhibition Assay | IC50=30.6624 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=30.9702 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=30.9725 μM | SANGER | |||
| BCPAP | Growth Inhibition Assay | IC50=31.8379 μM | SANGER | |||
| BC-3 | Growth Inhibition Assay | IC50=32.1403 μM | SANGER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=32.2358 μM | SANGER | |||
| NCI-H2009 | Growth Inhibition Assay | IC50=32.4981 μM | SANGER | |||
| HTC-C3 | Growth Inhibition Assay | IC50=33.7519 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=34.4407 μM | SANGER | |||
| CCRF-CEM | Growth Inhibition Assay | IC50=34.5715 μM | SANGER | |||
| AN3-CA | Growth Inhibition Assay | IC50=35.0568 μM | SANGER | |||
| NCI-H1734 | Growth Inhibition Assay | IC50=35.2561 μM | SANGER | |||
| Ca-Ski | Growth Inhibition Assay | IC50=35.4101 μM | SANGER | |||
| U-266 | Growth Inhibition Assay | IC50=35.6114 μM | SANGER | |||
| SBC-5 | Growth Inhibition Assay | IC50=35.7781 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=37.115 μM | SANGER | |||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=37.2248 μM | SANGER | |||
| PFSK-1 | Growth Inhibition Assay | IC50=37.2435 μM | SANGER | |||
| IMR-5 | Growth Inhibition Assay | IC50=37.2487 μM | SANGER | |||
| Daudi | Growth Inhibition Assay | IC50=37.3597 μM | SANGER | |||
| A498 | Growth Inhibition Assay | IC50=37.7218 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=37.7843 μM | SANGER | |||
| COLO-680N | Growth Inhibition Assay | IC50=38.2885 μM | SANGER | |||
| SK-MES-1 | Growth Inhibition Assay | IC50=38.3215 μM | SANGER | |||
| SR | Growth Inhibition Assay | IC50=38.5495 μM | SANGER | |||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=38.5637 μM | SANGER | |||
| SK-HEP-1 | Growth Inhibition Assay | IC50=38.7822 μM | SANGER | |||
| BPH-1 | Growth Inhibition Assay | IC50=38.8329 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=39.5817 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=39.8084 μM | SANGER | |||
| SW1088 | Growth Inhibition Assay | IC50=40.2107 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=40.2901 μM | SANGER | |||
| AsPC-1 | Growth Inhibition Assay | IC50=40.4583 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=40.6568 μM | SANGER | |||
| A172 | Growth Inhibition Assay | IC50=40.8511 μM | SANGER | |||
| SN12C | Growth Inhibition Assay | IC50=40.9385 μM | SANGER | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=40.9898 μM | SANGER | |||
| RPMI-2650 | Growth Inhibition Assay | IC50=41.1593 μM | SANGER | |||
| KYSE-140 | Growth Inhibition Assay | IC50=41.8123 μM | SANGER | |||
| KINGS-1 | Growth Inhibition Assay | IC50=42.4697 μM | SANGER | |||
| HSC-3 | Growth Inhibition Assay | IC50=42.6661 μM | SANGER | |||
| PC-14 | Growth Inhibition Assay | IC50=43.1882 μM | SANGER | |||
| COR-L105 | Growth Inhibition Assay | IC50=43.6502 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=44.2371 μM | SANGER | |||
| NCI-H661 | Growth Inhibition Assay | IC50=44.2958 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=44.3599 μM | SANGER | |||
| HCC1806 | Growth Inhibition Assay | IC50=44.5873 μM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=44.8453 μM | SANGER | |||
| IST-SL2 | Growth Inhibition Assay | IC50=45.1247 μM | SANGER | |||
| 8305C | Growth Inhibition Assay | IC50=45.309 μM | SANGER | |||
| UACC-62 | Growth Inhibition Assay | IC50=46.2875 μM | SANGER | |||
| COR-L23 | Growth Inhibition Assay | IC50=47.199 μM | SANGER | |||
| EFE-184 | Growth Inhibition Assay | IC50=47.388 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=47.4149 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=48.5315 μM | SANGER | |||
| SNG-M | Growth Inhibition Assay | IC50=49.434 μM | SANGER | |||
| A2058 | Growth Inhibition Assay | IC50=49.4885 μM | SANGER | |||
| HEK293 | Function assay | 60 mins | Inhibition of full length IGF-1 receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis, IC50 = 0.0028 μM. | 26951753 | ||
| Ba/F3 | Function assay | Inhibition of full length IGF-1 receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation, IC50 = 0.0076 μM. | 26951753 | |||
| HEK293 | Function assay | 60 mins | Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis, IC50 = 0.016 μM. | 26951753 | ||
| A431 | Function assay | Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.018 μM. | 20346655 | |||
| 3T3 | Function assay | Inhibition of human IGF1R expressed in mouse 3T3 cells by ELISA based assay, IC50 = 0.024 μM. | 21251824 | |||
| NIH 3T3 | Function assay | 2 hrs | Inhibition of full length human IGF-1R overexpressed in mouse NIH 3T3 cells assessed as IGF1-induced protein phosphorylation incubated for 2 hrs prior to IGF1 induction measured after 15 mins by ELISA, IC50 = 0.024 μM. | 24900721 | ||
| Ba/F3 | Function assay | Inhibition of full length insulin receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation, IC50 = 0.126 μM. | 26951753 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 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 | |||
| 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 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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 | |||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
Informations chimiques, stockage et stabilité
| Poids moléculaire | 421.49 | Formule | C26H23N5O |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 867160-71-2 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | N/A | Smiles | CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O | ||
Solubilité
|
In vitro |
DMSO
: 84 mg/mL
(199.29 mM)
Water : Insoluble Ethanol : Insoluble |
Calculateur de molarité
Calculateur de dilution
Calculateur de poids moléculaire
|
In vivo |
|||||
Calculateur de formulation in vivo (Solution claire)
Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
mg/kg
g
μL
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
Mécanisme daction
| Targets/IC50/Ki |
IGF-1R
(Cell-free assay) 35 nM
Insulin Receptor
(Cell-free assay) 75 nM
IRR
(Cell-free assay) 75 nM
|
|---|---|
| In vitro |
Linsitinib (OSI-906) inhibe l'autophosphorylation de l'IGF-1R et l'activation des protéines de signalisation en aval Akt, ERK1/2 et S6 kinase avec une IC50 de 0,028 à 0,13 μM. Il permet une conformation intermédiaire de la protéine cible grâce à des interactions avec l'hélice C et présente une stabilité métabolique favorable dans les microsomes hépatiques. Ce composé inhibe entièrement la phosphorylation de l'IR et de l'IGF-1R à une concentration de 1 μM et inhibe la prolifération de plusieurs lignées cellulaires tumorales, y compris le cancer du poumon non à petites cellules et la lignée cellulaire tumorale du cancer colorectal (CRC) avec une EC50 de 0,021 à 0,810 μM.
|
| Essai kinase |
essais biochimiques de Protein Tyrosine Kinase
|
|
Les essais de Protein Tyrosine Kinase sont réalisés en interne par des méthodes d'essai basées sur ELISA (IGF-1R, IR, EGFR et KDR) ou chez Upstate Inc. par une méthode radiométrique avec de l'ATP à une concentration de 100 µM. Les essais ELISA en interne utilisent du poly(Glu:Tyr) comme substrat lié à la surface des plaques d'essai à 96 puits et la phosphorylation est détectée à l'aide d'un anticorps anti-phosphotyrosine conjugué à la peroxydase de raifort. L'anticorps lié est quantifié à l'aide d'ABTS comme substrat de la peroxydase en mesurant l'absorbance à 405 / 490 nm. Tous les essais utilisent des domaines catalytiques de kinase recombinants purifiés. Les enzymes recombinantes d'IGF-1R ou d'EGFR humains sont exprimées sous forme de protéine de fusion glutathion S-transférase NH2-terminale dans des cellules d'insectes et sont purifiées en interne. Les valeurs d'IC50 sont déterminées à partir de la courbe dose-réponse sigmoïdale du pourcentage d'inhibition en fonction du log10 de la concentration du composé. Un minimum de trois mesures, effectuées en double, sont réalisées avec des essais en interne, sauf indication contraire. À une concentration de 1 µM, ce composé est profilé par rapport à un panel de kinases à l'aide du kit ProfilerProTM Kinase Selectivity Assay Kit.
|
|
| In vivo |
Linsitinib (OSI-906) inhibe la croissance tumorale dans un modèle de souris xénogreffe piloté par IGF-1R, avec 100 % de TGI et 55 % de régression à une dose de 75 mg/kg et 60 % de TGI et aucune régression à une dose de 25 mg/kg. Son administration induit différentes demi-vies d'élimination chez le chien, le rat et la souris, qui sont respectivement de 1,18 heures, 2,64 heures et 2,14 heures. Lorsqu'il est administré à différentes doses uniques une fois par jour chez des rats Sprague-Dawley femelles et des souris CD-1 femelles, il révèle que la Vmax n'est pas proportionnelle à sa dose. Ce composé élève les niveaux de glucose sanguin à une dose de 25 mg/kg après 12 jours d'administration. À une dose unique de 75 mg/kg dans un modèle de souris xénogreffe IGF-1R humain pleine longueur (LISN) piloté par IGF-1R, il atteint une inhibition maximale de la phosphorylation de l'IGF-1R (80 %) entre 4 et 24 heures avec des concentrations plasmatiques du médicament de 26,6-4,77 μM. Lorsqu'il est administré en dose unique de 60 mg/kg chez des souris xénogreffées NCI-H292, il inhibe la captation de glucose à 2, 4 et 24 heures post-traitement in vivo. Il inhibe également la croissance des tumeurs dans un modèle de souris xénogreffe NCI-H292.
|
Références |
|
Applications
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | pS6 / S6 p-STAT3(Y705) / STAT3 pSrc(Y416) / Src cleaved caspase-3 / cleaved PARP p-IGF1R / IGF1R / p-mTOR / mTOR p-EGFR / EGFR / p-IGF1R / IGF1R / p-IRS1 / IRS1 / p-ERK / ERK / p-AKT / AKT |
|
21257723 |
| Immunofluorescence | FoxO1 |
|
27535223 |
| Growth inhibition assay | Cell viability |
|
26136493 |
Informations sur lessai clinique
(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Promoteur/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| NCT02546544 | Completed | Relapsed Ewing Sarcoma|Refractory Ewing Sarcoma |
University of Oxford|European Organisation for Research and Treatment of Cancer - EORTC|European Commission|Astellas Pharma Inc|Oxford University Hospitals NHS Trust |
March 2014 | Phase 2 |
| NCT01672736 | Terminated | Multiple Myeloma |
University Health Network Toronto|Multiple Myeloma Research Consortium|Astellas Pharma Inc |
September 2012 | Phase 1|Phase 2 |
| NCT01529684 | Completed | Advanced Solid Tumors|Pharmacokinetics of 14C-OSI-906 |
Astellas Pharma Global Development Inc.|Astellas Pharma Inc |
March 19 2012 | Phase 1 |
| NCT01221077 | Completed | NSCLC|Non Small Cell Lung Cancer |
Astellas Pharma Inc |
April 8 2011 | Phase 2 |
Support technique
Tel: +1-832-582-8158 Ext:3
Si vous avez dautres questions, veuillez laisser un message.
Foire aux questions
Question 1:
Does it dissolve in the vehicle (30% PEG400/0.5%Tween 80/5% propylene glycol) or is it a suspension?
Réponse :
It is a suspension in 30% PEG400/0.5% Tween 80/5% propylene glycol.
Les produits sont destinés à la recherche uniquement. Ne pas utiliser chez lhomme. Nous ne vendons pas aux patients.
©Copyright 2013 Selleck Chemicals. Tous droits réservés.