- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
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- MAPK
- Cytoskeletal Signaling
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Linsitinib (OSI-906)
Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.
CAS No. 867160-71-2
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Linsitinib (OSI-906)関連製品
シグナル伝達経路
IGF-1R阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| 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 | |
| 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 | |
| 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 | |
| NALM-6 | Growth Inhibition Assay | IC50=6.3323 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=6.29622 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=6.27428 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=6.1671 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=6.16563 μM | SANGER | ||
| SCLC-21H | Growth Inhibition Assay | IC50=6.10843 μM | SANGER | ||
| TE-15 | Growth Inhibition Assay | IC50=6.06605 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=5.9397 μM | SANGER | ||
| TCCSUP | Growth Inhibition Assay | IC50=5.93259 μM | SANGER | ||
| COLO-679 | Growth Inhibition Assay | IC50=5.88948 μM | SANGER | ||
| 22RV1 | Growth Inhibition Assay | IC50=5.80019 μM | SANGER | ||
| YAPC | Growth Inhibition Assay | IC50=5.76201 μM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=5.74751 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=5.70227 μM | SANGER | ||
| MHH-ES-1 | Growth Inhibition Assay | IC50=5.59907 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=5.55933 μM | SANGER | ||
| DoTc2-4510 | Growth Inhibition Assay | IC50=5.45371 μM | SANGER | ||
| CPC-N | Growth Inhibition Assay | IC50=5.39419 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=5.30044 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=5.27235 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition Assay | IC50=5.25707 μM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=5.14517 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=4.95253 μM | SANGER | ||
| TE-441-T | Growth Inhibition Assay | IC50=4.90537 μM | SANGER | ||
| CAL-39 | Growth Inhibition Assay | IC50=4.8767 μM | SANGER | ||
| OVCAR-5 | Growth Inhibition Assay | IC50=4.81226 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=4.80933 μM | SANGER | ||
| PANC-10-05 | Growth Inhibition Assay | IC50=4.6984 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=4.45687 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=4.44885 μM | SANGER | ||
| LCLC-103H | Growth Inhibition Assay | IC50=4.32195 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=4.29819 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=4.28615 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=4.26887 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=4.15213 μM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=4.05362 μM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=4.01311 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=3.92086 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=3.83877 μM | SANGER | ||
| SW837 | Growth Inhibition Assay | IC50=3.76333 μM | SANGER | ||
| SK-LU-1 | Growth Inhibition Assay | IC50=3.76295 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=3.53429 μM | SANGER | ||
| LU-99A | Growth Inhibition Assay | IC50=3.47105 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=3.40713 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=3.25699 μM | SANGER | ||
| SNU-423 | Growth Inhibition Assay | IC50=3.20313 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=3.04992 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=3.04085 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=3.00565 μM | SANGER | ||
| NCI-H2141 | Growth Inhibition Assay | IC50=2.96896 μM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=2.95281 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=2.93404 μM | SANGER | ||
| NCI-H1623 | Growth Inhibition Assay | IC50=2.92024 μM | SANGER | ||
| CHP-126 | Growth Inhibition Assay | IC50=2.76317 μM | SANGER | ||
| NCI-H1882 | Growth Inhibition Assay | IC50=2.75227 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=2.70838 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=2.6021 μM | SANGER | ||
| HCC1143 | Growth Inhibition Assay | IC50=2.45368 μM | SANGER | ||
| CP66-MEL | Growth Inhibition Assay | IC50=2.29014 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=2.277 μM | SANGER | ||
| LP-1 | Growth Inhibition Assay | IC50=2.25807 μM | SANGER | ||
| OPM-2 | Growth Inhibition Assay | IC50=2.102 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=2.09844 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=2.05305 μM | SANGER | ||
| MC-IXC | Growth Inhibition Assay | IC50=1.9898 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=1.91298 μM | SANGER | ||
| NCI-H2171 | Growth Inhibition Assay | IC50=1.77716 μM | SANGER | ||
| LB647-SCLC | Growth Inhibition Assay | IC50=1.76583 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=1.73887 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=1.70945 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=1.66928 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=1.60098 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=1.51113 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=1.50193 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=1.48556 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=1.34568 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=1.34208 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=1.31462 μM | SANGER | ||
| RD | Growth Inhibition Assay | IC50=1.26455 μM | SANGER | ||
| CAL-85-1 | Growth Inhibition Assay | IC50=1.23138 μM | SANGER | ||
| T84 | Growth Inhibition Assay | IC50=1.20914 μM | SANGER | ||
| MEL-JUSO | Growth Inhibition Assay | IC50=1.15759 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=1.15444 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=1.12297 μM | SANGER | ||
| SIMA | Growth Inhibition Assay | IC50=1.06825 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=1.03653 μM | SANGER | ||
| CMK | Growth Inhibition Assay | IC50=0.99929 μM | SANGER | ||
| SNU-387 | Growth Inhibition Assay | IC50=0.99393 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=0.91066 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=0.90352 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=0.88263 μM | SANGER | ||
| PANC-08-13 | Growth Inhibition Assay | IC50=0.86377 μM | SANGER | ||
| COLO-668 | Growth Inhibition Assay | IC50=0.84666 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=0.76486 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=0.76046 μM | SANGER | ||
| RH-1 | Growth Inhibition Assay | IC50=0.74859 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=0.67082 μM | SANGER | ||
| SK-MM-2 | Growth Inhibition Assay | IC50=0.65491 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.60236 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=0.58257 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=0.556 μM | SANGER | ||
| SIG-M5 | Growth Inhibition Assay | IC50=0.53557 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=0.52267 μM | SANGER | ||
| SJRH30 | Growth Inhibition Assay | IC50=0.50822 μM | SANGER | ||
| A375 | Growth Inhibition Assay | IC50=0.47617 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=0.46758 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=0.45437 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=0.41368 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=0.41038 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=0.33758 μM | SANGER | ||
| SNU-C1 | Growth Inhibition Assay | IC50=0.29313 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=0.28432 μM | SANGER | ||
| LS-1034 | Growth Inhibition Assay | IC50=0.27132 μM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=0.27001 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=0.26348 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=0.26191 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=0.25915 μM | SANGER | ||
| HT-29 | Growth Inhibition Assay | IC50=0.24248 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=0.23698 μM | SANGER | ||
| NCI-H2122 | Growth Inhibition Assay | IC50=0.23299 μM | SANGER | ||
| NCI-H650 | Growth Inhibition Assay | IC50=0.21384 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=0.20955 μM | SANGER | ||
| NCI-H727 | Growth Inhibition Assay | IC50=0.19794 μM | SANGER | ||
| EW-7 | Growth Inhibition Assay | IC50=0.18881 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=0.18777 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=0.1823 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=0.18135 μM | SANGER | ||
| Saos-2 | Growth Inhibition Assay | IC50=0.16526 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=0.15896 μM | SANGER | ||
| GDM-1 | Growth Inhibition Assay | IC50=0.13672 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=0.10696 μM | SANGER | ||
| COLO-205 | Growth Inhibition Assay | IC50=0.10454 μM | SANGER | ||
| HMV-II | Growth Inhibition Assay | IC50=0.08846 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=0.08585 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=0.07822 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=0.03835 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=0.02806 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 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3. | ||||||
|---|---|---|---|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| In vitro | OSI-906 inhibits IGF-1R autophosphorylation and activation of the downstream signaling proteins Akt, ERK1/2 and S6 kinase with IC50 of 0.028 to 0.13 μM. OSI-906 enables an intermediate conformation of the target protein through interactions with the C-helix. OSI-906 displays favorable metabolic stability in liver microsomes. OSI-906 fully inhibits both IR and IGF-1R phosphorylation at a concentration of 1 μM. OSI-906 inhibits proliferation of several tumor cell lines including non-small-cell lung cancer and colorectal cancer (CRC) tumor cell line with EC50 of 0.021 to 0.810 μM. [1] | |||
|---|---|---|---|---|
| Kinase Assay | Protein kinase biochemical assays | |||
| Protein kinase assays are either performed in-house by ELISA-based assay methods (IGF-1R, IR, EGFR and KDR) or at Upstate Inc. by a radiometric method with ATP at 100 µM concentration. In-house ELISA assays use poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates and phosphorylation is detected using an antiphosphotyrosine antibody conjugated to horseradish peroxidase. The bound antibody is quantified using ABTS as the peroxidase substrate by measuring absorbance at 405 / 490 nm. All assays use purified recombinant kinase catalytic domains. Recombinant enzymes of human IGF-1R or EGFR are expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and are purified in house. IC50 values are determined from the sigmoidal dose–response plot of percent inhibition versus log10 compound concentration. A minimum of three measurements, performed in duplicate, are carried out with in-house assays unless otherwise indicated. OSI-906 at a concentration of 1 µM is profiled versus a panel of kinases using the ProfilerProTM Kinase Selectivity Assay Kit. | ||||
| 細胞実験 | 細胞株 | MCF7, NCI-H292, Colo-205, HT29, H358, H1703, BxPC3, A673, SW620, DU4475, HepG2 and Hepa-1, RKO 3T3/hulGF-IR and H292 cells | ||
| 濃度 | 0.02-0.8 μM | |||
| 反応時間 | 3 days | |||
| 実験の流れ | For assays of cell proliferation, cells are seeded into 96-well plates in appropriate media containing FCS 10% and incubated for 3 days in the presence of OSI-906 at various concentrations. Inhibition of cell growth is determined by luminescent quantitation of intracellular ATP content using CellTiterGlo. Data is presented as a fraction of maximal proliferation, calculated by dividing the cellular density in the presence of varying concentrations of OSI-906 by the cellular density of control cells treated with vehicle (DMSO) only. | |||
| 実験結果図 | Methods | Biomarkers | 結果図 | 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 | |
| In Vivo | ||
| In Vivo | OSI-906 inhibits tumor growth in an IGF-1R-driven xenograft mouse model, with 100% TGI and 55% regression at a dose of 75 mg/kg and 60% TGI and no regression at a dose of 25 mg/kg. OSI-906 administration induces different elimination half-lives of itself in dog, rat and mice, the elimination half-lives are 1.18 hours, 2.64 hours and 2.14 hours, respectively. OSI-906 administration at different single dose once-daily in femal Sprague-Dawley rat and femal CD-1 mouse reveal that the Vmax is not dose-proportional to OSI-906 dose. OSI-906 elevates the blood glucose levels at a dose of 25 mg/kg after 12 days administration. OSI-906 administration at a single dose of 75 mg/kg in IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model achieve maximal inhibition of IGF-1R phosphorylation (80%) between 4 and 24 hours with plasma drug concentrations of 26.6-4.77 μM. [1] OSI-906 administered as a single dose of at 60 mg/kg in NCI-H292 xenografts mice inhibits uptake of glucose at 2, 4, and 24 hours post-treatment in vivo. OSI-906 inhibits the growth of tumors in NCI-H292 xenograft mouse model. [2] | |
|---|---|---|
| 動物実験 | 動物モデル | IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model |
| 投与量 | 25 mg / kg and 75 mg / kg | |
| 投与経路 | Orally administrated at once-daily oral dose for 14 days | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | 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 |
化学情報
| 分子量 | 421.49 | 化学式 | C26H23N5O |
| CAS No. | 867160-71-2 | SDF | Download Linsitinib (OSI-906) SDFをダウンロードする |
| Smiles | CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O | ||
| 保管 | |||
|
In vitro |
DMSO : 84 mg/mL ( (199.29 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 : Insoluble Ethanol : Insoluble |
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。
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
* 必須
よくある質問（FAQ）
質問1:
Does the inhibitor dissolve in the vehicle (30% PEG400/0.5%Tween 80/5% propylene glycol) or is it a suspension?
回答
OSI-906 in 30% PEG400/0.5%Tween 80/5% propylene glycol is a suspension.
Tags: Linsitinib (OSI-906)を買う | Linsitinib (OSI-906) ic50 | Linsitinib (OSI-906)供給者 | Linsitinib (OSI-906)を購入する | Linsitinib (OSI-906)費用 | Linsitinib (OSI-906)生産者 | オーダーLinsitinib (OSI-906) | Linsitinib (OSI-906)化学構造 | Linsitinib (OSI-906)分子量 | Linsitinib (OSI-906)代理店
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