Linsitinib (OSI-906)
Linsitinib (OSI-906)是一种选择性IGF-1R抑制剂，在无细胞试验中IC50为35 nM；对InsR抑制作用适中，IC50为75 nM，对Abl，ALK，BTK，EGFR， FGFR1/2，PKA等没有抑制活性。Phase 3。
Linsitinib (OSI-906) Chemical Structure
CAS: 867160-71-2
产品质控
批次：
纯度：
99.99%
99.99
常与Linsitinib (OSI-906)一起在实验中被使用的化合物
Linsitinib和Osimertinib联合使用可抑制AXL低表达EGFR突变的NSCLC细胞系（包括HCC4006/HCC827/H3255细胞）的活力。
Gefitinib抑制HCC827细胞中HIF-1α和VEGF的表达，Linsitinib抑制H1975细胞中VEGF的产生。
Linsitinib和Lapatinib联合使用可显着抑制裸鼠KYSE450异种移植模型中异种移植物的生长。
Linsitinib和Afatinib联合治疗对H1975异种移植物中的肿瘤生长显示出不仅仅是相加效应。
Linsitinib和Aspirin抑制干细胞样结肠癌细胞的生长，降低CD133/CD44/CD24的表达，并上调CDX2/PTEN的表达。
Linsitinib (OSI-906)相关产品
| 相关靶点 | Insulin Receptor | 点击展开 |
|---|---|---|
| 相关产品 | NVP-AEW541 BMS-754807 Picropodophyllin (PPP) GSK1904529A BMS-536924 AG-1024 NVP-ADW742 NT157 PQ 401 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库 细胞周期化合物库 血管生成相关化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Linsitinib (OSI-906)是一种选择性IGF-1R抑制剂，在无细胞试验中IC50为35 nM；对InsR抑制作用适中，IC50为75 nM，对Abl，ALK，BTK，EGFR， FGFR1/2，PKA等没有抑制活性。Phase 3。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | OSI-906 抑制IGF-IR自磷酸化和下游信号蛋白AKT, ERK1/2和S6激酶的激活，IC50为0.028到 0.13 μM。OSI-906通过与C-螺旋相互作用而使靶点蛋白形成中间结构形态。OSI-906作用于肝脏微粒体，具有良好的代谢稳定性。OSI-906浓度为1μM时，完全抑制IR 和IGF-IR磷酸化。OSI-906抑制一些肿瘤细胞系增殖，包括非小细胞肺癌和结肠直肠癌(CRC)肿瘤细胞系，EC50为0.021到 0.810 μM。[1] | |||
|---|---|---|---|---|
| 激酶实验 | 蛋白激酶生化实验 | |||
| 通过以ELISA为基础的检测法(IGF-IR, IR, EGFR 和 KDR)或使用100 µM ATP的放射检测法进行蛋白激酶检测实验。在内部ELISA检测实验中，使用聚 (Glu:Tyr)作为底物，结合到96孔实验板表面，使用辣根过氧化物酶标记的自磷酸化抗体测定磷酸化。使用ABTS作为过氧化物酶底物，通过在405/490 nm处测量吸光度而测定结合的抗体。所有实验使用纯化的重组激酶催化域。在昆虫细胞中，人类IGF-IR或EGFR的重组酶表达作为NH2-末端谷胱甘肽S-转移酶融合蛋白，且在内部纯化。通过抑制百分数对log10药品浓度的S型剂量-反应曲线测定IC50值。进行内部实验需重复进行实验，除非另有说明，取三次测量的最小值。 | ||||
| 细胞实验 | 细胞系 | MCF7, NCI-H292, Colo-205, HT29, H358, H1703, BxPC3, A673, SW620, DU4475, HepG2 和Hepa-1, RKO 3T3/hulGF-IR, H292 细胞 | ||
| 浓度 | 0.02-0.8 μM | |||
| 孵育时间 | 3天 | |||
| 方法 | 为了测定细胞增殖，细胞接种在含FCS 10%的合适培养基上，在不同浓度OSI-906存在时，温育3天。通过细胞内ATP含量的荧光量化，使用CellTiterGlo测定抑制细胞生长的情况。数据作为衡量最大增殖的一部分，通过在不同浓度 OSI-906存在时的细胞密度除以对照组（只用DMSO处理）细胞密度。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-EGFR / EGFR / p-IGF1R / IGF1R / p-IRS1 / IRS1 / p-ERK / ERK / p-AKT / AKT p-IGF1R / IGF1R / p-mTOR / mTOR cleaved caspase-3 / cleaved PARP pSrc(Y416) / Src p-STAT3(Y705) / STAT3 pS6 / S6 |
|
26052929 | |
| Immunofluorescence | FoxO1 |
|
27535223 | |
| Growth inhibition assay | Cell viability |
|
26136493 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | OSI-906 作用于IGF-IR驱动的移植瘤鼠模型，抑制肿瘤生长，按 75 mg / kg剂量处理，导致100% TGI和 55% 衰退，按25 mg/kg剂量处理，导致 60% TGI，没有衰退。OSI-906处理犬，大鼠和小鼠，诱导不同的消除半衰期，消除半衰期分别为1.18 小时, 2.64小时 和2.14小时。OSI-906按不同剂量单独处理给药雌性Sprague-Dawley 大鼠和雌性CD-1小鼠，每天一次，Vmax值与OSI-906 剂量不成比例。OSI-906 按 25 mg/kg剂量处理12天，提高血糖值。OSI-906按75 mg/kg 剂量单独处理IGF-IR-驱动的人全长人类IGF-IR (LISN)移植鼠模型，在4 和24小时间最大程度抑制IGF-IR磷酸化(80%)，血浆药物浓度为26.6-4.77 μM。[1] OSI-906 按60 mg/kg剂量单独作用于NCI-H292 移植鼠，处理2，4，24小时，抑制糖吸收。OSI-906 作用于NCI-H292移植鼠模型，抑制肿瘤生长。[2] | |
|---|---|---|
| 动物实验 | Animal Models | IGF-IR驱动的全长人类IGF-IR (LISN) 移植小鼠模型 |
| Dosages | 25 mg/kg和75 mg/kg | |
| Administration | 口服处理，每天一次，持续14天 | |
| 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 |
化学信息&溶解度
| 分子量 | 421.49 | 分子式 | C26H23N5O |
| CAS号 | 867160-71-2 | SDF | Download Linsitinib (OSI-906) SDF |
| Smiles | CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 84 mg/mL ( (199.29 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
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如果有其他问题，请给我们留言。
* 必填项
常见问题及建议解决方法
问题 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.
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