solo per uso di ricerca
N. Cat.S2827
| Target correlati | PI3K Akt GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK |
|---|---|
| Altro mTOR Inibitori | Torin 2 AZD8055 Ridaforolimus (Deforolimus, MK-8669) Sapanisertib (MLN0128, INK-128) Torkinib (PP242) MHY1485 Vistusertib (AZD2014) KU-0063794 OSI-027 3BDO |
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dell'attività | PMID |
|---|---|---|---|---|---|---|
| ETK-1 | Growth Inhibition Assay | IC50=0.000306 μM | SANGER | |||
| OCUB-M | Growth Inhibition Assay | IC50=0.00194 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=0.00225 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=0.00242 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=0.00284 μM | SANGER | |||
| RL95-2 | Growth Inhibition Assay | IC50=0.0032 μM | SANGER | |||
| BL-70 | Growth Inhibition Assay | IC50=0.00337 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=0.00379 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=0.00634 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=0.00651 μM | SANGER | |||
| BL-41 | Growth Inhibition Assay | IC50=0.00696 μM | SANGER | |||
| MRK-nu-1 | Growth Inhibition Assay | IC50=0.00707 μM | SANGER | |||
| EW-1 | Growth Inhibition Assay | IC50=0.00749 μM | SANGER | |||
| EVSA-T | Growth Inhibition Assay | IC50=0.00892 μM | SANGER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=0.00929 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=0.00984 μM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=0.01007 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=0.01083 μM | SANGER | |||
| NALM-6 | Growth Inhibition Assay | IC50=0.01102 μM | SANGER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=0.01137 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=0.01192 μM | SANGER | |||
| KALS-1 | Growth Inhibition Assay | IC50=0.01198 μM | SANGER | |||
| OPM-2 | Growth Inhibition Assay | IC50=0.0129 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=0.01296 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=0.01319 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=0.01359 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=0.01392 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=0.01395 μM | SANGER | |||
| PSN1 | Growth Inhibition Assay | IC50=0.01409 μM | SANGER | |||
| SK-LMS-1 | Growth Inhibition Assay | IC50=0.01413 μM | SANGER | |||
| LS-411N | Growth Inhibition Assay | IC50=0.01439 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=0.01451 μM | SANGER | |||
| ACN | Growth Inhibition Assay | IC50=0.015 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=0.01533 μM | SANGER | |||
| CMK | Growth Inhibition Assay | IC50=0.01543 μM | SANGER | |||
| GB-1 | Growth Inhibition Assay | IC50=0.01553 μM | SANGER | |||
| KE-37 | Growth Inhibition Assay | IC50=0.01573 μM | SANGER | |||
| no-10 | Growth Inhibition Assay | IC50=0.01584 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=0.01622 μM | SANGER | |||
| HEL | Growth Inhibition Assay | IC50=0.0164 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=0.01646 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=0.01774 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=0.01818 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=0.01844 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=0.02137 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=0.02167 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.02203 μM | SANGER | |||
| SW872 | Growth Inhibition Assay | IC50=0.02247 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=0.02261 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=0.02323 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=0.0233 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=0.02337 μM | SANGER | |||
| TE-11 | Growth Inhibition Assay | IC50=0.02372 μM | SANGER | |||
| KURAMOCHI | Growth Inhibition Assay | IC50=0.02414 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=0.02426 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=0.02469 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=0.02488 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=0.0255 μM | SANGER | |||
| MZ7-mel | Growth Inhibition Assay | IC50=0.02609 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=0.02633 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=0.0265 μM | SANGER | |||
| GR-ST | Growth Inhibition Assay | IC50=0.02655 μM | SANGER | |||
| MC116 | Growth Inhibition Assay | IC50=0.0268 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=0.0275 μM | SANGER | |||
| ATN-1 | Growth Inhibition Assay | IC50=0.02789 μM | SANGER | |||
| MFH-ino | Growth Inhibition Assay | IC50=0.02812 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=0.02815 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=0.02871 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=0.02872 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=0.02917 μM | SANGER | |||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.02996 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=0.03094 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=0.03097 μM | SANGER | |||
| CESS | Growth Inhibition Assay | IC50=0.03099 μM | SANGER | |||
| GAK | Growth Inhibition Assay | IC50=0.03186 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.03226 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=0.03311 μM | SANGER | |||
| CCRF-CEM | Growth Inhibition Assay | IC50=0.03371 μM | SANGER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=0.03448 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=0.03556 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=0.03582 μM | SANGER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.03622 μM | SANGER | |||
| EB-3 | Growth Inhibition Assay | IC50=0.03643 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=0.03691 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=0.03759 μM | SANGER | |||
| CP67-MEL | Growth Inhibition Assay | IC50=0.03759 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=0.0379 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=0.03854 μM | SANGER | |||
| HCE-4 | Growth Inhibition Assay | IC50=0.03855 μM | SANGER | |||
| LC-1F | Growth Inhibition Assay | IC50=0.03989 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=0.04019 μM | SANGER | |||
| SJSA-1 | Growth Inhibition Assay | IC50=0.04188 μM | SANGER | |||
| Daudi | Growth Inhibition Assay | IC50=0.04225 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=0.04246 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=0.04361 μM | SANGER | |||
| TE-15 | Growth Inhibition Assay | IC50=0.04435 μM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=0.04561 μM | SANGER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=0.04629 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=0.04776 μM | SANGER | |||
| HCC1599 | Growth Inhibition Assay | IC50=0.04879 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=0.04949 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=0.04956 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=0.05271 μM | SANGER | |||
| IST-SL2 | Growth Inhibition Assay | IC50=0.05362 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=0.0573 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=0.05763 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.05799 μM | SANGER | |||
| KINGS-1 | Growth Inhibition Assay | IC50=0.05803 μM | SANGER | |||
| HC-1 | Growth Inhibition Assay | IC50=0.05827 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=0.05938 μM | SANGER | |||
| LS-123 | Growth Inhibition Assay | IC50=0.05942 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=0.06225 μM | SANGER | |||
| SNB75 | Growth Inhibition Assay | IC50=0.06341 μM | SANGER | |||
| SR | Growth Inhibition Assay | IC50=0.06374 μM | SANGER | |||
| LOUCY | Growth Inhibition Assay | IC50=0.06394 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=0.06403 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=0.0642 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=0.06548 μM | SANGER | |||
| KLE | Growth Inhibition Assay | IC50=0.06584 μM | SANGER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=0.06598 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=0.06605 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=0.0678 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=0.06893 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=0.06995 μM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=0.07173 μM | SANGER | |||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.07212 μM | SANGER | |||
| ARH-77 | Growth Inhibition Assay | IC50=0.07278 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=0.07549 μM | SANGER | |||
| PF-382 | Growth Inhibition Assay | IC50=0.07569 μM | SANGER | |||
| KM12 | Growth Inhibition Assay | IC50=0.0764 μM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=0.07658 μM | SANGER | |||
| RPMI-8402 | Growth Inhibition Assay | IC50=0.07789 μM | SANGER | |||
| OMC-1 | Growth Inhibition Assay | IC50=0.07804 μM | SANGER | |||
| HT | Growth Inhibition Assay | IC50=0.08 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=0.08055 μM | SANGER | |||
| KNS-42 | Growth Inhibition Assay | IC50=0.08203 μM | SANGER | |||
| BC-3 | Growth Inhibition Assay | IC50=0.08204 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=0.08296 μM | SANGER | |||
| NCI-H23 | Growth Inhibition Assay | IC50=0.0844 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=0.08696 μM | SANGER | |||
| LC4-1 | Growth Inhibition Assay | IC50=0.08738 μM | SANGER | |||
| SIG-M5 | Growth Inhibition Assay | IC50=0.08904 μM | SANGER | |||
| LP-1 | Growth Inhibition Assay | IC50=0.08938 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=0.09016 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=0.0912 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=0.09153 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=0.09165 μM | SANGER | |||
| RXF393 | Growth Inhibition Assay | IC50=0.09462 μM | SANGER | |||
| NB5 | Growth Inhibition Assay | IC50=0.09625 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=0.09741 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=0.09825 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=0.09833 μM | SANGER | |||
| L-428 | Growth Inhibition Assay | IC50=0.1032 μM | SANGER | |||
| ST486 | Growth Inhibition Assay | IC50=0.10606 μM | SANGER | |||
| SK-MM-2 | Growth Inhibition Assay | IC50=0.10709 μM | SANGER | |||
| COR-L279 | Growth Inhibition Assay | IC50=0.10832 μM | SANGER | |||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=0.10843 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=0.10918 μM | SANGER | |||
| HCE-T | Growth Inhibition Assay | IC50=0.1094 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=0.11119 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=0.11273 μM | SANGER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=0.11394 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=0.11529 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=0.11598 μM | SANGER | |||
| NB17 | Growth Inhibition Assay | IC50=0.11652 μM | SANGER | |||
| LB647-SCLC | Growth Inhibition Assay | IC50=0.11705 μM | SANGER | |||
| CAL-148 | Growth Inhibition Assay | IC50=0.118 μM | SANGER | |||
| K052 | Growth Inhibition Assay | IC50=0.11851 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=0.12233 μM | SANGER | |||
| KARPAS-422 | Growth Inhibition Assay | IC50=0.12432 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=0.12515 μM | SANGER | |||
| SCC-3 | Growth Inhibition Assay | IC50=0.12851 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=0.12975 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=0.13086 μM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=0.1313 μM | SANGER | |||
| U-266 | Growth Inhibition Assay | IC50=0.13245 μM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=0.13535 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=0.13587 μM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=0.13596 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=0.13746 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=0.13953 μM | SANGER | |||
| SCH | Growth Inhibition Assay | IC50=0.13974 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=0.14104 μM | SANGER | |||
| MDA-MB-134-VI | Growth Inhibition Assay | IC50=0.14252 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=0.14719 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=0.1492 μM | SANGER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=0.15539 μM | SANGER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=0.16076 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.16101 μM | SANGER | |||
| IMR-5 | Growth Inhibition Assay | IC50=0.16483 μM | SANGER | |||
| Calu-6 | Growth Inhibition Assay | IC50=0.16537 μM | SANGER | |||
| NCI-H1882 | Growth Inhibition Assay | IC50=0.16728 μM | SANGER | |||
| NCI-H446 | Growth Inhibition Assay | IC50=0.16891 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=0.1802 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=0.18121 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=0.18436 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=0.18628 μM | SANGER | |||
| NCI-H748 | Growth Inhibition Assay | IC50=0.18911 μM | SANGER | |||
| COLO-829 | Growth Inhibition Assay | IC50=0.20673 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=0.2073 μM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=0.21718 μM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=0.22045 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=0.22228 μM | SANGER | |||
| TALL-1 | Growth Inhibition Assay | IC50=0.22921 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=0.22962 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=0.2351 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=0.23993 μM | SANGER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=0.24316 μM | SANGER | |||
| DG-75 | Growth Inhibition Assay | IC50=0.26195 μM | SANGER | |||
| D-336MG | Growth Inhibition Assay | IC50=0.26557 μM | SANGER | |||
| KMOE-2 | Growth Inhibition Assay | IC50=0.27538 μM | SANGER | |||
| NB1 | Growth Inhibition Assay | IC50=0.27926 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=0.27989 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=0.28479 μM | SANGER | |||
| RPMI-6666 | Growth Inhibition Assay | IC50=0.2884 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=0.28985 μM | SANGER | |||
| BT-474 | Growth Inhibition Assay | IC50=0.29334 μM | SANGER | |||
| COLO-668 | Growth Inhibition Assay | IC50=0.29429 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=0.29689 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=0.29905 μM | SANGER | |||
| L-540 | Growth Inhibition Assay | IC50=0.30081 μM | SANGER | |||
| MOLT-13 | Growth Inhibition Assay | IC50=0.30183 μM | SANGER | |||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=0.30205 μM | SANGER | |||
| NCI-H64 | Growth Inhibition Assay | IC50=0.30331 μM | SANGER | |||
| CP66-MEL | Growth Inhibition Assay | IC50=0.31415 μM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=0.32188 μM | SANGER | |||
| NCI-H2196 | Growth Inhibition Assay | IC50=0.33036 μM | SANGER | |||
| MHH-CALL-2 | Growth Inhibition Assay | IC50=0.33468 μM | SANGER | |||
| HCC2157 | Growth Inhibition Assay | IC50=0.33954 μM | SANGER | |||
| LS-1034 | Growth Inhibition Assay | IC50=0.36388 μM | SANGER | |||
| BOKU | Growth Inhibition Assay | IC50=0.37199 μM | SANGER | |||
| GDM-1 | Growth Inhibition Assay | IC50=0.37234 μM | SANGER | |||
| TGW | Growth Inhibition Assay | IC50=0.37453 μM | SANGER | |||
| SNU-C1 | Growth Inhibition Assay | IC50=0.38215 μM | SANGER | |||
| LS-513 | Growth Inhibition Assay | IC50=0.39071 μM | SANGER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=0.39971 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=0.40177 μM | SANGER | |||
| EKVX | Growth Inhibition Assay | IC50=0.44461 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=0.464 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=0.46768 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=0.47227 μM | SANGER | |||
| NCI-H187 | Growth Inhibition Assay | IC50=0.4784 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=0.50055 μM | SANGER | |||
| NCI-H69 | Growth Inhibition Assay | IC50=0.50247 μM | SANGER | |||
| NCI-H1694 | Growth Inhibition Assay | IC50=0.50697 μM | SANGER | |||
| CA46 | Growth Inhibition Assay | IC50=0.50917 μM | SANGER | |||
| EHEB | Growth Inhibition Assay | IC50=0.51193 μM | SANGER | |||
| NCCIT | Growth Inhibition Assay | IC50=0.54321 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=0.54962 μM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=0.55296 μM | SANGER | |||
| MC-CAR | Growth Inhibition Assay | IC50=0.55431 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=0.56172 μM | SANGER | |||
| NCI-H524 | Growth Inhibition Assay | IC50=0.58748 μM | SANGER | |||
| NCI-H1963 | Growth Inhibition Assay | IC50=0.6258 μM | SANGER | |||
| SU-DHL-1 | Growth Inhibition Assay | IC50=0.64526 μM | SANGER | |||
| NCI-H1522 | Growth Inhibition Assay | IC50=0.64883 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=0.6535 μM | SANGER | |||
| D-263MG | Growth Inhibition Assay | IC50=0.66101 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=0.68104 μM | SANGER | |||
| NCI-H1417 | Growth Inhibition Assay | IC50=0.69711 μM | SANGER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=0.77236 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.78235 μM | SANGER | |||
| IST-SL1 | Growth Inhibition Assay | IC50=0.85825 μM | SANGER | |||
| COLO-824 | Growth Inhibition Assay | IC50=0.87835 μM | SANGER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=0.90958 μM | SANGER | |||
| NCI-H719 | Growth Inhibition Assay | IC50=0.96657 μM | SANGER | |||
| SF539 | Growth Inhibition Assay | IC50=0.98396 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=0.98663 μM | SANGER | |||
| A253 | Growth Inhibition Assay | IC50=0.98885 μM | SANGER | |||
| TE-441-T | Growth Inhibition Assay | IC50=1.0435 μM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=1.11354 μM | SANGER | |||
| CPC-N | Growth Inhibition Assay | IC50=1.15888 μM | SANGER | |||
| NCI-H2107 | Growth Inhibition Assay | IC50=1.17261 μM | SANGER | |||
| ECC4 | Growth Inhibition Assay | IC50=1.18693 μM | SANGER | |||
| NCI-H2141 | Growth Inhibition Assay | IC50=1.19299 μM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=1.32928 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=1.3304 μM | SANGER | |||
| LU-165 | Growth Inhibition Assay | IC50=1.45467 μM | SANGER | |||
| Raji | Growth Inhibition Assay | IC50=1.47259 μM | SANGER | |||
| EW-24 | Growth Inhibition Assay | IC50=1.54619 μM | SANGER | |||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=1.56551 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=1.64877 μM | SANGER | |||
| SCLC-21H | Growth Inhibition Assay | IC50=1.66651 μM | SANGER | |||
| SIMA | Growth Inhibition Assay | IC50=1.68233 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=1.70765 μM | SANGER | |||
| REH | Growth Inhibition Assay | IC50=1.71078 μM | SANGER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=1.93551 μM | SANGER | |||
| DMS-153 | Growth Inhibition Assay | IC50=1.9759 μM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=2.20878 μM | SANGER | |||
| NCI-H345 | Growth Inhibition Assay | IC50=2.61905 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=2.75381 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=2.95394 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=3.65396 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=3.71688 μM | SANGER | |||
| D-283MED | Growth Inhibition Assay | IC50=3.7587 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=4.11485 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=4.18898 μM | SANGER | |||
| NCI-H2081 | Growth Inhibition Assay | IC50=4.29174 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=4.43191 μM | SANGER | |||
| P31-FUJ | Growth Inhibition Assay | IC50=4.45019 μM | SANGER | |||
| DMS-79 | Growth Inhibition Assay | IC50=4.93183 μM | SANGER | |||
| KASUMI-1 | Growth Inhibition Assay | IC50=4.97509 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=5.25014 μM | SANGER | |||
| LAN-6 | Growth Inhibition Assay | IC50=5.51736 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=5.56029 μM | SANGER | |||
| JVM-2 | Growth Inhibition Assay | IC50=5.67092 μM | SANGER | |||
| U-87-MG | Growth Inhibition Assay | IC50=5.89964 μM | SANGER | |||
| SHP-77 | Growth Inhibition Assay | IC50=5.94928 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition Assay | IC50=6.27013 μM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=6.39924 μM | SANGER | |||
| WSU-NHL | Growth Inhibition Assay | IC50=6.51609 μM | SANGER | |||
| CAS-1 | Growth Inhibition Assay | IC50=7.09749 μM | SANGER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=8.23152 μM | SANGER | |||
| ES5 | Growth Inhibition Assay | IC50=9.52286 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=9.95902 μM | SANGER | |||
| NCI-H2171 | Growth Inhibition Assay | IC50=10.5927 μM | SANGER | |||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=11.3718 μM | SANGER | |||
| NCI-H1395 | Growth Inhibition Assay | IC50=12.2699 μM | SANGER | |||
| NCI-H1436 | Growth Inhibition Assay | IC50=13.3195 μM | SANGER | |||
| RCC10RGB | Growth Inhibition Assay | IC50=13.3221 μM | SANGER | |||
| SW684 | Growth Inhibition Assay | IC50=13.9797 μM | SANGER | |||
| NCI-H1650 | Growth Inhibition Assay | IC50=15.0447 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=15.2021 μM | SANGER | |||
| EC-GI-10 | Growth Inhibition Assay | IC50=15.8644 μM | SANGER | |||
| CHP-126 | Growth Inhibition Assay | IC50=17.1918 μM | SANGER | |||
| NCI-H226 | Growth Inhibition Assay | IC50=18.0403 μM | SANGER | |||
| NCI-H1838 | Growth Inhibition Assay | IC50=20.1848 μM | SANGER | |||
| EW-11 | Growth Inhibition Assay | IC50=24.2718 μM | SANGER | |||
| EB2 | Growth Inhibition Assay | IC50=31.5318 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=43.9229 μM | SANGER | |||
| U-698-M | Growth Inhibition Assay | IC50=48.8671 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=49.3893 μM | SANGER | |||
| PC3 | Function assay | Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting, EC50 = 1.8 μM. | 21322566 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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 | |||
| 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 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | |||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
| Peso molecolare | 607.62 | Formula | C35H28F3N5O2 |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 1222998-36-8 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | N/A | Smiles | CCC(=O)N1CCN(CC1)C2=C(C=C(C=C2)N3C(=O)C=CC4=CN=C5C=CC(=CC5=C43)C6=CC7=CC=CC=C7N=C6)C(F)(F)F | ||
|
In vitro |
DMSO
: 3 mg/mL
(4.93 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.
| Targets/IC50/Ki |
mTORC1
(Cell-free assay) 2 nM
mTOR
(Cell-free assay) 4.32 nM
DNA-PK
(Cell-free assay) 6.34 nM
mTORC2
(Cell-free assay) 10 nM
p110γ
(Cell-free assay) 171 nM
C2α
(Cell-free assay) 176 nM
|
|---|---|
| In vitro |
Torin1 inibisce la fosforilazione dei substrati di mTORC1 e mTORC2 nelle cellule a concentrazioni rispettivamente di 2 e 10 nM. Inoltre, Torin1 mostra una selettività 1000 volte superiore per mTOR rispetto a PI3K (EC50 = 1800 nM) e una selettività di legame 100 volte superiore rispetto ad altre 450 protein chinasi. Torin1 provoca l'arresto del ciclo cellulare attraverso un meccanismo resistente alla rapamicina che è anche indipendente da mTORC2. Torin1 interrompe i fenotipi dipendenti da mTORC1 più completamente della rapamicina. Le funzioni di mTORC1 resistenti alla rapamicina sono necessarie per la traduzione cap-dipendente. In uno studio recente, è stato riportato che Torin1 aumenta la secrezione di neurotensina e l'espressione genica attraverso l'attivazione della via MEK/ERK/c-Jun nella linea cellulare endocrina umana BON.
|
| Saggio chinasico |
Saggi chinasici in vitro di mTORC1 e mTORC2
|
|
Per produrre mTORC1 solubile, vengono generate linee cellulari HEK-293T che esprimono stabilmente Raptor con tag FLAG N-terminale utilizzando retrovirus MSCV pseudotipato con virus della stomatite vescicolare G. Per mTORC2, vengono generate cellule HeLa simili che esprimono stabilmente Protor-1 con tag FLAG N-terminale. Entrambi i complessi vengono purificati lisando le cellule in 50 mm HEPES, pH 7,4, 10 mm pirofosfato di sodio, 10 mm β-glicerofosfato di sodio, 100 mm NaCl, 2 mm EDTA, 0,3% CHAPS. Le cellule vengono lisate a 4 °C per 30 minuti, e la frazione insolubile viene rimossa mediante microcentrifugazione a 13.000 rpm per 10 minuti. I surnatanti vengono incubati con agarosio di anticorpo monoclonale FLAG-M2 per 1 ora e poi lavati tre volte con tampone di lisi e una volta con tampone di lisi contenente una concentrazione finale di 0,5 M NaCl. Il mTORC1 purificato viene eluito con 100 μg/mL di peptide 3×FLAG in 50 mm HEPES, pH 7,4, 100 mm NaCl. L'eluato può essere alicottato e conservato a -80 °C. I substrati S6K1 e Akt1 vengono purificati. I saggi chinasici vengono eseguiti per 20 minuti a 30 °C in un volume finale di 20 μL costituito dal tampone chinasico (25 mm HEPES, pH 7,4, 50 mm KCl, 10 mm MgCl2, 500 μm ATP) e 150 ng di S6K1 o Akt1 inattivi come substrati. Le reazioni vengono interrotte dall'aggiunta di 80 μL di tampone campione e bollite per 5 minuti. I campioni vengono successivamente analizzati mediante SDS-PAGE e immunoblotting.
|
|
| In vivo |
Torin1 è efficace a una dose di 20 mg/kg in un modello di xenotrapianto U87MG e dimostra una buona inibizione farmacodinamica degli effettori a valle di mTOR nei tessuti tumorali e periferici.
|
Riferimenti |
|
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | ATF4 / p-S6K(T389) / S6K / p-eIF2α(S51) / eIF2α / 4EBP1 / eIF3b LC3 / p62 / PARP / pAKT(S473) / p4EBP1(S65) / pS6K1(T389) / pS6(S235/236) p-mTOR(S2481) / mTOR / rictor / Sin1 / p-Akt S473 / p-Akt T450 / p-Akt T308 / p-S6K1 T389 / S6K1 Vinculin / p-S6 |
|
28494858 |
| Immunofluorescence | lipin-1 |
|
28347999 |
| Growth inhibition assay | Cell viability |
|
28757207 |
Domanda 1:
How to re-constitute it for i.p. administration?
Risposta:
It can be dissolved in 5% DMSO/30% PEG 300/ddH2O at 0.25 mg/ml clearly, and in 10% DMSO/corn oil at 0.5 mg/ml, it is also a clear solution.