- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- 化合物ライブラリー
- 抗体
- 新製品
- お問い合わせ
AZD8055
AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.
CAS No. 1009298-09-2
文献中Selleckの製品使用例（253）
製品安全説明書
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AZD8055関連製品
シグナル伝達経路
mTOR阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| H1048 | Apoptosis Assay | 500 nM | 72 h | nhances ABT-263–induced apoptosis | 25737542 |
| H86 | Apoptosis Assay | 500 nM | 72 h | nhances ABT-263–induced apoptosis | 25737542 |
| H196 | Apoptosis Assay | 500 nM | 72 h | nhances ABT-263–induced apoptosis | 25737542 |
| H446 | Apoptosis Assay | 500 nM | 72 h | nhances ABT-263–induced apoptosis | 25737542 |
| OCI/AML3 | Growth Inhibition Assay | 0.2 μM | 48 h | enhances cell growth inhibition induced by selumetinib | 24739393 |
| U937 | Growth Inhibition Assay | 0.2 μM | 48 h | enhances cell growth inhibition induced by selumetinib | 24739393 |
| MOLM13 | Growth Inhibition Assay | 0.2 μM | 48 h | enhances cell growth inhibition induced by selumetinib | 24739393 |
| MCF7 | Growth Inhibition Assay | 20 nM | 72 h | reduces the PELP1-mediated increase in cell viability | 24688046 |
| 293T | Function Assay | 20 nM | 3 h | disrupts Akt-mediated TIF-IA stability, translocation, and activity | 24363449 |
| SW620 | Growth Inhibition Assay | 0.001-10μM | 24 h | inhibits the cell proliferation as the concentration rises | 24363449 |
| Huh7 | Growth Inhibition Assay | 5-100 nM | 0-24 h | increases cell death in a concentration- and time-dependent manner | 24297300 |
| Hep3B | Growth Inhibition Assay | 5-100 nM | 0-24 h | increases cell death in a concentration- and time-dependent manner | 24297300 |
| Huh7 | Function Assay | 100 nM | 12 h | induces autophagy | 24297300 |
| L3.6pl | Growth Inhibition Assay | 1 μM | 72 h | inhibits the cell growth combined with BMS-777607 | 24233399 |
| TE671 | Apoptosis Assay | 1 μM | 48 h | increases cell apoptosis induced by ABT-737 | 24133218 |
| RD | Apoptosis Assay | 1 μM | 48 h | increases cell apoptosis induced by ABT-737 | 24133218 |
| RMS13 | Apoptosis Assay | 1 μM | 48 h | increases cell apoptosis induced by ABT-737 | 24133218 |
| RH30 | Apoptosis Assay | 1 μM | 48 h | increases cell apoptosis induced by ABT-737 | 24133218 |
| Hep-2 | Growth Inhibition Assay | 0.01-1 μM | 12-96 h | increases cell death in a concentration- and time-dependent manner | 24103749 |
| SCC-9 | Growth Inhibition Assay | 0.01-1 μM | 12-96 h | increases cell death in a concentration- and time-dependent manner | 24103749 |
| Hep-2 | Function Assay | 0.1/0.5 μM | 24 h | blocks mTORC1 and mTORC2 activation | 24103749 |
| SCC-9 | Function Assay | 0.1/0.5 μM | 24 h | blocks mTORC1 and mTORC2 activation | 24103749 |
| PANC-1 | Apoptosis Assay | 500 nM | 48 h | sensitizes pancreatic cancer cells to radiotherapy | 23886294 |
| RMG2 | Apoptosis Assay | 1-1000 nM | 72 h | inhibits the cell viability concentration dependently | 23615631 |
| HAC2 | Apoptosis Assay | 1-1000 nM | 72 h | inhibits the cell viability concentration dependently | 23615631 |
| HT-29 | Apoptosis Assay | 1 μM | 72 h | attenuates 5-FU-induced cell death | 21949121 |
| DLD1 | Apoptosis Assay | 1 μM | 72 h | attenuates 5-FU-induced cell death | 21949121 |
| HT-29 | Function Assay | 1 μM | 72 h | induces autophagy to confer cytoprotection | 21949121 |
| DLD1 | Function Assay | 1 μM | 72 h | induces autophagy to confer cytoprotection | 21949121 |
| H838 | Function Assay | 1 μM | 48 h | induces cell autophagy | 20364113 |
| H838 | Growth Inhibition Assay | 0-3 μM | 72 h | induces growth inhibition and autophagy | 20028854 |
| A549 | Growth Inhibition Assay | 0-3 μM | 72 h | induces growth inhibition and autophagy | 20028854 |
| TFK-1 | Growth Inhibition Assay | 72 h | IC50=47 nM | 25152244 | |
| EGI-1 | Growth Inhibition Assay | 72 h | IC50=53 nM | 25152244 | |
| U87-MG | Growth Inhibition Assay | 72 h | GI50 = 79 nM | 24249640 | |
| Mewo | Growth Inhibition Assay | IC50=1.09248 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=1.08934 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=1.08431 μM | SANGER | ||
| KOSC-2 | Growth Inhibition Assay | IC50=1.08021 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=1.0794 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=1.06726 μM | SANGER | ||
| SCH | Growth Inhibition Assay | IC50=1.0345 μM | SANGER | ||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=1.03406 μM | SANGER | ||
| PANC-03-27 | Growth Inhibition Assay | IC50=1.03141 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=1.02963 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=1.02827 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=1.02675 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=1.01364 μM | SANGER | ||
| SW13 | Growth Inhibition Assay | IC50=0.98392 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=0.9736 μM | SANGER | ||
| NCI-H1792 | Growth Inhibition Assay | IC50=0.97101 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=0.96773 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=0.96198 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=0.95924 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=0.94277 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=0.93845 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=0.93677 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=0.93256 μM | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=0.92922 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=0.92897 μM | SANGER | ||
| UACC-893 | Growth Inhibition Assay | IC50=0.92855 μM | SANGER | ||
| C-33-A | Growth Inhibition Assay | IC50=0.90442 μM | SANGER | ||
| NCI-H1573 | Growth Inhibition Assay | IC50=0.90229 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=0.89372 μM | SANGER | ||
| BxPC-3 | Growth Inhibition Assay | IC50=0.88833 μM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=0.88734 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=0.88714 μM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=0.88395 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=0.88384 μM | SANGER | ||
| HCC1419 | Growth Inhibition Assay | IC50=0.86928 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=0.86817 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=0.86495 μM | SANGER | ||
| CAL-120 | Growth Inhibition Assay | IC50=0.86041 μM | SANGER | ||
| RPMI-8866 | Growth Inhibition Assay | IC50=0.85822 μM | SANGER | ||
| HCC1569 | Growth Inhibition Assay | IC50=0.85207 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=0.85121 μM | SANGER | ||
| RT-112 | Growth Inhibition Assay | IC50=0.84937 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=0.84092 μM | SANGER | ||
| MHH-ES-1 | Growth Inhibition Assay | IC50=0.83457 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=0.83116 μM | SANGER | ||
| PFSK-1 | Growth Inhibition Assay | IC50=0.83039 μM | SANGER | ||
| KYSE-450 | Growth Inhibition Assay | IC50=0.82725 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=0.82675 μM | SANGER | ||
| NCI-H2347 | Growth Inhibition Assay | IC50=0.82401 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=0.81911 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=0.81798 μM | SANGER | ||
| SNU-423 | Growth Inhibition Assay | IC50=0.81422 μM | SANGER | ||
| HPAF-II | Growth Inhibition Assay | IC50=0.80794 μM | SANGER | ||
| SN12C | Growth Inhibition Assay | IC50=0.80668 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=0.8021 μM | SANGER | ||
| CAL-62 | Growth Inhibition Assay | IC50=0.79924 μM | SANGER | ||
| OE33 | Growth Inhibition Assay | IC50=0.79914 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=0.7933 μM | SANGER | ||
| NCI-H650 | Growth Inhibition Assay | IC50=0.79144 μM | SANGER | ||
| NCI-H1563 | Growth Inhibition Assay | IC50=0.78926 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=0.78736 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=0.78482 μM | SANGER | ||
| KYSE-140 | Growth Inhibition Assay | IC50=0.78168 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=0.78029 μM | SANGER | ||
| LU-99A | Growth Inhibition Assay | IC50=0.77649 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=0.77057 μM | SANGER | ||
| DMS-273 | Growth Inhibition Assay | IC50=0.76922 μM | SANGER | ||
| NCI-H1623 | Growth Inhibition Assay | IC50=0.76261 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=0.75991 μM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=0.7597 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=0.75943 μM | SANGER | ||
| A375 | Growth Inhibition Assay | IC50=0.75193 μM | SANGER | ||
| HLE | Growth Inhibition Assay | IC50=0.74844 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=0.74736 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=0.74629 μM | SANGER | ||
| AsPC-1 | Growth Inhibition Assay | IC50=0.73795 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=0.73533 μM | SANGER | ||
| HTC-C3 | Growth Inhibition Assay | IC50=0.73172 μM | SANGER | ||
| OMC-1 | Growth Inhibition Assay | IC50=0.72738 μM | SANGER | ||
| MC-IXC | Growth Inhibition Assay | IC50=0.72718 μM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=0.72484 μM | SANGER | ||
| PC-3 | Growth Inhibition Assay | IC50=0.7223 μM | SANGER | ||
| EFM-19 | Growth Inhibition Assay | IC50=0.70847 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=0.70755 μM | SANGER | ||
| 22RV1 | Growth Inhibition Assay | IC50=0.70717 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=0.70691 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=0.7059 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=0.70319 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.70173 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.70063 μM | SANGER | ||
| COLO-800 | Growth Inhibition Assay | IC50=0.69813 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=0.68924 μM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=0.68507 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=0.68501 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=0.68444 μM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=0.68405 μM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=0.68064 μM | SANGER | ||
| EFO-27 | Growth Inhibition Assay | IC50=0.67979 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=0.67846 μM | SANGER | ||
| MDA-MB-157 | Growth Inhibition Assay | IC50=0.6781 μM | SANGER | ||
| MEL-HO | Growth Inhibition Assay | IC50=0.67752 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=0.67689 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=0.6745 μM | SANGER | ||
| SK-OV-3 | Growth Inhibition Assay | IC50=0.67187 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=0.66537 μM | SANGER | ||
| KYSE-150 | Growth Inhibition Assay | IC50=0.66186 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=0.64153 μM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=0.63639 μM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=0.63167 μM | SANGER | ||
| NCI-H522 | Growth Inhibition Assay | IC50=0.62992 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.62502 μM | SANGER | ||
| CAMA-1 | Growth Inhibition Assay | IC50=0.62152 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=0.62126 μM | SANGER | ||
| NCI-H2452 | Growth Inhibition Assay | IC50=0.61917 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=0.61049 μM | SANGER | ||
| NCI-H1437 | Growth Inhibition Assay | IC50=0.60619 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=0.60351 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=0.60094 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=0.59851 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=0.59609 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=0.59162 μM | SANGER | ||
| PC-14 | Growth Inhibition Assay | IC50=0.5897 μM | SANGER | ||
| BCPAP | Growth Inhibition Assay | IC50=0.58791 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=0.58675 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=0.58645 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=0.58541 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=0.58478 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=0.57751 μM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=0.57741 μM | SANGER | ||
| SW780 | Growth Inhibition Assay | IC50=0.57595 μM | SANGER | ||
| PANC-08-13 | Growth Inhibition Assay | IC50=0.57389 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=0.57192 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=0.56884 μM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=0.5591 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=0.55658 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=0.55518 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=0.55123 μM | SANGER | ||
| YH-13 | Growth Inhibition Assay | IC50=0.54938 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=0.53878 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=0.53447 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=0.53195 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=0.53015 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=0.52543 μM | SANGER | ||
| CAL-39 | Growth Inhibition Assay | IC50=0.52268 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=0.51333 μM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=0.5087 μM | SANGER | ||
| NCI-H460 | Growth Inhibition Assay | IC50=0.50597 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=0.50568 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=0.50021 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=0.48968 μM | SANGER | ||
| VM-CUB-1 | Growth Inhibition Assay | IC50=0.47286 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=0.4719 μM | SANGER | ||
| M14 | Growth Inhibition Assay | IC50=0.4717 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=0.46947 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=0.46292 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=0.45754 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=0.45726 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=0.45686 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=0.45336 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=0.4515 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=0.44554 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=0.43848 μM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=0.43697 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=0.43372 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=0.43247 μM | SANGER | ||
| EPLC-272H | Growth Inhibition Assay | IC50=0.43077 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=0.4307 μM | SANGER | ||
| MFE-280 | Growth Inhibition Assay | IC50=0.43032 μM | SANGER | ||
| OVCAR-5 | Growth Inhibition Assay | IC50=0.42933 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=0.42908 μM | SANGER | ||
| MFM-223 | Growth Inhibition Assay | IC50=0.42617 μM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=0.42267 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=0.41695 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=0.41074 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=0.40882 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=0.40787 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=0.40667 μM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=0.4053 μM | SANGER | ||
| SK-LU-1 | Growth Inhibition Assay | IC50=0.39208 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=0.39026 μM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=0.38379 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=0.36553 μM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=0.35314 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=0.35035 μM | SANGER | ||
| NCI-H520 | Growth Inhibition Assay | IC50=0.34834 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=0.34268 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=0.34188 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=0.34047 μM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=0.33619 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=0.32705 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=0.32703 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=0.32331 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=0.31864 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=0.30986 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=0.30805 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=0.30198 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=0.2974 μM | SANGER | ||
| HT | Growth Inhibition Assay | IC50=0.2938 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=0.29164 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=0.28589 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=0.27475 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=0.27407 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=0.27383 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=0.27367 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=0.27215 μM | SANGER | ||
| LK-2 | Growth Inhibition Assay | IC50=0.26824 μM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=0.26414 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=0.25041 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=0.22084 μM | SANGER | ||
| BEN | Growth Inhibition Assay | IC50=0.21293 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=0.20688 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=0.20297 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=0.20202 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=0.20029 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=0.19651 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=0.1955 μM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=0.1897 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=0.18966 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=0.18032 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=0.17019 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=0.16983 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=0.16447 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=0.14723 μM | SANGER | ||
| ME-180 | Growth Inhibition Assay | IC50=0.14681 μM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=0.14073 μM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=0.13531 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=0.135 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=0.10347 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=0.0998 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=0.0935 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.09061 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=0.08641 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=0.08047 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=0.08043 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=0.08009 μM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=0.07951 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=0.06692 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.06569 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=0.05453 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=0.04581 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=0.04056 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.03371 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=0.02938 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=0.02331 μM | SANGER | ||
| AGS | Growth Inhibition Assay | IC50=1.09459 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=1.09628 μM | SANGER | ||
| SW48 | Growth Inhibition Assay | IC50=1.10911 μM | SANGER | ||
| KYSE-180 | Growth Inhibition Assay | IC50=1.11021 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=1.11237 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=1.11759 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=1.13171 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=1.134 μM | SANGER | ||
| NCI-H1755 | Growth Inhibition Assay | IC50=1.13941 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=1.14001 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=1.1445 μM | SANGER | ||
| NCI-H2405 | Growth Inhibition Assay | IC50=1.14574 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=1.15017 μM | SANGER | ||
| MDA-MB-453 | Growth Inhibition Assay | IC50=1.15624 μM | SANGER | ||
| SCC-15 | Growth Inhibition Assay | IC50=1.16956 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=1.17056 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=1.1707 μM | SANGER | ||
| HEC-1 | Growth Inhibition Assay | IC50=1.17627 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=1.17983 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=1.19082 μM | SANGER | ||
| Detroit562 | Growth Inhibition Assay | IC50=1.19439 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=1.20441 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=1.21326 μM | SANGER | ||
| MKN7 | Growth Inhibition Assay | IC50=1.21702 μM | SANGER | ||
| MDA-MB-415 | Growth Inhibition Assay | IC50=1.21702 μM | SANGER | ||
| BT-20 | Growth Inhibition Assay | IC50=1.22444 μM | SANGER | ||
| NCI-H2030 | Growth Inhibition Assay | IC50=1.24106 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=1.24753 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=1.24776 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=1.25171 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=1.25606 μM | SANGER | ||
| NCI-H596 | Growth Inhibition Assay | IC50=1.25929 μM | SANGER | ||
| KYSE-410 | Growth Inhibition Assay | IC50=1.27014 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=1.27167 μM | SANGER | ||
| LN-405 | Growth Inhibition Assay | IC50=1.28021 μM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=1.28823 μM | SANGER | ||
| BFTC-909 | Growth Inhibition Assay | IC50=1.29434 μM | SANGER | ||
| OC-314 | Growth Inhibition Assay | IC50=1.29929 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=1.31135 μM | SANGER | ||
| SKG-IIIa | Growth Inhibition Assay | IC50=1.31428 μM | SANGER | ||
| GAK | Growth Inhibition Assay | IC50=1.31858 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=1.32641 μM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=1.32902 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=1.32998 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=1.34345 μM | SANGER | ||
| COR-L23 | Growth Inhibition Assay | IC50=1.34845 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=1.35797 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=1.36376 μM | SANGER | ||
| SW1088 | Growth Inhibition Assay | IC50=1.36612 μM | SANGER | ||
| AM-38 | Growth Inhibition Assay | IC50=1.37199 μM | SANGER | ||
| CHP-134 | Growth Inhibition Assay | IC50=1.37844 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=1.38555 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=1.39067 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=1.40601 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=1.41046 μM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=1.42854 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=1.43774 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=1.43842 μM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=1.44775 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=1.4556 μM | SANGER | ||
| TCCSUP | Growth Inhibition Assay | IC50=1.4696 μM | SANGER | ||
| SW1990 | Growth Inhibition Assay | IC50=1.47533 μM | SANGER | ||
| UM-UC-3 | Growth Inhibition Assay | IC50=1.47675 μM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=1.48607 μM | SANGER | ||
| NCI-H1299 | Growth Inhibition Assay | IC50=1.50086 μM | SANGER | ||
| RO82-W-1 | Growth Inhibition Assay | IC50=1.52081 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=1.52187 μM | SANGER | ||
| SNU-387 | Growth Inhibition Assay | IC50=1.52241 μM | SANGER | ||
| CAL-85-1 | Growth Inhibition Assay | IC50=1.52599 μM | SANGER | ||
| 647-V | Growth Inhibition Assay | IC50=1.5388 μM | SANGER | ||
| SBC-5 | Growth Inhibition Assay | IC50=1.54593 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=1.55714 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=1.55819 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=1.55908 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=1.56474 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=1.56617 μM | SANGER | ||
| RH-1 | Growth Inhibition Assay | IC50=1.56762 μM | SANGER | ||
| KYSE-270 | Growth Inhibition Assay | IC50=1.57423 μM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=1.57969 μM | SANGER | ||
| JEG-3 | Growth Inhibition Assay | IC50=1.58094 μM | SANGER | ||
| SCC-25 | Growth Inhibition Assay | IC50=1.58432 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=1.60158 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=1.61351 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=1.61438 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=1.61741 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=1.61825 μM | SANGER | ||
| Calu-3 | Growth Inhibition Assay | IC50=1.65213 μM | SANGER | ||
| HT-3 | Growth Inhibition Assay | IC50=1.6566 μM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=1.67343 μM | SANGER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=1.67797 μM | SANGER | ||
| RPMI-2650 | Growth Inhibition Assay | IC50=1.68317 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=1.70874 μM | SANGER | ||
| MDA-MB-231 | Growth Inhibition Assay | IC50=1.71993 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=1.72207 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=1.7356 μM | SANGER | ||
| KYSE-70 | Growth Inhibition Assay | IC50=1.74442 μM | SANGER | ||
| GMS-10 | Growth Inhibition Assay | IC50=1.74662 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=1.74812 μM | SANGER | ||
| SW900 | Growth Inhibition Assay | IC50=1.74993 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=1.75168 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=1.75492 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=1.75682 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=1.77268 μM | SANGER | ||
| BT-474 | Growth Inhibition Assay | IC50=1.78171 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=1.79741 μM | SANGER | ||
| COLO-680N | Growth Inhibition Assay | IC50=1.82381 μM | SANGER | ||
| Saos-2 | Growth Inhibition Assay | IC50=1.82445 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=1.83313 μM | SANGER | ||
| U-118-MG | Growth Inhibition Assay | IC50=1.84622 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=1.85501 μM | SANGER | ||
| NCI-H2052 | Growth Inhibition Assay | IC50=1.8641 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=1.86462 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=1.89165 μM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=1.89545 μM | SANGER | ||
| ACHN | Growth Inhibition Assay | IC50=1.90786 μM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=1.91096 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=1.93325 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=1.94184 μM | SANGER | ||
| SW684 | Growth Inhibition Assay | IC50=1.97371 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=1.98086 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=1.9821 μM | SANGER | ||
| OVCAR-8 | Growth Inhibition Assay | IC50=2.00295 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=2.01774 μM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=2.02049 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=2.02577 μM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=2.04871 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=2.05036 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=2.05568 μM | SANGER | ||
| AU565 | Growth Inhibition Assay | IC50=2.05905 μM | SANGER | ||
| CW-2 | Growth Inhibition Assay | IC50=2.06875 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=2.09377 μM | SANGER | ||
| KP-4 | Growth Inhibition Assay | IC50=2.10312 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=2.10823 μM | SANGER | ||
| NCI-H1395 | Growth Inhibition Assay | IC50=2.10986 μM | SANGER | ||
| CAS-1 | Growth Inhibition Assay | IC50=2.11546 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=2.2269 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=2.28181 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=2.30088 μM | SANGER | ||
| ESS-1 | Growth Inhibition Assay | IC50=2.3051 μM | SANGER | ||
| PANC-10-05 | Growth Inhibition Assay | IC50=2.37024 μM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=2.38708 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=2.38874 μM | SANGER | ||
| KNS-42 | Growth Inhibition Assay | IC50=2.39105 μM | SANGER | ||
| 639-V | Growth Inhibition Assay | IC50=2.42758 μM | SANGER | ||
| SJRH30 | Growth Inhibition Assay | IC50=2.45161 μM | SANGER | ||
| SW1783 | Growth Inhibition Assay | IC50=2.47078 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=2.4828 μM | SANGER | ||
| SK-MEL-30 | Growth Inhibition Assay | IC50=2.4883 μM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=2.49402 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=2.49429 μM | SANGER | ||
| H-EMC-SS | Growth Inhibition Assay | IC50=2.5465 μM | SANGER | ||
| SK-HEP-1 | Growth Inhibition Assay | IC50=2.55236 μM | SANGER | ||
| HCC1395 | Growth Inhibition Assay | IC50=2.55655 μM | SANGER | ||
| HuCCT1 | Growth Inhibition Assay | IC50=2.5639 μM | SANGER | ||
| SiHa | Growth Inhibition Assay | IC50=2.58719 μM | SANGER | ||
| EFO-21 | Growth Inhibition Assay | IC50=2.58764 μM | SANGER | ||
| NCI-H1666 | Growth Inhibition Assay | IC50=2.59076 μM | SANGER | ||
| UMC-11 | Growth Inhibition Assay | IC50=2.59868 μM | SANGER | ||
| COLO-679 | Growth Inhibition Assay | IC50=2.61233 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=2.65253 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=2.65408 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=2.68768 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=2.68856 μM | SANGER | ||
| HOP-92 | Growth Inhibition Assay | IC50=2.7011 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=2.71442 μM | SANGER | ||
| NCI-H810 | Growth Inhibition Assay | IC50=2.72198 μM | SANGER | ||
| 769-P | Growth Inhibition Assay | IC50=2.7228 μM | SANGER | ||
| SAS | Growth Inhibition Assay | IC50=2.765 μM | SANGER | ||
| M059J | Growth Inhibition Assay | IC50=2.78318 μM | SANGER | ||
| RD | Growth Inhibition Assay | IC50=2.79471 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=2.83433 μM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=2.86502 μM | SANGER | ||
| KYSE-510 | Growth Inhibition Assay | IC50=2.89504 μM | SANGER | ||
| NCI-N87 | Growth Inhibition Assay | IC50=2.91807 μM | SANGER | ||
| MKN1 | Growth Inhibition Assay | IC50=3.00163 μM | SANGER | ||
| NCI-H2170 | Growth Inhibition Assay | IC50=3.00451 μM | SANGER | ||
| OVCAR-3 | Growth Inhibition Assay | IC50=3.02115 μM | SANGER | ||
| KLE | Growth Inhibition Assay | IC50=3.06812 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=3.09343 μM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=3.11112 μM | SANGER | ||
| SCC-9 | Growth Inhibition Assay | IC50=3.11366 μM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=3.12423 μM | SANGER | ||
| LCLC-103H | Growth Inhibition Assay | IC50=3.23894 μM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=3.27633 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=3.32164 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=3.46431 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=3.46502 μM | SANGER | ||
| BT-549 | Growth Inhibition Assay | IC50=3.50209 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=3.54158 μM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=3.61798 μM | SANGER | ||
| SW626 | Growth Inhibition Assay | IC50=3.71128 μM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=3.73247 μM | SANGER | ||
| IGR-1 | Growth Inhibition Assay | IC50=3.74248 μM | SANGER | ||
| NCI-H2291 | Growth Inhibition Assay | IC50=3.75336 μM | SANGER | ||
| NCI-H441 | Growth Inhibition Assay | IC50=3.82433 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=3.86031 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=3.91271 μM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=3.91436 μM | SANGER | ||
| HT55 | Growth Inhibition Assay | IC50=3.91773 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=3.95864 μM | SANGER | ||
| RERF-LC-MS | Growth Inhibition Assay | IC50=3.96525 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=4.12881 μM | SANGER | ||
| RMG-I | Growth Inhibition Assay | IC50=4.21454 μM | SANGER | ||
| CFPAC-1 | Growth Inhibition Assay | IC50=4.21685 μM | SANGER | ||
| S-117 | Growth Inhibition Assay | IC50=4.22024 μM | SANGER | ||
| NCI-H2122 | Growth Inhibition Assay | IC50=4.30931 μM | SANGER | ||
| J82 | Growth Inhibition Assay | IC50=4.33441 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=4.35477 μM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=4.41298 μM | SANGER | ||
| UACC-62 | Growth Inhibition Assay | IC50=4.46545 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=4.49115 μM | SANGER | ||
| RCM-1 | Growth Inhibition Assay | IC50=4.5292 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=4.65359 μM | SANGER | ||
| SW756 | Growth Inhibition Assay | IC50=4.69135 μM | SANGER | ||
| HCC38 | Growth Inhibition Assay | IC50=4.71197 μM | SANGER | ||
| YAPC | Growth Inhibition Assay | IC50=4.71313 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=4.78112 μM | SANGER | ||
| HCC1937 | Growth Inhibition Assay | IC50=4.85125 μM | SANGER | ||
| OAW-28 | Growth Inhibition Assay | IC50=4.92435 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=5.08328 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=5.23486 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=5.27837 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition Assay | IC50=5.39432 μM | SANGER | ||
| TGBC11TKB | Growth Inhibition Assay | IC50=5.45786 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=5.5052 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=5.55801 μM | SANGER | ||
| Ca-Ski | Growth Inhibition Assay | IC50=5.62566 μM | SANGER | ||
| COLO-741 | Growth Inhibition Assay | IC50=5.71995 μM | SANGER | ||
| HT-29 | Growth Inhibition Assay | IC50=5.80475 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=5.81008 μM | SANGER | ||
| Capan-2 | Growth Inhibition Assay | IC50=5.95994 μM | SANGER | ||
| NCI-H630 | Growth Inhibition Assay | IC50=6.11441 μM | SANGER | ||
| COLO-678 | Growth Inhibition Assay | IC50=6.15092 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=6.17336 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=6.24943 μM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=6.2649 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=6.27118 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=6.33399 μM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=6.40302 μM | SANGER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=6.45445 μM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=6.45616 μM | SANGER | ||
| C3A | Growth Inhibition Assay | IC50=6.52004 μM | SANGER | ||
| NCI-H1650 | Growth Inhibition Assay | IC50=6.70522 μM | SANGER | ||
| DU-145 | Growth Inhibition Assay | IC50=6.7703 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=6.77873 μM | SANGER | ||
| LS-1034 | Growth Inhibition Assay | IC50=7.04412 μM | SANGER | ||
| HCC1954 | Growth Inhibition Assay | IC50=7.48134 μM | SANGER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=7.48533 μM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=7.51498 μM | SANGER | ||
| OE19 | Growth Inhibition Assay | IC50=7.65503 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=7.71421 μM | SANGER | ||
| NCI-H2342 | Growth Inhibition Assay | IC50=7.71521 μM | SANGER | ||
| U-87-MG | Growth Inhibition Assay | IC50=8.03334 μM | SANGER | ||
| MKN28 | Growth Inhibition Assay | IC50=8.11515 μM | SANGER | ||
| HT-1197 | Growth Inhibition Assay | IC50=8.25907 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=8.34245 μM | SANGER | ||
| NCI-H226 | Growth Inhibition Assay | IC50=8.44331 μM | SANGER | ||
| NCI-H2029 | Growth Inhibition Assay | IC50=9.06759 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=9.45588 μM | SANGER | ||
| ZR-75-30 | Growth Inhibition Assay | IC50=9.92634 μM | SANGER | ||
| SW837 | Growth Inhibition Assay | IC50=10.2293 μM | SANGER | ||
| NCI-H1651 | Growth Inhibition Assay | IC50=10.2326 μM | SANGER | ||
| NCI-H727 | Growth Inhibition Assay | IC50=10.4495 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=10.8365 μM | SANGER | ||
| NCI-H2087 | Growth Inhibition Assay | IC50=11.0434 μM | SANGER | ||
| FTC-133 | Growth Inhibition Assay | IC50=11.4051 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=12.124 μM | SANGER | ||
| NCI-H1838 | Growth Inhibition Assay | IC50=12.5151 μM | SANGER | ||
| Calu-6 | Growth Inhibition Assay | IC50=14.1021 μM | SANGER | ||
| HCC70 | Growth Inhibition Assay | IC50=14.451 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=15.2159 μM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=15.3843 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=15.532 μM | SANGER | ||
| no-10 | Growth Inhibition Assay | IC50=15.938 μM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=16.3675 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=17.5166 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=19.0607 μM | SANGER | ||
| COLO-824 | Growth Inhibition Assay | IC50=20.9276 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=21.0748 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=21.175 μM | SANGER | ||
| L-428 | Growth Inhibition Assay | IC50=21.4016 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=21.502 μM | SANGER | ||
| DoTc2-4510 | Growth Inhibition Assay | IC50=23.8475 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=26.7957 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=33.3464 μM | SANGER | ||
| SW1463 | Growth Inhibition Assay | IC50=33.983 μM | SANGER | ||
| SW1417 | Growth Inhibition Assay | IC50=37.0952 μM | SANGER | ||
| NB12 | Growth Inhibition Assay | IC50=39.4655 μM | SANGER | ||
| NY | Growth Inhibition Assay | IC50=41.3201 μM | SANGER | ||
| TamR | Growth Inhibition Assay | IC50=18 nM | 24457069 | ||
| MCF7-X | Growth Inhibition Assay | IC50=24 nM | 24457069 | ||
| T47D-tamR | Growth Inhibition Assay | IC50=19 nM | 24457069 | ||
| Rh41 | Growth Inhibition Assay | IC50=30.7 nM | 21337679 | ||
| Rh18 | Growth Inhibition Assay | IC50=41.4 nM | 21337679 | ||
| Rh30 | Growth Inhibition Assay | IC50=14 nM | 21337679 | ||
| BT-12 | Growth Inhibition Assay | IC50=24.7 nM | 21337679 | ||
| CHLA-266 | Growth Inhibition Assay | IC50=1.1 nM | 21337679 | ||
| TC-71 | Growth Inhibition Assay | IC50=46.5 nM | 21337679 | ||
| CHLA-9 | Growth Inhibition Assay | IC50=15.3 nM | 21337679 | ||
| CHLA-10 | Growth Inhibition Assay | IC50=3.9 nM | 21337679 | ||
| CHLA-258 | Growth Inhibition Assay | IC50=10.4 nM | 21337679 | ||
| GBM2 | Growth Inhibition Assay | IC50=40.7 nM | 21337679 | ||
| NB-1643 | Growth Inhibition Assay | IC50=33.8 nM | 21337679 | ||
| NB-EBc1 | Growth Inhibition Assay | IC50=27.1 nM | 21337679 | ||
| CHLA-90 | Growth Inhibition Assay | IC50=34.5 nM | 21337679 | ||
| CHLA-136 | Growth Inhibition Assay | IC50=162.6 nM | 21337679 | ||
| NALM-6 | Growth Inhibition Assay | IC50=32.9 nM | 21337679 | ||
| COG-LL-317 | Growth Inhibition Assay | IC50=1.3 nM | 21337679 | ||
| RS4;11 | Growth Inhibition Assay | IC50=35 nM | 21337679 | ||
| MOLT-4 | Growth Inhibition Assay | IC50=8.6 nM | 21337679 | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=4.1 nM | 21337679 | ||
| Kasumi-1 | Growth Inhibition Assay | IC50=1.4 nM | 21337679 | ||
| Karpas-299 | Growth Inhibition Assay | IC50=21.7 nM | 21337679 | ||
| Ramos-RA1 | Growth Inhibition Assay | IC50=8.2 nM | 21337679 | ||
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生物活性
| 製品説明 | AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1. | ||||
|---|---|---|---|---|---|
| 特性 | First drug to inhibit both types of mTOR protein. | ||||
| Targets |
|
| In Vitro | ||||
| In vitro | AZD8055 shows low activity (∼1,000-fold) against all PI3K isoforms (α, β, γ, δ) and other members of the PI3K-like kinase family (ATM and DNA-PK). AZD8055 inhibits the phosphorylation of mTORC1 (p70S6K and 4E-BP1) as well as phosphorylation of the mTORC2 (Akt) and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 can be fully inhibited by AZD8055, resulting in significant inhibition of cap-dependent translation. AZD8055 potently inhibits proliferation in U87MG, A549 and H838 cells with IC50 of 53, 50 and 20 nM, respectively. AZD8055 also induces autophagy and increased LC3-II levels in H838 and A549 cells. [1] AZD8055 decreases AML blast cell proliferation and cell cycle progression, reduces the clonogenic growth of leukemic progenitors and induces caspase-dependent apoptosis in leukemic cells but not in normal immature CD34+ cells. [2] AZD8055 indicates inhibitory against the pediatric preclinical testing program (PPTP) cell lines with IC50 of 24.7 nM and induces significant differences in EFS distribution. [3] | |||
|---|---|---|---|---|
| Kinase Assay | Cell-based determinations of mTOR inhibition | |||
| A high-throughput screening cell-based assay is developed using MDA-MB-468 cells to detect mTORC1 and mTORC2 activity. Cells are exposed for 2 hours to increasing concentrations of AZD8055. At the end of the incubation period, cells are fixed, washed, and probed with antibodies against S473 pAkt or against S235/236 phosphorylated S6 (pS6). Levels of phosphorylation are assessed using an Acumen laser scanning cytometer. | ||||
| 細胞実験 | 細胞株 | U87MG, A549 and H838 cells | ||
| 濃度 | 1 nM - 1 μM | |||
| 反応時間 | 72 to 96 hours | |||
| 実験の流れ | Cells are exposed to AZD8055 for 72 to 96 hours and stained for cell nuclei (0.03 mg/mL Hoechst 33342) and acidic vesicles (1 μg/mL acridine orange). Images are captured at 450 and 536 nm on an ArrayScan II platform, and the percentage of acidic vesicles and the number of cells are quantified. For LC3 assessment, cells are exposed to e64d/pepstatin (10 μg/mL) for 30 to 90 min before incubation with AZD8055. Cells are lysed on ice and analyzed by immunoblotting. | |||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | p-mTOR / p-AKT / p-4EBP1 / p-P70S6K / p-PRAS40 p-EGFR / EGFR p-FOXO1 / FOXO1 / p-FOXO3a / FOXO3a |
|
24457069 | |
| Immunofluorescence | p-4EBP1 / EIF4E / mTOR LC3B / p62 |
|
24600487 | |
| Growth inhibition assay | Cell viability |
|
29263324 | |
| In Vivo | ||
| In Vivo | AZD8055 inhibits the pS6 and pAkt in U87MG and A549 xenografts at 2.5/10 mg/kg, which leads to tumor growth inhibition. AZD8055 shows significant antitumor activity in many xenografts, including U87MG, BT474c, A549, Calu-3, LoVo, SW620, PC3 and MES-SA at a dose of 10/20 mg/kg. [1] AZD8055 induces ~40% reduction in tumour volume, accompanied by ablation of phosphorylation of Akt, S6K and SGK protein kinases. Administration of AZD8055 (5mg/kg, Bid) and SAHA (100 mg/kg/d) results in complete tumor growth inhibition in PTEN+/−LKB1+/hypo xenografts without side effects on mice by inhibition of mTORC1 and mTORC2 signaling. [4] | |
|---|---|---|
| 動物実験 | 動物モデル | U87MG, BT474c, A549, Calu-3, LoVo, SW620, PC3 and MES-SA U87-MG and A549 are established in pathogen-free, female nude mice (nu/nu:Alpk). |
| 投与量 | 2.5-20 mg/kg | |
| 投与経路 | Oral gavage once or twice daily | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01316809 | Completed | Glioblastoma Multiforme|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Malignant Glioma|Brainstem Glioma |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
March 4 2011 | Phase 1 |
| NCT00999882 | Completed | Cancer|Advanced Hepatocellular Carcinoma |
AstraZeneca |
October 2009 | Phase 1 |
| NCT00973076 | Completed | Cancer|Solid Tumors|Advanced Solid Malignancies |
AstraZeneca |
August 2009 | Phase 1 |
| NCT00731263 | Completed | Solid Tumors |
AstraZeneca |
July 2008 | Phase 1 |
| NCT01194193 | Withdrawn | Cancer|Advanced Solid Tumours|Lymphomas |
AstraZeneca |
Phase 1 | |
化学情報
| 分子量 | 465.54 | 化学式 | C25H31N5O4 |
| CAS No. | 1009298-09-2 | SDF | Download AZD8055 SDFをダウンロードする |
| Smiles | CC1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=C(C=C4)OC)CO)N5CCOCC5C | ||
| 保管 | |||
|
In vitro |
DMSO : 93 mg/mL ( (199.76 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。) Ethanol : 93 mg/mL Water : 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。
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