MK-2206 2HCl
MK-2206 2HCl是一种高度选择性的Akt1/2/3抑制剂，在无细胞试验中IC50分别为8 nM/12 nM/65 nM；对250种其他蛋白激酶没有抑制活性。MK-2206 2HCl 在肿瘤细胞中可诱导自噬和凋亡。Phase 2。
MK-2206 2HCl Chemical Structure
CAS: 1032350-13-2
产品质控
批次：
纯度：
99.92%
99.92
MK-2206 2HCl相关产品
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 |
|---|---|---|---|---|---|
| Rh30 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| OHS-50 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| MG 63 (6-TG R) | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| SK-N-SH | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| BT-37 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| DAOY | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| NCI-H292 | Cytotoxic Assay | 3 μM | 72 h | Inhibition of cell proliferation | 20571069 |
| A431 | Kinase Assay | 5 μM | 5 h | Suppresses the signaling of Akt and Erk | 20571069 |
| HepG2 | Cytotoxic Assay | 10 μM | 24 h | Sensitizes resistant cells to the cytotoxic effect of | 21205925 |
| Sk-Hep1 | Cytotoxic Assay | 10 μM | 24 h | Sensitizes resistant cells to the cytotoxic effect of | 21205925 |
| OCUT1 cells harbored PIK3CA (H1047R+/+) | Growth Inhibition Assay | 3 μM | 5 d | IC50=0.14 μM | 21289267 |
| FTC133 cells harbored PTEN (allele deletion and R130+) | Growth Inhibition Assay | 3 μM | 5 d | IC50=0.18 μM | 21289267 |
| C643 cells harbored HRAS (G13R+/−) | Growth Inhibition Assay | 3 μM | 5 d | IC50=0.27 μM | 21289267 |
| Hth7 cells harbored NRAS (Q61R+/−) | Growth Inhibition Assay | 3 μM | 5 d | IC50=4.5 μM | 21289267 |
| HC11 | Function Assay | 10 μM | 24 h | Inhibits β-casein and ADRP synthesis | 22426621 |
| CEM-S | Cytotoxic Assay | 10 μM | 48 h | IC50=5.1 μM | 22614243 |
| MOLT-4 | Function Assay | 10 μM | 24 h | Blocks cells in the G0/G1 phase of the cell cycle | 22614243 |
| CEM-R | Function Assay | 4 μM | 4 h | Increases the amount of cleaved LC4A/B, a well-established autophagy marker | 22614243 |
| CEM-S | Function Assay | 4 μM | 4 h | Increases the amount of cleaved LC5A/B, a well-established autophagy marker | 22614243 |
| LoVo | Growth Inhibition Assay | IC50=1.32534 μM | SANGER | ||
| SJ-GBM2 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| C2BBe1 | Growth Inhibition Assay | IC50=231.905 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=36.67 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=36.6538 μM | SANGER | ||
| SW48 | Growth Inhibition Assay | IC50=36.2474 μM | SANGER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=36.1198 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=34.4684 μM | SANGER | ||
| COLO-800 | Growth Inhibition Assay | IC50=34.3647 μM | SANGER | ||
| OE33 | Growth Inhibition Assay | IC50=34.2855 μM | SANGER | ||
| 769-P | Growth Inhibition Assay | IC50=32.3641 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=32.2897 μM | SANGER | ||
| NCI-H2170 | Growth Inhibition Assay | IC50=31.8516 μM | SANGER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=31.069 μM | SANGER | ||
| HT-1197 | Growth Inhibition Assay | IC50=30.0598 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=29.8157 μM | SANGER | ||
| PANC-03-27 | Growth Inhibition Assay | IC50=29.444 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=29.1465 μM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=28.5417 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=28.2964 μM | SANGER | ||
| YAPC | Growth Inhibition Assay | IC50=28.2564 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=28.1112 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=26.0274 μM | SANGER | ||
| NCI-H1755 | Growth Inhibition Assay | IC50=25.9945 μM | SANGER | ||
| BT-549 | Growth Inhibition Assay | IC50=25.9011 μM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=25.6465 μM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=25.6888 μM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=25.5918 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=25.3563 μM | SANGER | ||
| NCI-H2342 | Growth Inhibition Assay | IC50=25.1953 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=24.619 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=24.4885 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=24.3302 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=24.4874 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=24.294 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=24.2226 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=23.8709 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=23.7759 μM | SANGER | ||
| S-117 | Growth Inhibition Assay | IC50=23.7651 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=23.5234 μM | SANGER | ||
| M14 | Growth Inhibition Assay | IC50=23.4088 μM | SANGER | ||
| NCI-H2405 | Growth Inhibition Assay | IC50=23.2533 μM | SANGER | ||
| AM-38 | Growth Inhibition Assay | IC50=22.8689 μM | SANGER | ||
| Rh41 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| NB1643 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| BT-12 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| RD | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| Saos-2 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| A673 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| HCT116 | Growth inhibition assay | 72 h | IC50 = 7.5 μM | 24900862 | |
| NCI-H460 | Growth inhibition assay | 72 h | IC50 = 5.4 μM | 24900862 | |
| HeLa | Function assay | 1 h | IC50 = 0.0228 μM | 29100733 | |
| K1 cells harbored PIK3CA (E542K+/+) | Growth Inhibition Assay | 3 μM | 5 d | IC50=0.52 μM | 21289267 |
| TPC1 cells harbored RET/PTC1 rearrangement | Growth Inhibition Assay | 3 μM | 5 d | IC50=0.59 μM | 21289267 |
| Hth74 | Growth Inhibition Assay | 3 μM | 5 d | IC50=2.19 μM | 21289267 |
| KAT18 | Growth Inhibition Assay | 3 μM | 5 d | IC50=4.62 μM | 21289267 |
| SW1736 | Growth Inhibition Assay | 100 μM | 5 d | IC50=47.56 μM | 21289267 |
| WRO | Growth Inhibition Assay | 1000 μM | 5 d | IC50>1000 μM | 21289267 |
| LN229 | Apoptosis Assay | 0.5 μM | 60 h | Augments apoptogenic effects of | 22057914 |
| TAD2 | Growth Inhibition Assay | 1000 μM | 5 d | IC50>1000 μM | 21289267 |
| T98G | Apoptosis Assay | 0.5 μM | 60 h | Augments apoptogenic effects of | 22057914 |
| MOLT-4 | Cytotoxic Assay | 10 μM | 48 h | IC50=1.7 μM | 22614243 |
| CEM-R | Cytotoxic Assay | 10 μM | 48 h | IC50=3.3 μM | 22614243 |
| MOLT-4 | Function Assay | 4 μM | 4 h | Increases the amount of cleaved LC3A/B, a well-established autophagy marker | 22614243 |
| HepG2 cell | Kinase Assay | 20 μM | 24 h | Downregulates the phosphorylation of AKT | 23797319 |
| HepG2 cell | Growth Inhibition Assay | 30 μM | 24 h | Inhibits cell growth | 23797319 |
| HepG2 cell | Apoptosis Assay | 20 μM | 24 h | Induces cell apoptosis | 23797319 |
| GEO | Growth Inhibition Assay | 500 nM | 72 h | Inhibits cell growth | 24581231 |
| CNE-1 | Growth Inhibition Assay | 10 μM | 96 h | IC50=2.96 μM | 25336925 |
| CNE-2 | Growth Inhibition Assay | 10 μM | 96 h | IC50=4.53 μM | 25336925 |
| SUNE-1 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.52 μM | 25336925 |
| HONE-1 | Growth Inhibition Assay | 10 μM | 96 h | IC50=3.37 μM | 25336925 |
| CNE-2 | Function Assay | 10 μM | 48 h | Induces cell cycle arrest at G1 | 25336925 |
| HONE-1 | Function Assay | 10 μM | 48 h | Induces cell cycle arrest at G1 | 25336925 |
| NEC8 | Growth Inhibition Assay | IC50=0.09651 μM | SANGER | ||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=0.1162 μM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=0.13738 μM | SANGER | ||
| AsPC-1 | Growth Inhibition Assay | IC50=0.22122 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=0.2825 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=0.30283 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=0.3032 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=0.34455 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=0.3461 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.37321 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=0.37679 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=0.38883 μM | SANGER | ||
| EFM-19 | Growth Inhibition Assay | IC50=0.4401 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=0.44035 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=0.46868 μM | SANGER | ||
| NCI-H1563 | Growth Inhibition Assay | IC50=0.48189 μM | SANGER | ||
| HCC1419 | Growth Inhibition Assay | IC50=0.48892 μM | SANGER | ||
| H-EMC-SS | Growth Inhibition Assay | IC50=0.49939 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=0.52961 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=0.55249 μM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=0.56783 μM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=0.57761 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=0.5826 μM | SANGER | ||
| HCC70 | Growth Inhibition Assay | IC50=0.59827 μM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=0.61048 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=0.6213 μM | SANGER | ||
| HT | Growth Inhibition Assay | IC50=0.63239 μM | SANGER | ||
| MDA-MB-415 | Growth Inhibition Assay | IC50=0.63626 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=0.63723 μM | SANGER | ||
| DU-145 | Growth Inhibition Assay | IC50=0.64745 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=0.70966 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=0.73025 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=0.74403 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=0.80582 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=0.82411 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=0.83442 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=0.86253 μM | SANGER | ||
| HOP-92 | Growth Inhibition Assay | IC50=0.87223 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=0.8872 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=0.92751 μM | SANGER | ||
| MFE-280 | Growth Inhibition Assay | IC50=0.96465 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=0.97939 μM | SANGER | ||
| NCI-H520 | Growth Inhibition Assay | IC50=0.98592 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=0.99734 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=1.14485 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=1.17156 μM | SANGER | ||
| EPLC-272H | Growth Inhibition Assay | IC50=1.17256 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=1.23725 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=1.24065 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=1.28203 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=1.2899 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=1.29795 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=1.33701 μM | SANGER | ||
| MFM-223 | Growth Inhibition Assay | IC50=1.34461 μM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=1.35265 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=1.37616 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=1.49116 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=1.49558 μM | SANGER | ||
| DMS-273 | Growth Inhibition Assay | IC50=1.51959 μM | SANGER | ||
| ME-180 | Growth Inhibition Assay | IC50=1.56891 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=1.68225 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=1.71242 μM | SANGER | ||
| OMC-1 | Growth Inhibition Assay | IC50=1.74677 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=1.79737 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=1.81074 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=1.87101 μM | SANGER | ||
| SNU-387 | Growth Inhibition Assay | IC50=1.88406 μM | SANGER | ||
| SW1088 | Growth Inhibition Assay | IC50=1.94606 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=2.11433 μM | SANGER | ||
| OC-314 | Growth Inhibition Assay | IC50=2.15086 μM | SANGER | ||
| RMG-I | Growth Inhibition Assay | IC50=2.16398 μM | SANGER | ||
| NCI-H1395 | Growth Inhibition Assay | IC50=2.18091 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=2.23845 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=2.24317 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=2.29923 μM | SANGER | ||
| OAW-28 | Growth Inhibition Assay | IC50=2.29951 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=2.31552 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=2.33253 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=2.33484 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=2.38191 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=2.38983 μM | SANGER | ||
| VM-CUB-1 | Growth Inhibition Assay | IC50=2.39083 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=2.41044 μM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=2.41939 μM | SANGER | ||
| YH-13 | Growth Inhibition Assay | IC50=2.46153 μM | SANGER | ||
| T-24 | Growth Inhibition Assay | IC50=2.47881 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=2.49287 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=2.49759 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=2.60487 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=2.62953 μM | SANGER | ||
| AGS | Growth Inhibition Assay | IC50=2.72137 μM | SANGER | ||
| HCC1395 | Growth Inhibition Assay | IC50=2.75187 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=2.75266 μM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=2.83872 μM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=2.86117 μM | SANGER | ||
| SNU-423 | Growth Inhibition Assay | IC50=2.89242 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=2.96865 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=3.04611 μM | SANGER | ||
| EoL-1- | Growth Inhibition Assay | IC50=3.07058 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=3.09464 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=3.1119 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=3.19529 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=3.20694 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=3.21879 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=3.22859 μM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=3.38179 μM | SANGER | ||
| OVCAR-3 | Growth Inhibition Assay | IC50=3.40786 μM | SANGER | ||
| NCI-H1623 | Growth Inhibition Assay | IC50=3.41224 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=3.45626 μM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=3.46678 μM | SANGER | ||
| RT-112 | Growth Inhibition Assay | IC50=3.52388 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=3.62278 μM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=3.62456 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=3.63338 μM | SANGER | ||
| SJRH30 | Growth Inhibition Assay | IC50=3.69122 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=3.70711 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=3.72038 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=3.80976 μM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=3.81788 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=3.88428 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=3.93622 μM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=4.02305 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=4.02966 μM | SANGER | ||
| SCC-25 | Growth Inhibition Assay | IC50=4.06566 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=4.09534 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=4.14191 μM | SANGER | ||
| Calu-3 | Growth Inhibition Assay | IC50=4.24416 μM | SANGER | ||
| NCI-H460 | Growth Inhibition Assay | IC50=4.26443 μM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=4.37778 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=4.38146 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=4.41579 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=4.41838 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=4.44304 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=4.53697 μM | SANGER | ||
| KLE | Growth Inhibition Assay | IC50=4.70198 μM | SANGER | ||
| CAL-39 | Growth Inhibition Assay | IC50=4.72146 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=4.80609 μM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=4.942 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=4.94673 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=4.96142 μM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=5.20009 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=5.21165 μM | SANGER | ||
| BT-20 | Growth Inhibition Assay | IC50=5.21353 μM | SANGER | ||
| MEL-HO | Growth Inhibition Assay | IC50=5.37336 μM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=5.46339 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=5.59428 μM | SANGER | ||
| RPMI-2650 | Growth Inhibition Assay | IC50=5.66199 μM | SANGER | ||
| PFSK-1 | Growth Inhibition Assay | IC50=5.72732 μM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=5.80633 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=5.86472 μM | SANGER | ||
| Saos-2 | Growth Inhibition Assay | IC50=5.8653 μM | SANGER | ||
| SK-OV-3 | Growth Inhibition Assay | IC50=5.99816 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=6.08773 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=6.19649 μM | SANGER | ||
| BT-474 | Growth Inhibition Assay | IC50=6.233 μM | SANGER | ||
| BFTC-909 | Growth Inhibition Assay | IC50=6.30345 μM | SANGER | ||
| NB12 | Growth Inhibition Assay | IC50=6.39071 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=6.45169 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=6.60143 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=6.6306 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=6.63604 μM | SANGER | ||
| LN-405 | Growth Inhibition Assay | IC50=6.79672 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=6.80079 μM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=6.81961 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=6.83817 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=6.93038 μM | SANGER | ||
| AU565 | Growth Inhibition Assay | IC50=6.96957 μM | SANGER | ||
| RD | Growth Inhibition Assay | IC50=6.98284 μM | SANGER | ||
| SW1463 | Growth Inhibition Assay | IC50=7.11168 μM | SANGER | ||
| LU-99A | Growth Inhibition Assay | IC50=7.14322 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=7.2924 μM | SANGER | ||
| MC-IXC | Growth Inhibition Assay | IC50=7.48576 μM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=7.48764 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=7.54804 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=7.66233 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=7.67336 μM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=7.79334 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=8.04429 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=8.15268 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=8.18067 μM | SANGER | ||
| HCC1954 | Growth Inhibition Assay | IC50=8.45104 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=8.45936 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=8.53257 μM | SANGER | ||
| SKG-IIIa | Growth Inhibition Assay | IC50=8.63069 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=8.64643 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=8.64696 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=8.68219 μM | SANGER | ||
| CAMA-1 | Growth Inhibition Assay | IC50=8.77146 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=8.78629 μM | SANGER | ||
| ESS-1 | Growth Inhibition Assay | IC50=8.88704 μM | SANGER | ||
| HEC-1 | Growth Inhibition Assay | IC50=8.89866 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=9.02224 μM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=9.04232 μM | SANGER | ||
| EFO-27 | Growth Inhibition Assay | IC50=9.16412 μM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=9.16628 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=9.2087 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=9.27402 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=9.31761 μM | SANGER | ||
| SHP-77 | Growth Inhibition Assay | IC50=9.39935 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=9.53277 μM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=9.65544 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=9.80238 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=9.84984 μM | SANGER | ||
| MDA-MB-157 | Growth Inhibition Assay | IC50=9.92878 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=9.99974 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=10.2006 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=10.2164 μM | SANGER | ||
| OVCAR-5 | Growth Inhibition Assay | IC50=10.2433 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=10.3973 μM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=10.4353 μM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=10.9041 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=11.3897 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=11.424 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=11.4668 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=11.5271 μM | SANGER | ||
| SW756 | Growth Inhibition Assay | IC50=11.5294 μM | SANGER | ||
| PC-3 | Growth Inhibition Assay | IC50=11.5764 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=11.636 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=11.7093 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=11.7509 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=11.7982 μM | SANGER | ||
| NCI-H1299 | Growth Inhibition Assay | IC50=11.8093 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=11.8228 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=11.9663 μM | SANGER | ||
| CFPAC-1 | Growth Inhibition Assay | IC50=11.9782 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=12.0313 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=12.0716 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=12.1177 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=12.1854 μM | SANGER | ||
| RH-1 | Growth Inhibition Assay | IC50=12.2184 μM | SANGER | ||
| BCPAP | Growth Inhibition Assay | IC50=12.4749 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=12.5209 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=12.5869 μM | SANGER | ||
| KYSE-140 | Growth Inhibition Assay | IC50=12.8595 μM | SANGER | ||
| Ca-Ski | Growth Inhibition Assay | IC50=12.9041 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=12.9115 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=13.1912 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=13.2327 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=13.345 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=13.6483 μM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=13.9739 μM | SANGER | ||
| SCC-15 | Growth Inhibition Assay | IC50=13.9775 μM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=14.1664 μM | SANGER | ||
| SW780 | Growth Inhibition Assay | IC50=14.5025 μM | SANGER | ||
| NCI-H2291 | Growth Inhibition Assay | IC50=14.5878 μM | SANGER | ||
| JEG-3 | Growth Inhibition Assay | IC50=14.6326 μM | SANGER | ||
| CAL-120 | Growth Inhibition Assay | IC50=14.7027 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=14.7997 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=14.9611 μM | SANGER | ||
| PC-14 | Growth Inhibition Assay | IC50=14.9654 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=15.0111 μM | SANGER | ||
| OE19 | Growth Inhibition Assay | IC50=15.1541 μM | SANGER | ||
| CAS-1 | Growth Inhibition Assay | IC50=15.4184 μM | SANGER | ||
| NCI-H727 | Growth Inhibition Assay | IC50=15.4221 μM | SANGER | ||
| SiHa | Growth Inhibition Assay | IC50=15.7594 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=15.7694 μM | SANGER | ||
| MDA-MB-453 | Growth Inhibition Assay | IC50=16.1642 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=16.6373 μM | SANGER | ||
| SK-LU-1 | Growth Inhibition Assay | IC50=16.6956 μM | SANGER | ||
| Detroit562 | Growth Inhibition Assay | IC50=16.7318 μM | SANGER | ||
| HCC1569 | Growth Inhibition Assay | IC50=16.8337 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=16.8419 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=17.0479 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=17.0707 μM | SANGER | ||
| SW1783 | Growth Inhibition Assay | IC50=17.128 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=17.3303 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=17.5512 μM | SANGER | ||
| KOSC-2 | Growth Inhibition Assay | IC50=17.6757 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=17.6937 μM | SANGER | ||
| M059J | Growth Inhibition Assay | IC50=17.703 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=17.9673 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=18.1382 μM | SANGER | ||
| CAL-85-1 | Growth Inhibition Assay | IC50=18.2357 μM | SANGER | ||
| 639-V | Growth Inhibition Assay | IC50=18.3354 μM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=18.4727 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=18.5232 μM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=18.7286 μM | SANGER | ||
| NCI-N87 | Growth Inhibition Assay | IC50=18.9008 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=19.0646 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=19.1546 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=19.2286 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=19.3024 μM | SANGER | ||
| KYSE-270 | Growth Inhibition Assay | IC50=20.0217 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=20.0941 μM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=20.1665 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=20.3374 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=20.5497 μM | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=20.6883 μM | SANGER | ||
| NCI-H441 | Growth Inhibition Assay | IC50=20.7379 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=20.8134 μM | SANGER | ||
| HT-3 | Growth Inhibition Assay | IC50=21.5631 μM | SANGER | ||
| 22RV1 | Growth Inhibition Assay | IC50=21.5685 μM | SANGER | ||
| LK-2 | Growth Inhibition Assay | IC50=21.5953 μM | SANGER | ||
| CW-2 | Growth Inhibition Assay | IC50=21.6069 μM | SANGER | ||
| KYSE-510 | Growth Inhibition Assay | IC50=21.6095 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=21.7166 μM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=22.034 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=22.1697 μM | SANGER | ||
| NCI-H2122 | Growth Inhibition Assay | IC50=22.2432 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=22.3895 μM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=441.083 μM | SANGER | ||
| HCC38 | Growth Inhibition Assay | IC50=401.593 μM | SANGER | ||
| NCI-H2052 | Growth Inhibition Assay | IC50=398.472 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=392.596 μM | SANGER | ||
| SBC-5 | Growth Inhibition Assay | IC50=386.985 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=383.36 μM | SANGER | ||
| T84 | Growth Inhibition Assay | IC50=374.712 μM | SANGER | ||
| LU-135 | Growth Inhibition Assay | IC50=367.035 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=363.589 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=347.401 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=344.167 μM | SANGER | ||
| NCI-H1993 | Growth Inhibition Assay | IC50=342.365 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=342.326 μM | SANGER | ||
| NCI-H630 | Growth Inhibition Assay | IC50=332.294 μM | SANGER | ||
| KP-N-YN | Growth Inhibition Assay | IC50=341.123 μM | SANGER | ||
| C3A | Growth Inhibition Assay | IC50=311.802 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=309.983 μM | SANGER | ||
| NCI-H810 | Growth Inhibition Assay | IC50=310.57 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=304.32 μM | SANGER | ||
| L-428 | Growth Inhibition Assay | IC50=297.616 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=297.51 μM | SANGER | ||
| IGR-1 | Growth Inhibition Assay | IC50=295.659 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=294.409 μM | SANGER | ||
| C8166 | Growth Inhibition Assay | IC50=278.506 μM | SANGER | ||
| TGBC11TKB | Growth Inhibition Assay | IC50=278.178 μM | SANGER | ||
| RERF-LC-MS | Growth Inhibition Assay | IC50=276.007 μM | SANGER | ||
| COLO-680N | Growth Inhibition Assay | IC50=272.527 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=270.1 μM | SANGER | ||
| GAK | Growth Inhibition Assay | IC50=253.002 μM | SANGER | ||
| RPMI-8866 | Growth Inhibition Assay | IC50=249.27 μM | SANGER | ||
| NCI-H2347 | Growth Inhibition Assay | IC50=247.713 μM | SANGER | ||
| LS-1034 | Growth Inhibition Assay | IC50=246.266 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=246.09 μM | SANGER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=243.795 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=216.125 μM | SANGER | ||
| KNS-42 | Growth Inhibition Assay | IC50=216.574 μM | SANGER | ||
| RCM-1 | Growth Inhibition Assay | IC50=214.762 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=207.909 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=207.948 μM | SANGER | ||
| SW1116 | Growth Inhibition Assay | IC50=207.077 μM | SANGER | ||
| HuCCT1 | Growth Inhibition Assay | IC50=204.208 μM | SANGER | ||
| NCI-H650 | Growth Inhibition Assay | IC50=202.103 μM | SANGER | ||
| COLO-678 | Growth Inhibition Assay | IC50=201.45 μM | SANGER | ||
| HT-29 | Growth Inhibition Assay | IC50=201.212 μM | SANGER | ||
| SCC-9 | Growth Inhibition Assay | IC50=191 μM | SANGER | ||
| KYSE-150 | Growth Inhibition Assay | IC50=191.888 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=188.333 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=186.84 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=185.054 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=180.165 μM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=178.467 μM | SANGER | ||
| no-10 | Growth Inhibition Assay | IC50=178.134 μM | SANGER | ||
| MDA-MB-231 | Growth Inhibition Assay | IC50=177.503 μM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=166.845 μM | SANGER | ||
| NY | Growth Inhibition Assay | IC50=165.314 μM | SANGER | ||
| A673 | Growth Inhibition Assay | IC50=161.705 μM | SANGER | ||
| SAS | Growth Inhibition Assay | IC50=162.678 μM | SANGER | ||
| Capan-2 | Growth Inhibition Assay | IC50=160.553 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=158.674 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=154.694 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition Assay | IC50=153.064 μM | SANGER | ||
| BEN | Growth Inhibition Assay | IC50=153.928 μM | SANGER | ||
| KYSE-450 | Growth Inhibition Assay | IC50=151.539 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=149.928 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=147.878 μM | SANGER | ||
| OVCAR-8 | Growth Inhibition Assay | IC50=145.636 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=144.501 μM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=142.14 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=139.833 μM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=137.217 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=135.993 μM | SANGER | ||
| U-87-MG | Growth Inhibition Assay | IC50=133.604 μM | SANGER | ||
| NCI-H2087 | Growth Inhibition Assay | IC50=131.483 μM | SANGER | ||
| NCI-H1651 | Growth Inhibition Assay | IC50=131.243 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=128.988 μM | SANGER | ||
| BALL-1 | Growth Inhibition Assay | IC50=126.23 μM | SANGER | ||
| COLO-679 | Growth Inhibition Assay | IC50=126.753 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=126.158 μM | SANGER | ||
| SN12C | Growth Inhibition Assay | IC50=124.176 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=125.514 μM | SANGER | ||
| NCI-H2452 | Growth Inhibition Assay | IC50=122.21 μM | SANGER | ||
| SK-MEL-30 | Growth Inhibition Assay | IC50=123.244 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=121.676 μM | SANGER | ||
| SW1990 | Growth Inhibition Assay | IC50=120.951 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=117.398 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=109.28 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=107.777 μM | SANGER | ||
| HLE | Growth Inhibition Assay | IC50=105.282 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=100.121 μM | SANGER | ||
| SW684 | Growth Inhibition Assay | IC50=98.6654 μM | SANGER | ||
| NCI-H2029 | Growth Inhibition Assay | IC50=96.9566 μM | SANGER | ||
| NCI-H1792 | Growth Inhibition Assay | IC50=96.8992 μM | SANGER | ||
| SCH | Growth Inhibition Assay | IC50=96.3877 μM | SANGER | ||
| COLO-792 | Growth Inhibition Assay | IC50=95.2564 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=92.9106 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=91.5611 μM | SANGER | ||
| KYSE-410 | Growth Inhibition Assay | IC50=91.4042 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=89.9028 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=86.8872 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=86.1977 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=85.4641 μM | SANGER | ||
| DoTc2-4510 | Growth Inhibition Assay | IC50=84.2185 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=84.0892 μM | SANGER | ||
| HTC-C3 | Growth Inhibition Assay | IC50=83.4702 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=83.3071 μM | SANGER | ||
| PANC-08-13 | Growth Inhibition Assay | IC50=81.1768 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=80.2154 μM | SANGER | ||
| CAL-62 | Growth Inhibition Assay | IC50=80.095 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=79.0546 μM | SANGER | ||
| KYSE-180 | Growth Inhibition Assay | IC50=77.5454 μM | SANGER | ||
| PANC-10-05 | Growth Inhibition Assay | IC50=77.4243 μM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=75.5708 μM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=75.4516 μM | SANGER | ||
| NCI-H1437 | Growth Inhibition Assay | IC50=74.4048 μM | SANGER | ||
| NCI-H522 | Growth Inhibition Assay | IC50=72.3413 μM | SANGER | ||
| COLO-668 | Growth Inhibition Assay | IC50=71.8451 μM | SANGER | ||
| Mewo | Growth Inhibition Assay | IC50=71.505 μM | SANGER | ||
| KYSE-70 | Growth Inhibition Assay | IC50=70.7835 μM | SANGER | ||
| LCLC-103H | Growth Inhibition Assay | IC50=70.6705 μM | SANGER | ||
| SK-HEP-1 | Growth Inhibition Assay | IC50=69.9486 μM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=68.3238 μM | SANGER | ||
| SW620 | Growth Inhibition Assay | IC50=66.2039 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=65.8481 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=65.5649 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=65.0095 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=64.5514 μM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=64.1245 μM | SANGER | ||
| C-33-A | Growth Inhibition Assay | IC50=64.0957 μM | SANGER | ||
| NCI-H596 | Growth Inhibition Assay | IC50=62.7496 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=61.3903 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=60.5294 μM | SANGER | ||
| 647-V | Growth Inhibition Assay | IC50=60.1347 μM | SANGER | ||
| COLO-824 | Growth Inhibition Assay | IC50=60.0719 μM | SANGER | ||
| TCCSUP | Growth Inhibition Assay | IC50=59.5279 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=58.9506 μM | SANGER | ||
| MHH-ES-1 | Growth Inhibition Assay | IC50=58.4814 μM | SANGER | ||
| FTC-133 | Growth Inhibition Assay | IC50=58.0969 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=57.778 μM | SANGER | ||
| HPAF-II | Growth Inhibition Assay | IC50=56.4073 μM | SANGER | ||
| MKN7 | Growth Inhibition Assay | IC50=56.0285 μM | SANGER | ||
| UACC-62 | Growth Inhibition Assay | IC50=55.1046 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=54.6322 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=49.4793 μM | SANGER | ||
| HT55 | Growth Inhibition Assay | IC50=49.1474 μM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=48.4016 μM | SANGER | ||
| U-118-MG | Growth Inhibition Assay | IC50=48.3702 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=48.2845 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=47.3736 μM | SANGER | ||
| RO82-W-1 | Growth Inhibition Assay | IC50=46.9822 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=45.9076 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=45.8967 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=45.4842 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=45.2548 μM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=43.6019 μM | SANGER | ||
| NCI-H1573 | Growth Inhibition Assay | IC50=43.3477 μM | SANGER | ||
| Calu-6 | Growth Inhibition Assay | IC50=43.2382 μM | SANGER | ||
| HCC1937 | Growth Inhibition Assay | IC50=42.7843 μM | SANGER | ||
| UMC-11 | Growth Inhibition Assay | IC50=41.263 μM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=40.9113 μM | SANGER | ||
| BxPC-3 | Growth Inhibition Assay | IC50=40.5686 μM | SANGER | ||
| COLO-741 | Growth Inhibition Assay | IC50=40.1304 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=39.8274 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=39.5512 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=39.3424 μM | SANGER | ||
| EFO-21 | Growth Inhibition Assay | IC50=38.9349 μM | SANGER | ||
| SW1417 | Growth Inhibition Assay | IC50=38.0552 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=36.9033 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=33.9822 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=33.863 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=33.6605 μM | SANGER | ||
| SW626 | Growth Inhibition Assay | IC50=33.1776 μM | SANGER | ||
| COR-L23 | Growth Inhibition Assay | IC50=32.9073 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=30.4942 μM | SANGER | ||
| ZR-75-30 | Growth Inhibition Assay | IC50=30.2383 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=27.721 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=27.6012 μM | SANGER | ||
| NCI-H226 | Growth Inhibition Assay | IC50=27.4578 μM | SANGER | ||
| SW948 | Growth Inhibition Assay | IC50=27.1344 μM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=27.0879 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=27.0803 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=26.5021 μM | SANGER | ||
| CHP-134 | Growth Inhibition Assay | IC50=26.3867 μM | SANGER | ||
| GMS-10 | Growth Inhibition Assay | IC50=26.2353 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=26.2103 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=26.0949 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=25.0458 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=23.8133 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=23.4232 μM | SANGER | ||
| NCI-H1650 | Growth Inhibition Assay | IC50=22.764 μM | SANGER | ||
| SK-N-MC | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | Function assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | MK-2206 2HCl是一种高度选择性的Akt1/2/3抑制剂，在无细胞试验中IC50分别为8 nM/12 nM/65 nM；对250种其他蛋白激酶没有抑制活性。MK-2206 2HCl 在肿瘤细胞中可诱导自噬和凋亡。Phase 2。 | ||||||
|---|---|---|---|---|---|---|---|
| 特性 | MK-2206是第一个进入临床研究阶段的Akt小分子变构抑制剂。 | ||||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | MK-2206是变构抑制剂，由pleckstrin同源结构域激活。MK-2206抑制Akt的苏氨酸308位点和丝氨酸473位点的自身磷酸化作用。另外，MK-2206阻止Akt调节的下游信号分子（包括TSC2, PRAS40，及核糖体S6蛋白）的磷酸化作用。与抑制Ras 突变型细胞系(如NCI-H358, NCI-H23, NCI-H1299, 和Calu-6)相比，MK-2206 更有效地抑制Ras野生型细胞系(如A431, HCC827, 和NCI-H292)。MK-2206和细胞毒素药剂联用作用于肺部NCI-H460肿瘤细胞或者卵巢A2780肿瘤细胞，MK-2206也显示出协同效应。[1] |
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|---|---|---|---|---|
| 激酶实验 | Akt激酶实验 | |||
| 通过得到的GSK 生物素肽段基质测定Akt激酶。使用含镧系金属螯合物偶联单抗的均相时间分辨荧光(HTRF)测定肽段磷酸化程度，这种单抗专门作用于与链霉亲和素——藻蓝素(SA-APC)载体相结合的磷酸化作用，SA-APC载体可以结合到肽段的部分生物素上。当镧系金属螯合物与藻蓝素相接触时，无辐射的能量从镧系金属螯合物传递给藻蓝素，然后藻蓝素发射波值为655纳米的光线。工作液:100X 蛋白酶抑制剂混合物(PIC)：1mg/ml苯甲脒，0.5 mg/ml 抑肽素, 0.5 mg/ml亮抑肽酶, 0.5 mg/ml 抑肽酶。10X实验 buffer: 500 mM HEPES（pH 为7.5）, 1% PEG, 16.6 mM EDTA, 1 mM EGTA, 1% BSA, 20 mM 9-甘油磷酸。抑制 buffer：50 mM HEPES（pH为7.3）, 16.6 mM EDTA, 0.1% BSA, 0.1% Triton X-100, 0.17 nM 标记的单抗, 0.0067mg/ml SA-APC。ATP/MgCl2工作液: 1X 实验buffer, 1 mM DTT, 1X PIC, 5% 甘油, 激活的Akt。肽段工作液：1X实验buffer, 1 mM DTT, 1X PIC, 5% 甘油 2 TM GSK生物素肽段。工作液加到合适的孔中，然后加入总负荷为16的 ATP/MgCl2，反应开始。含MK-2206的实验组和对照组加入总负荷为10的肽段工作液。然后加入总负荷为13的酶液，混匀。反应进行50分钟，然后加入总负荷为60的均相时间分辨荧光抑制buffer停止反应。阻断的反应在室温下温育30分钟以上，然后使用仪器读数。 | ||||
| 细胞实验 | 细胞系 | A431, HCC827, NCI-H292, NCI-H358, NCI-H23, NCI-H1299, Calu-6,和NCI-H460细胞 | ||
| 浓度 | 0, 0.3, 1,和3 μM | |||
| 孵育时间 | 72或96小时 | |||
| 方法 | MK-2206溶解在DMSO中，在实验使用前用培养基稀释。细胞按2~3×103密度接种在96孔板上，温育24小时。MK-2206 (分为0, 0.3, 1,和3 μmol四组)处理细胞，72或者96小时后，测定细胞增殖情况。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-AKT(T308) / p-AKT(S473) / pGSK3β(S9) / pFOXO1 / pPRAS(T246) / pBAD / pS6K(T389) / p4E-BP1 |
|
22932669 | |
| Growth inhibition assay | Cell viability |
|
24665203 | |
| Immunofluorescence | LC3 CFTR/LC3 HMGA2 |
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24490764 | |
| ELISA | VEGFA |
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29449553 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | MK-2206和这些细胞毒素药剂联用作用于NCI-H292移植瘤，MK-2206显示出非常有效的抗癌活性。卵巢癌A2780移植瘤中，按动物体重，每千克处理240mg MK-2206,则可抑制70%以上的Akt1/2在苏氨酸308位点和丝氨酸473位点的磷酸化，导致肿瘤生长抑制率达到60%。[1] |
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| 动物实验 | Animal Models | 携带SK-OV-3, NCI-H292, HCC70, PC-3,和NCI-H460模型的雄性CD1裸鼠 |
| Dosages | 120 mg/kg | |
| Administration | 口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01480154 | Active not recruiting | Advanced Malignant Solid Neoplasm|Stage III Cutaneous Melanoma AJCC v7|Stage III Prostate Cancer AJCC v7|Stage III Renal Cell Cancer AJCC v7|Stage IIIA Cutaneous Melanoma AJCC v7|Stage IIIB Cutaneous Melanoma AJCC v7|Stage IIIC Cutaneous Melanoma AJCC v7|Stage IV Cutaneous Melanoma AJCC v6 and v7|Stage IV Prostate Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7 |
National Cancer Institute (NCI) |
November 23 2011 | Phase 1 |
| NCT01466868 | Terminated | Diffuse Large B Cell Lymphoma |
Centre Leon Berard|National Cancer Institute France |
November 2011 | Phase 2 |
化学信息&溶解度
| 分子量 | 480.39 | 分子式 | C25H21N5O.2HCl |
| CAS号 | 1032350-13-2 | SDF | Download MK-2206 2HCl SDF |
| Smiles | C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 25 mg/mL ( (52.04 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : 2 mg/mL (4.16 mM) Ethanol : Insoluble |
摩尔浓度计算器 |
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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。
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常见问题及建议解决方法
问题 1:
What is your recommendation for preparing the solution and how would you deliver it to the mice (i.p. or gavage)?
回答：
You can resuspend MK-2206 in 15% Captisol at up to 17mg/ml. It's a suspension and is for oral gavage use only.
问题 2:
I would want to know if MK-2206 could cross the blood brain barrier?
回答：
MK-2206 can cross BBB based on the following reference: https://clinicaltrials.gov/ct2/show/NCT01249105.
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