NU7441 (KU-57788)
NU7441 (KU-57788)是一种高度有效的，选择性DNA-PK抑制剂，在无细胞试验中IC50为14 nM，也会抑制 mTOR 和 PI3K，对应的IC50值分别为1.7 μM和5 μM。它可降低NHEJ的频率，而增强Cas9介导DNA剪接后发生的同源重组修复率。
NU7441 (KU-57788) Chemical Structure
CAS: 503468-95-9
客户使用Selleck的NU7441 (KU-57788)发表文献255篇
产品质控
批次：
纯度：
99.94%
99.94
常与NU7441 (KU-57788)一起在实验中被使用的化合物
NU7441和KU-0060648降低非同源末端连接(NHEJ)途径的频率，同时增加同源定向重组(HDR)的速率。
NU7441和KU-55933联合治疗显着增加MDCK细胞的X射线细胞毒性。
NU7441和Olaparib联合IR可增强SCC1和SCC6细胞系以及小鼠中HPV阴性HNSCC的抑制作用。
NU7441和NU7026是有效的DNA-PK抑制剂，可抑制DSB修复途径并增强癌细胞对电离辐射或化学增强的敏感性。
NU7441 (KU-57788)相关产品
| 相关化合物库 | FDA药物库 天然产物库 凋亡分子化合物库 DNA损伤/ DNA修复化合物库 细胞周期化合物库 | 点击展开 |
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相关信号通路图
DNA-PK抑制剂选择性比较
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 |
|---|---|---|---|---|---|
| INA-6 | Function assay | 10 uM | 4 hrs | Inhibition of heat shock response in human INA-6 cells assessed as reduction in HSF-1 mediated upregulation of the HSP72 protein expression at 10 uM preincubated for 4 hrs followed by HSP90 inhibitor and HSR inducer NVP-AUY922 addition measured after 4 hr | 28453931 |
| INA-6 | Function assay | 10 uM | 4 hrs | Inhibition of heat shock response in human INA-6 cells assessed as reduction in HSF-1 mediated upregulation of the HSP72 mRNA expression at 10 uM preincubated for 4 hrs followed by HSP90 inhibitor and HSR inducer NVP-AUY922 addition measured after 4 hrs b | 28453931 |
| INA-6 | Function assay | 10 uM | 4 hrs | Downregulation of NVP-AUY922-induced HSF-1 protein expression in human INA-6 cells at 10 uM preincubated for 4 hrs followed by NVP-AUY922 addition measured after 4 hrs by Western blot method | 28453931 |
| INA-6 | Function assay | 10 uM | 4 hrs | Inhibition of NVP-AUY922-induced HSF-1 phosphorylation in human INA-6 cells at 10 uM preincubated for 4 hrs followed by NVP-AUY922 addition measured after 4 hrs by Western blot method | 28453931 |
| INA-6 | Function assay | 10 uM | 4 hrs | Downregulation of NVP-AUY922-induced HSF-1 mRNA expression in human INA-6 cells at 10 uM preincubated for 4 hrs followed by NVP-AUY922 addition measured after 4 hrs by RT-PCR method | 28453931 |
| NCI-H1755 | Growth Inhibition Assay | IC50=10.2428 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=10.2426 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=9.96939 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=9.70137 μM | SANGER | ||
| HCC1937 | Growth Inhibition Assay | IC50=9.69865 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=9.1661 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=9.09612 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=8.95964 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=8.37762 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=8.37589 μM | SANGER | ||
| HT | Growth Inhibition Assay | IC50=8.3649 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=8.34686 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=8.2793 μM | SANGER | ||
| PC-3 | Growth Inhibition Assay | IC50=8.27392 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=8.25093 μM | SANGER | ||
| CHP-134 | Growth Inhibition Assay | IC50=8.24185 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=8.21122 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=8.16962 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=8.03654 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=7.94352 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=7.74955 μM | SANGER | ||
| RO82-W-1 | Growth Inhibition Assay | IC50=7.74533 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=7.7433 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=7.71743 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=7.64131 μM | SANGER | ||
| AU565 | Growth Inhibition Assay | IC50=7.59833 μM | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=7.36823 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=7.32622 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=7.31328 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=7.30203 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=7.30051 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=7.26659 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition Assay | IC50=7.24359 μM | SANGER | ||
| EPLC-272H | Growth Inhibition Assay | IC50=7.16246 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=7.09786 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=6.97588 μM | SANGER | ||
| NCI-H2347 | Growth Inhibition Assay | IC50=6.93213 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=6.91068 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=6.82502 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=6.79761 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=6.69369 μM | SANGER | ||
| UM-UC-3 | Growth Inhibition Assay | IC50=6.64334 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=6.63291 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=6.32721 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=6.17522 μM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=6.07338 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=5.83606 μM | SANGER | ||
| PFSK-1 | Growth Inhibition Assay | IC50=5.62194 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=5.56599 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=5.53661 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=5.51378 μM | SANGER | ||
| KYSE-410 | Growth Inhibition Assay | IC50=5.47636 μM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=5.41773 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=5.3242 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=5.32024 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=5.296 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=5.25292 μM | SANGER | ||
| HCC70 | Growth Inhibition Assay | IC50=5.03939 μM | SANGER | ||
| MDA-MB-415 | Growth Inhibition Assay | IC50=5.00314 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=4.80128 μM | SANGER | ||
| MEL-HO | Growth Inhibition Assay | IC50=4.77989 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=4.77116 μM | SANGER | ||
| SN12C | Growth Inhibition Assay | IC50=4.71898 μM | SANGER | ||
| EFO-27 | Growth Inhibition Assay | IC50=4.66525 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=4.60715 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=4.59685 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=4.58263 μM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=4.44953 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=4.40888 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=4.32921 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=4.27935 μM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=4.25813 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=4.24854 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=4.22524 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=3.9149 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=3.91041 μM | SANGER | ||
| YH-13 | Growth Inhibition Assay | IC50=3.87189 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=3.65312 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=3.62676 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=3.61736 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=3.59985 μM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=3.59368 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=3.48077 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=3.46729 μM | SANGER | ||
| NY | Growth Inhibition Assay | IC50=3.45022 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=3.44993 μM | SANGER | ||
| SK-MEL-30 | Growth Inhibition Assay | IC50=3.42598 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=3.41341 μM | SANGER | ||
| PANC-08-13 | Growth Inhibition Assay | IC50=3.41278 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=3.28085 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=3.20352 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=3.1531 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=2.77328 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=2.69633 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=2.67924 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=2.61338 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=2.56702 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=2.56023 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=2.38783 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=2.3739 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=2.35564 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=2.21888 μM | SANGER | ||
| G-361 | Growth Inhibition Assay | IC50=2.2168 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=2.19909 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=2.16687 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=2.16609 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=2.1649 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=2.14146 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=1.79479 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=1.74013 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=1.69361 μM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=1.58294 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=1.5535 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=1.4584 μM | SANGER | ||
| 639-V | Growth Inhibition Assay | IC50=1.44128 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=1.3819 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=1.24745 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=1.21368 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=1.18093 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=1.14231 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=1.11546 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=0.98833 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=0.86749 μM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=0.62216 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=0.60994 μM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=0.46636 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=0.32345 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=0.28407 μM | SANGER | ||
| A172 | Growth Inhibition Assay | IC50=0.15316 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=0.02143 μM | SANGER | ||
| NCI-H1437 | Growth Inhibition Assay | IC50=10.5725 μM | SANGER | ||
| VM-CUB-1 | Growth Inhibition Assay | IC50=10.6164 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=10.6404 μM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=10.7145 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=10.7559 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=10.7626 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=10.8094 μM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=10.8202 μM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=10.8347 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=10.8376 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=10.8586 μM | SANGER | ||
| GMS-10 | Growth Inhibition Assay | IC50=10.8971 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=10.9071 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=11.0559 μM | SANGER | ||
| HTC-C3 | Growth Inhibition Assay | IC50=11.0714 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=11.0723 μM | SANGER | ||
| NCI-H1563 | Growth Inhibition Assay | IC50=11.1011 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=11.4811 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=11.6824 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=11.7267 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=11.7508 μM | SANGER | ||
| NCI-H650 | Growth Inhibition Assay | IC50=11.8961 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=11.9315 μM | SANGER | ||
| COLO-679 | Growth Inhibition Assay | IC50=11.946 μM | SANGER | ||
| FTC-133 | Growth Inhibition Assay | IC50=12.0076 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=12.0569 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=12.1902 μM | SANGER | ||
| BALL-1 | Growth Inhibition Assay | IC50=12.2662 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=12.3074 μM | SANGER | ||
| HOP-92 | Growth Inhibition Assay | IC50=12.5233 μM | SANGER | ||
| M14 | Growth Inhibition Assay | IC50=13.0335 μM | SANGER | ||
| SKG-IIIa | Growth Inhibition Assay | IC50=13.0554 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=13.058 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=13.1356 μM | SANGER | ||
| NCI-H2030 | Growth Inhibition Assay | IC50=13.2062 μM | SANGER | ||
| SNU-423 | Growth Inhibition Assay | IC50=13.381 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=13.6232 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=13.7475 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=13.7513 μM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=14.0727 μM | SANGER | ||
| AGS | Growth Inhibition Assay | IC50=14.1319 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=14.1488 μM | SANGER | ||
| BFTC-909 | Growth Inhibition Assay | IC50=14.5055 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=14.7706 μM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=15.1067 μM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=15.2333 μM | SANGER | ||
| 647-V | Growth Inhibition Assay | IC50=15.2705 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=15.3291 μM | SANGER | ||
| ME-180 | Growth Inhibition Assay | IC50=15.4783 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=15.5623 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=15.6245 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=15.6437 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=15.8919 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=15.8928 μM | SANGER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=15.971 μM | SANGER | ||
| SW1783 | Growth Inhibition Assay | IC50=16.0993 μM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=16.5365 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=16.5586 μM | SANGER | ||
| PANC-03-27 | Growth Inhibition Assay | IC50=16.7662 μM | SANGER | ||
| RH-1 | Growth Inhibition Assay | IC50=16.825 μM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=16.8446 μM | SANGER | ||
| ZR-75-30 | Growth Inhibition Assay | IC50=16.9361 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=16.9408 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=17.0079 μM | SANGER | ||
| SW684 | Growth Inhibition Assay | IC50=17.0154 μM | SANGER | ||
| RPMI-8866 | Growth Inhibition Assay | IC50=17.0699 μM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=17.5201 μM | SANGER | ||
| NCI-H2291 | Growth Inhibition Assay | IC50=18.4345 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=18.488 μM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=18.5452 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=18.7427 μM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=19.0714 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=19.1591 μM | SANGER | ||
| NCI-H596 | Growth Inhibition Assay | IC50=19.6391 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=19.8926 μM | SANGER | ||
| D-336MG | Growth Inhibition Assay | IC50=19.9322 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=20.1559 μM | SANGER | ||
| HEC-1 | Growth Inhibition Assay | IC50=20.4978 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=20.5443 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=20.5583 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=20.5688 μM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=20.6719 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=21.0396 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=21.2258 μM | SANGER | ||
| CW-2 | Growth Inhibition Assay | IC50=21.2705 μM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=21.36 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=21.376 μM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=21.4481 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=21.6113 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=21.6316 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=21.8152 μM | SANGER | ||
| NCI-H2452 | Growth Inhibition Assay | IC50=21.8647 μM | SANGER | ||
| HPAF-II | Growth Inhibition Assay | IC50=21.8923 μM | SANGER | ||
| D-542MG | Growth Inhibition Assay | IC50=21.9069 μM | SANGER | ||
| NCI-H630 | Growth Inhibition Assay | IC50=22.0296 μM | SANGER | ||
| TGBC11TKB | Growth Inhibition Assay | IC50=22.049 μM | SANGER | ||
| BCPAP | Growth Inhibition Assay | IC50=22.611 μM | SANGER | ||
| HLE | Growth Inhibition Assay | IC50=22.697 μM | SANGER | ||
| NCI-H727 | Growth Inhibition Assay | IC50=22.735 μM | SANGER | ||
| RD | Growth Inhibition Assay | IC50=22.7518 μM | SANGER | ||
| NCI-H522 | Growth Inhibition Assay | IC50=22.8431 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=23.0641 μM | SANGER | ||
| SK-LU-1 | Growth Inhibition Assay | IC50=23.4683 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=23.7863 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=23.8527 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=24.0161 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=24.1028 μM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=24.3093 μM | SANGER | ||
| MKN1 | Growth Inhibition Assay | IC50=24.68 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=24.8519 μM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=25.1845 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=25.2208 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=25.2483 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=25.5807 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=25.5898 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=26.0283 μM | SANGER | ||
| U-118-MG | Growth Inhibition Assay | IC50=26.0808 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=26.234 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=27.0704 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=27.11 μM | SANGER | ||
| LB373-MEL-D | Growth Inhibition Assay | IC50=27.1294 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=27.1817 μM | SANGER | ||
| RMG-I | Growth Inhibition Assay | IC50=27.2029 μM | SANGER | ||
| SW1088 | Growth Inhibition Assay | IC50=27.5042 μM | SANGER | ||
| SK-OV-3 | Growth Inhibition Assay | IC50=27.7593 μM | SANGER | ||
| KP-N-YN | Growth Inhibition Assay | IC50=27.8043 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=28.2456 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=28.5582 μM | SANGER | ||
| MKN7 | Growth Inhibition Assay | IC50=28.5964 μM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=28.7401 μM | SANGER | ||
| KYSE-450 | Growth Inhibition Assay | IC50=28.8091 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=29.2906 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=29.3048 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=29.4299 μM | SANGER | ||
| RT-112 | Growth Inhibition Assay | IC50=29.4611 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=29.8544 μM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=29.8786 μM | SANGER | ||
| AM-38 | Growth Inhibition Assay | IC50=30.0606 μM | SANGER | ||
| AsPC-1 | Growth Inhibition Assay | IC50=30.8053 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=30.8737 μM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=30.9638 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=31.0744 μM | SANGER | ||
| NCI-H1703 | Growth Inhibition Assay | IC50=31.0905 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=31.4651 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=31.9181 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=32.0128 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=32.0739 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=32.0838 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=32.3922 μM | SANGER | ||
| MHH-ES-1 | Growth Inhibition Assay | IC50=32.4872 μM | SANGER | ||
| C-33-A | Growth Inhibition Assay | IC50=32.7728 μM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=32.9495 μM | SANGER | ||
| Detroit562 | Growth Inhibition Assay | IC50=33.6657 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=33.9322 μM | SANGER | ||
| NCI-H1395 | Growth Inhibition Assay | IC50=34.0799 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=36.4743 μM | SANGER | ||
| NCI-H520 | Growth Inhibition Assay | IC50=36.7541 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=37.3344 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=37.8089 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=38.124 μM | SANGER | ||
| HT-3 | Growth Inhibition Assay | IC50=38.4436 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=38.9519 μM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=39.0124 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=39.1852 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=39.1894 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=39.2448 μM | SANGER | ||
| HMV-II | Growth Inhibition Assay | IC50=39.5047 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=40.1502 μM | SANGER | ||
| SW13 | Growth Inhibition Assay | IC50=40.519 μM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=40.8066 μM | SANGER | ||
| MDA-MB-157 | Growth Inhibition Assay | IC50=40.9462 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=41.8714 μM | SANGER | ||
| HuCCT1 | Growth Inhibition Assay | IC50=42.5289 μM | SANGER | ||
| KYSE-510 | Growth Inhibition Assay | IC50=43.1754 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=44.0304 μM | SANGER | ||
| SW900 | Growth Inhibition Assay | IC50=44.0758 μM | SANGER | ||
| CAS-1 | Growth Inhibition Assay | IC50=44.0991 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=44.5658 μM | SANGER | ||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=44.6112 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=44.781 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=44.7903 μM | SANGER | ||
| LCLC-103H | Growth Inhibition Assay | IC50=44.8703 μM | SANGER | ||
| U-87-MG | Growth Inhibition Assay | IC50=45.1022 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=45.1379 μM | SANGER | ||
| OVCAR-8 | Growth Inhibition Assay | IC50=45.3564 μM | SANGER | ||
| KYSE-150 | Growth Inhibition Assay | IC50=47.1052 μM | SANGER | ||
| OE33 | Growth Inhibition Assay | IC50=47.1429 μM | SANGER | ||
| CAL-62 | Growth Inhibition Assay | IC50=47.4068 μM | SANGER | ||
| TCCSUP | Growth Inhibition Assay | IC50=47.6264 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=47.6621 μM | SANGER | ||
| CP66-MEL | Growth Inhibition Assay | IC50=48.0704 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=48.1874 μM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=48.279 μM | SANGER | ||
| BT-549 | Growth Inhibition Assay | IC50=48.3729 μM | SANGER | ||
| IGR-1 | Growth Inhibition Assay | IC50=48.6645 μM | SANGER | ||
| NCI-H1299 | Growth Inhibition Assay | IC50=48.7248 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=49.9268 μM | SANGER | ||
| CLL | Function assay | Inhibition of DNA-PK autophosphorylation at Ser2056 residue in human CLL cells by Western blot method, IC50 = 0.03 μM. | 22835870 | ||
| HeLa | Function assay | Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells, EC50 = 0.212 μM. | 23855836 | ||
| CHO | Function assay | Inhibition of human ERG expressed in cisapride treated CHO cells by Ion Works assay, IC50 = 14 μM. | 23855836 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS 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 | NU7441 (KU-57788)是一种高度有效的，选择性DNA-PK抑制剂，在无细胞试验中IC50为14 nM，也会抑制 mTOR 和 PI3K，对应的IC50值分别为1.7 μM和5 μM。它可降低NHEJ的频率，而增强Cas9介导DNA剪接后发生的同源重组修复率。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | NU7441抑制DNA依赖性蛋白激酶 (DNA-PK) 比抑制其他PI3K相关激酶 (PIKK)家族成员选择性高，IC50 为14 nM。[1] 电离辐射诱导或Etoposide诱导 DNA 损伤后，1 μM NU7441提高γH2AX病灶的持久性。NU7441 浓度为 0.5 μM 或 1 μM时，作用于SW620 和 LoVo细胞，显著提高电离辐射，Etoposide, 和 Doxorubicin 诱导的G2-M累积增多。[2] NU7441浓度为1 μM时，引起 Doxorubicin和电离辐射诱导的DNA双链断裂的持久性，也稍微降低同源重组活性 DNA-PK充足的 M059-Fus-1和 DNA-PK缺陷的 M059 J人类肿瘤细胞。[3] NU7441浓度为 10 μM 时，作用于缺乏和表达polη的细胞，抑制UV诱导 RPA p34过度磷酸化。[4] NU7441 浓度为1 μM时，作用于慢性淋巴细胞性白血病细胞。提高Fludarabine诱导的γH2AX病灶水平，也相应地降低Fludarabine诱导的细胞死亡。[5] NU7441浓度为 1 μM时，作用于慢性淋巴细胞性白血病细胞，抑制Mitoxantrone诱导的DNA-PKcs自磷酸化和修复。[6]它可降低NHEJ的频率，而增强Cas9介导DNA剪接后发生的同源重组修复率 [7]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | SW620, LoVo, V3-YAC和 V3细胞 | ||
| 浓度 | 0.5 μM或 1 μM | |||
| 孵育时间 | 17 小时 | |||
| 方法 | 通过克隆实验测定NU7441，Etoposide, Doxorubicin, 和电离辐射作用于SW620, LoVo, V3,和 V3-YAC细胞存活的效果。在有或无 NU7441(0.5 或 1.0 μM)存在时，使用Etoposide 或Doxorubicin处理6孔板或6-cm盘中指数生长的细胞16小时。放射增敏研究中， NU7441加到细胞中，1小时后，使用辐射处理。使用γ-射线 (3.1 Gy/min 137Cesium)处理V3和V3-YAC 细胞。使用可用设备，使用X-射线 (2.9 Gy/min at 230 kV, 10 mA) 处理SW620 和 LoVo 细胞。辐射处理后，在有或无NU7441存在时，细胞再温育16小时。胰蛋白酶消化，收集细胞，计数，然后按每盘 100 到105 的密度接种在10-cm 直径的Petri盘中， 盘中含无药物培养基，用于形成集落。使用结晶紫对集落进行染色，10 到 14天后，使用自动集落计数器计数。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-DNA-PKcs / DNA-PKcs / p-ATM / ATM / p-ATR / ATR / Ku70 / p-CHK1 / p-CHK2/ p-AKT / RAD51 p-mTOR(Ser2448) / mTOR / p-S6K(Thr389) |
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29344644 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | NU7441按 10 mg/kg剂量腹腔注射处理携带SW620移植瘤的小鼠，按无毒剂量处理至少4小时，然后提高 Etoposide诱导的肿瘤生长延迟2倍。 [2] | |
|---|---|---|
| 动物实验 | Animal Models | 携带 SW620移植瘤的雌性裸鼠 |
| Dosages | 10 mg/kg | |
| Administration | 腹腔注射 | |
化学信息&溶解度
| 分子量 | 413.49 | 分子式 | C25H19NO3S |
| CAS号 | 503468-95-9 | SDF | Download NU7441 (KU-57788) SDF |
| Smiles | C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC5=C4SC6=CC=CC=C56 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 5 mg/mL ( (12.09 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
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如果有其他问题，请给我们留言。
* 必填项
常见问题及建议解决方法
问题 1:
Could you please suggest formulations of the drug for in vivo injection?
回答：
We tested the following formulation for in vivo use, 4% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 1mg/mL. It is a clear solution.
问题 2:
Previous aliquots were clear and colorless while this time, it becomes yellow when the powder was dissolved in DMSO? Could you advice on this?
回答：
Slight color variation due to different processing is normal and usually doesn't interfere with the function.
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