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 mTORPI3K,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

NU7441 (KU-57788) Chemical Structure

CAS: 503468-95-9

规格 价格 库存 购买数量
5mg 565.91 现货
10mg 974.57 现货
50mg 3040.41 现货
200mg 7928.18 现货
1g 16134.3 现货
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常与NU7441 (KU-57788)一起在实验中被使用的化合物

KU-0060648


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。

Robert F, et al. Genome Med. 2015 Aug 27;7(1):93.

KU-55933


NU7441和KU-55933联合治疗显着增加MDCK细胞的X射线细胞毒性。

Koike M, et al. J Vet Med Sci. 2022 Nov; 84(11): 1485–1490.

Olaparib (AZD2281)


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。

Zeng L, et al. Front Genet. 2020 Sep 10;11:1036.

NU7026


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。

Li LY, et al. Front Pharmacol. 2021 Feb 8;11:629266.

Gemcitabine


NU7441与Gemcitabine联合减少荷瘤小鼠的肿瘤体积。

Han J, et al. Cancer Med. 2023 Mar;12(5):5939-5952.

NU7441 (KU-57788)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
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
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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 mTORPI3K,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
DNA-PK [1]
(Cell-free assay)
mTOR [1]
(cell-free assay)
PI3K [1]
(cell-free assay)
14 nM 1.7 μM 5 μM
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, 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。提高诱导的γH2AX病灶水平,也相应地降低诱导的细胞死亡。[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, 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。

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) 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)

体外溶解度
批次:

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
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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:
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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