NU7441 (KU-57788)

NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.

NU7441 (KU-57788)化学構造

CAS No. 503468-95-9

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 59500 国内在庫あり
JPY 145500 国内在庫あり
JPY 295500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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NU7441 (KU-57788)と併用されることが多い化合物

KU-0060648


NU7441 and KU-0060648 reduce the frequency of the non-homologous end joining (NHEJ) pathway while increasing the rate of homology-directed recombination (HDR).

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

KU-55933


NU7441 and KU-55933 combination treatment significantly increase X-ray cytotoxicity in MDCK cells.

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

NU7026


NU7441 and NU7026 are potent DNA-PK inhibitors that inhibit the DSBs repair pathway and enhance the sensitivity of cancer cells to ionizing radiation or chemo-potentiation.

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

NU7441 (KU-57788)関連製品

シグナル伝達経路

DNA-PK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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

製品説明 NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.
Targets
DNA-PK [1]
(Cell-free assay)
mTOR [1]
(cell-free assay)
PI3K [1]
(cell-free assay)
14 nM 1.7 μM 5 μM
In Vitro
In vitro

NU7441 increases the persistence of γH2AX foci after ionizing radiation–induced DNA damage. NU7441 (0.5 μM or 1 μM) appreciably increases G2-M accumulation induced by ionizing radiation, and doxorubicin in both SW620 and LoVo cells. [2] NU7441 causes persistence of doxorubicin- and ionising radiation-induced DNA double-strand break and also slightly decreases homologous recombination activity DNA-PK-proficient M059-Fus-1 and DNA-PK-deficient M059 J human tumour cells. [3] NU7441 inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner both in cells lacking and cells expressing polymerase η. [4] NU7441 increases levels of -induced γH2AX foci and correspondingly decreased -induced cell death in chronic lymphocytic leukemia cells. [5] NU7441 also inhibits -induced DNA-PKcs autophosphorylation and repair in chronic lymphocytic leukemia cells. [6] It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage[7].

細胞実験 細胞株 SW620, LoVo, V3-YAC and V3 cells
濃度 0.5 μM or 1 μM
反応時間 17 hours
実験の流れ

The effect of NU7441 on cellular survival following exposure to doxorubicin, and ionizing radiation is measured in SW620, LoVo, V3, and V3-YAC cells by clonogenic assays. Briefly, growing cells in six-well plates or 6-cm dishes are exposed to doxorubicin with or without NU7441 (0.5 or 1.0 μM) for 16 hours. For radiosensitization studies, NU7441 is added to the cells 1 hour before irradiation. V3 and V3-YAC cells are exposed to γ-irradiation (3.1 Gy/min 137Cesium). SW620 and LoVo are exposed to X-irradiation (2.9 Gy/min at 230 kV, 10 mA) due to the equipment available. After irradiation, the cells are incubated with or without NU7441 for a further 16 hours. Cells are then harvested by trypsinization, counted, and seeded into 10-cm diameter Petri dishes at densities varying from 100 to 105 per dish in drug-free medium for colony formation. Colonies are stained with crystal violet after 10 to 14 days and counted with an automated colony counter. The survival reduction factor (SRF) is calculated as the surviving fraction of cells in the absence of NU7441 divided by the surviving fraction of cells in the presence of NU7441 for any given dose or concentration of cytotoxic agent. The dose modification ratio (DMR90) is calculated as the concentration/dose of cytotoxic agent required to kill 90% of the cells in the absence of NU7441 divided by the concentration/dose of cytotoxic agent required to kill 90% of the cells in the presence of NU7441.

実験結果図 Methods Biomarkers 結果図 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
In Vivo
In Vivo

NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases induced tumor growth delay 2-fold in mice bearing SW620 xenografts. [2]

動物実験 動物モデル Female rude mice bearing SW620 xenografts
投与量 10 mg/kg
投与経路 Intraperitoneally administrated

化学情報

分子量 413.49 化学式

C25H19NO3S

CAS No. 503468-95-9 SDF Download NU7441 (KU-57788) SDFをダウンロードする
Smiles C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC5=C4SC6=CC=CC=C56
保管

In vitro
Batch:

DMSO : 5 mg/mL ( (12.09 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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よくある質問(FAQ)

質問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.

質問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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