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Nutlin-3a inibitore di MDM2

N. Cat.S8059

Nutlin-3a ((-)-Nutlin-3), l'enantiomero attivo di Nutlin-3, inibisce l'interazione p53/MDM2 con una IC50 di 90 nM in un saggio senza cellule. Nutlin-3a induce autophagy e apoptosis in modo p53-dipendente.
Nutlin-3a MDM2/MDMX Inibitore Chemical Structure

Struttura chimica

Peso molecolare: 581.49

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Controllo Qualità (Quality Control)

Lotto: Purezza: 99.79%
99.79

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dell'attività PMID
MV-4-11 Growth Inhibition Assay IC50=0.61237 μM SANGER
H4 Growth Inhibition Assay IC50=0.6628 μM SANGER
PA-1 Growth Inhibition Assay IC50=0.87096 μM SANGER
NKM-1 Growth Inhibition Assay IC50=1.04931 μM SANGER
NEC8 Growth Inhibition Assay IC50=1.21572 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=1.26701 μM SANGER
K5 Growth Inhibition Assay IC50=1.42072 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=1.60854 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=1.78604 μM SANGER
CHP-212 Growth Inhibition Assay IC50=1.81369 μM SANGER
CTB-1 Growth Inhibition Assay IC50=2.02246 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=2.32853 μM SANGER
A101D Growth Inhibition Assay IC50=2.3501 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=2.42279 μM SANGER
ES4 Growth Inhibition Assay IC50=2.43155 μM SANGER
SW780 Growth Inhibition Assay IC50=2.50883 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=2.5411 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=2.56214 μM SANGER
ML-2 Growth Inhibition Assay IC50=2.56576 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=2.57451 μM SANGER
JVM-3 Growth Inhibition Assay IC50=2.59324 μM SANGER
A3-KAW Growth Inhibition Assay IC50=2.61818 μM SANGER
DK-MG Growth Inhibition Assay IC50=2.62471 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=2.64318 μM SANGER
HT-144 Growth Inhibition Assay IC50=2.64577 μM SANGER
NB69 Growth Inhibition Assay IC50=2.65334 μM SANGER
A172 Growth Inhibition Assay IC50=2.67588 μM SANGER
RS4-11 Growth Inhibition Assay IC50=2.72407 μM SANGER
DU-4475 Growth Inhibition Assay IC50=2.79502 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=2.82556 μM SANGER
BV-173 Growth Inhibition Assay IC50=2.84439 μM SANGER
U-2-OS Growth Inhibition Assay IC50=2.9107 μM SANGER
CHP-134 Growth Inhibition Assay IC50=2.93882 μM SANGER
D-502MG Growth Inhibition Assay IC50=2.97154 μM SANGER
KS-1 Growth Inhibition Assay IC50=3.01623 μM SANGER
A204 Growth Inhibition Assay IC50=3.05588 μM SANGER
KGN Growth Inhibition Assay IC50=3.08496 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=3.12028 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=3.12694 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=3.17026 μM SANGER
NB10 Growth Inhibition Assay IC50=3.20966 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=3.26827 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=3.27843 μM SANGER
HCT-116 Growth Inhibition Assay IC50=3.30335 μM SANGER
G-401 Growth Inhibition Assay IC50=3.36322 μM SANGER
MN-60 Growth Inhibition Assay IC50=3.44092 μM SANGER
SW982 Growth Inhibition Assay IC50=3.50848 μM SANGER
RKO Growth Inhibition Assay IC50=3.53936 μM SANGER
D-283MED Growth Inhibition Assay IC50=3.57986 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=3.62558 μM SANGER
A549 Growth Inhibition Assay IC50=3.63552 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=3.65708 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=3.74297 μM SANGER
G-402 Growth Inhibition Assay IC50=3.80832 μM SANGER
GOTO Growth Inhibition Assay IC50=3.84333 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=3.85675 μM SANGER
NH-12 Growth Inhibition Assay IC50=4.01959 μM SANGER
CTV-1 Growth Inhibition Assay IC50=4.07973 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=4.24392 μM SANGER
RH-18 Growth Inhibition Assay IC50=4.27706 μM SANGER
NB17 Growth Inhibition Assay IC50=4.31768 μM SANGER
A375 Growth Inhibition Assay IC50=4.33524 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=4.41411 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=4.50155 μM SANGER
CAL-54 Growth Inhibition Assay IC50=4.53019 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=4.62717 μM SANGER
D-247MG Growth Inhibition Assay IC50=4.75072 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=4.91127 μM SANGER
MCF7 Growth Inhibition Assay IC50=5.44244 μM SANGER
697 Growth Inhibition Assay IC50=5.4455 μM SANGER
ONS-76 Growth Inhibition Assay IC50=5.57009 μM SANGER
C32 Growth Inhibition Assay IC50=5.60029 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=5.73887 μM SANGER
MEL-HO Growth Inhibition Assay IC50=5.85667 μM SANGER
LoVo Growth Inhibition Assay IC50=6.01624 μM SANGER
AGS Growth Inhibition Assay IC50=6.14828 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=6.22421 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=6.386 μM SANGER
RVH-421 Growth Inhibition Assay IC50=6.42428 μM SANGER
SW954 Growth Inhibition Assay IC50=6.55572 μM SANGER
NB5 Growth Inhibition Assay IC50=6.56183 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=6.58793 μM SANGER
AM-38 Growth Inhibition Assay IC50=6.75639 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=6.76494 μM SANGER
LS-513 Growth Inhibition Assay IC50=6.79026 μM SANGER
A427 Growth Inhibition Assay IC50=6.87829 μM SANGER
WM-115 Growth Inhibition Assay IC50=6.9323 μM SANGER
COLO-829 Growth Inhibition Assay IC50=7.24188 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=7.39228 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=7.44879 μM SANGER
HT-1080 Growth Inhibition Assay IC50=7.48254 μM SANGER
HCC2218 Growth Inhibition Assay IC50=7.6297 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=7.87069 μM SANGER
KM-H2 Growth Inhibition Assay IC50=7.88694 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=7.94414 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=8.21122 μM SANGER
MKN45 Growth Inhibition Assay IC50=8.26602 μM SANGER
D-392MG Growth Inhibition Assay IC50=8.52722 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=8.86695 μM SANGER
CAL-51 Growth Inhibition Assay IC50=9.10251 μM SANGER
COLO-678 Growth Inhibition Assay IC50=9.32811 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=9.55856 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=9.94476 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=10.3961 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=10.6508 μM SANGER
NB12 Growth Inhibition Assay IC50=11.503 μM SANGER
UACC-257 Growth Inhibition Assay IC50=11.8695 μM SANGER
LAN-6 Growth Inhibition Assay IC50=11.9928 μM SANGER
SW1573 Growth Inhibition Assay IC50=12.3086 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=12.4175 μM SANGER
SHP-77 Growth Inhibition Assay IC50=12.5574 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=12.6573 μM SANGER
22RV1 Growth Inhibition Assay IC50=12.8059 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=13.3973 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=13.4202 μM SANGER
IGR-1 Growth Inhibition Assay IC50=14.0347 μM SANGER
EW-3 Growth Inhibition Assay IC50=14.1639 μM SANGER
JEG-3 Growth Inhibition Assay IC50=14.4953 μM SANGER
ES3 Growth Inhibition Assay IC50=14.6562 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=14.7111 μM SANGER
P30-OHK Growth Inhibition Assay IC50=15.0496 μM SANGER
GP5d Growth Inhibition Assay IC50=15.1466 μM SANGER
HMV-II Growth Inhibition Assay IC50=15.3333 μM SANGER
COLO-679 Growth Inhibition Assay IC50=15.501 μM SANGER
JAR Growth Inhibition Assay IC50=15.7205 μM SANGER
NCI-H1666 Growth Inhibition Assay IC50=15.9399 μM SANGER
SW48 Growth Inhibition Assay IC50=15.9516 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=15.9989 μM SANGER
HT-1197 Growth Inhibition Assay IC50=16.0352 μM SANGER
HL-60 Growth Inhibition Assay IC50=16.0384 μM SANGER
BEN Growth Inhibition Assay IC50=16.5638 μM SANGER
HAL-01 Growth Inhibition Assay IC50=16.8909 μM SANGER
SW900 Growth Inhibition Assay IC50=16.9132 μM SANGER
SBC-1 Growth Inhibition Assay IC50=17.5429 μM SANGER
SH-4 Growth Inhibition Assay IC50=17.5841 μM SANGER
UACC-62 Growth Inhibition Assay IC50=17.7637 μM SANGER
BHT-101 Growth Inhibition Assay IC50=19.8705 μM SANGER
DB Growth Inhibition Assay IC50=21.5649 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=21.5872 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=22.7379 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=23.3524 μM SANGER
KG-1 Growth Inhibition Assay IC50=23.4946 μM SANGER
LXF-289 Growth Inhibition Assay IC50=23.714 μM SANGER
HCC1954 Growth Inhibition Assay IC50=24.8844 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=26.4981 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=26.6488 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=27.5684 μM SANGER
RMG-I Growth Inhibition Assay IC50=29.4139 μM SANGER
H9 Growth Inhibition Assay IC50=31.3008 μM SANGER
GR-ST Growth Inhibition Assay IC50=32.4453 μM SANGER
Mo-T Growth Inhibition Assay IC50=32.5046 μM SANGER
SW1088 Growth Inhibition Assay IC50=32.9801 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=33.0797 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=33.1661 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=34.6073 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=34.6776 μM SANGER
LU-99A Growth Inhibition Assay IC50=35.0007 μM SANGER
BE-13 Growth Inhibition Assay IC50=35.6545 μM SANGER
GAK Growth Inhibition Assay IC50=35.695 μM SANGER
NCI-H1573 Growth Inhibition Assay IC50=35.8818 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=36.1527 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=36.316 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=37.0691 μM SANGER
CAL-27 Growth Inhibition Assay IC50=37.7231 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=39.3181 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=39.598 μM SANGER
EFO-21 Growth Inhibition Assay IC50=40.5814 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=41.5084 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=43.8037 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=45.0233 μM SANGER
EW-16 Growth Inhibition Assay IC50=46.3137 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=46.7167 μM SANGER
COR-L105 Growth Inhibition Assay IC50=46.8857 μM SANGER
DEL Growth Inhibition Assay IC50=48.0429 μM SANGER
JVM-2 Growth Inhibition Assay IC50=48.0558 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=49.4538 μM SANGER
BL21 (DE3) Function assay Binding affinity to human recombinant Mdm2 T101W mutant expressed in Escherichia coli BL21 (DE3) cells by antagonist induced dissociation assay, Kd = 0.5 μM. 18680271
BL21 (DE3) Function assay Binding affinity to human recombinant Mdm2 K98W mutant expressed in Escherichia coli BL21 (DE3) cells by antagonist induced dissociation assay, Kd = 0.5 μM. 18680271
BL21 (DE3) Function assay Binding affinity to human recombinant Mdm2 F55W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration, Kd = 0.5 μM. 18680271
SJSA1 Antiproliferative assay 3 days Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum, IC50 = 0.7 μM. 22524527
HCT116 Function assay 24 hrs Induction of p53-Ser15 phosphorylation in human HCT116 cells after 24 hrs, IC50 = 1 μM. 19856920
BL21 (DE3) Function assay Binding affinity to human recombinant Mdm2 T101W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration, Kd = 1 μM. 18680271
BL21 (DE3) Function assay Binding affinity to human recombinant Mdm2 K98W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration, Kd = 1 μM. 18680271
SJSA1 Cytotoxicity assay Cytotoxicity against human SJSA1 cells, IC50 = 1 μM. 25396320
RKO Cytotoxicity assay Cytotoxicity against human RKO cells, IC50 = 1 μM. 25396320
HCT116 Cytotoxicity assay Cytotoxicity against human HCT116 cells, IC50 = 1 μM. 25396320
SJSA1 Growth inhibition assay Growth inhibition of human SJSA1 cells expressing MDM2 by SRB assay, GI50 = 1.3 μM. 21875801
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay, IC50 = 1.3 μM. 30221935
HCT116 Function assay 8 hrs Induction of p53 in human HCT116 cells coexpressing pp53TA-luc assessed as inhibition of cell proliferation after 8 hrs by firefly/renilla luciferase reporter assay, IC50 = 1.39 μM. 19856920
HGF Cytotoxicity assay 24 hrs Cytotoxicity against human HGF cells after 24 hrs by MTT assay, IC50 = 1.4 μM. 23802716
SJSA1 Antiproliferative assay 72 hrs Antiproliferative activity against human SJSA1 cells expressing wild type p53 incubated for 72 hrs by MTS assay, IC50 = 1.44 μM. 30221935
SJSA1 Cytotoxicity assay 5 days Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay, IC50 = 1.5 μM. 24900694
RKO Cytotoxicity assay 5 days Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay, IC50 = 1.5 μM. 24900694
HCT116 Cytotoxicity assay 5 days Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay, IC50 = 1.5 μM. 24900694
A2780 Growth inhibition assay Growth inhibition of human A2780 cells expressing MDM2 by SRB assay, GI50 = 1.6 μM. 21875801
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by CellTiterGlo luciferase-based assay, IC50 = 1.6 μM. 24139845
SJSA1 Antiproliferative assay Antiproliferative activity against human SJSA1 cells, IC50 = 1.9 μM. 24656661
SJSA1 Antiproliferative assay 72 hrs Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 72 hrs by CellTitre-Glo assay, IC50 = 1.9 μM. 26985323
HCT116 Growth inhibition assay Growth inhibition of human HCT116 cells expressing MDM2 by SRB assay, GI50 = 2.1 μM. 21875801
NGP Cytotoxicity assay 72 hrs Cytotoxicity against human NGP cells after 72 hrs by sulforhodamine B assay, GI50 = 2.1 μM. 21314128
LS Cytotoxicity assay 72 hrs Cytotoxicity against human LS cells after 72 hrs by sulforhodamine B assay, GI50 = 2.3 μM. 21314128
SJSA1 Cytotoxicity assay 72 hrs Cytotoxicity against human SJSA1 cells after 72 hrs by sulforhodamine B assay, GI50 = 2.6 μM. 21314128
MCF7 Cytotoxicity assay 24 hrs Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 2.9 μM. 23802716
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity in p53 (+/+) human HCT116 cells incubated for 72 hrs by MTS assay, IC50 = 4 μM. 28987608
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 4.62 μM. 23601819
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells expressing wild type p53 after 72 hrs by SRB assay, IC50 = 4.62 μM. 23611770
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 5.01 μM. 27101893
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 5.1 μM. 25479770
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 5.21 μM. 27101893
UKF-NB-3 Cytotoxicity assay 96 hrs Cytotoxicity against doxorubicin-resistant human UKF-NB-3 cells after 96 hrs by MTT assay, IC50 = 5.56 μM. 20947617
SJSA1 Function assay 7 hrs Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum, IC50 = 7.1 μM. 22524527
HCT116 Growth inhibition assay 48 hrs Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay, GI50 = 8 μM. 29089230
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay, IC50 = 8.5 μM. 30045621
HCT116 Antiproliferative assay 24 hrs Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis, GI50 = 9 μM. 29691156
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay, IC50 = 9.07 μM. 30045621
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay, IC50 = 9.58 μM. 30045621
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay, IC50 = 10.2 μM. 23802716
NCI-H1299 Antiproliferative assay 72 hrs Antiproliferative activity against p53 -/- human NCI-H1299 cells incubated for 72 hrs by MTS assay, IC50 = 10.4 μM. 30221935
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 11.6 μM. 25618595
Saos2 Antiproliferative assay 72 hrs Antiproliferative activity against human p53-deficient Saos2 cells after 72 hrs by MTT assay, IC50 = 12.1 μM. 22940704
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human p53 expressing HCT116 cells after 72 hrs by sulforhodamine B assay, GI50 = 13 μM. 21314128
U2OS Antiproliferative assay 72 hrs Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay, IC50 = 14.31 μM. 23046248
H1299 Cytotoxicity assay 72 hrs Cytotoxicity against human H1299 cells after 72 hrs by CellTiterGlo luciferase-based assay, IC50 = 14.7 μM. 24139845
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay, IC50 = 15 μM. 22940704
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay, IC50 = 15.12 μM. 23046248
U937 Cytotoxicity assay 24 hrs Cytotoxicity against human U937 cells after 24 hrs by MTT assay, IC50 = 15.6 μM. 23802716
Saos2 Cytotoxicity assay 72 hrs Cytotoxicity against human Saos2 cells after 72 hrs by sulforhodamine B assay, GI50 = 18 μM. 21314128
U2OS Antiproliferative assay 72 hrs Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay, IC50 = 19.6 μM. 22940704
NCI-H1299 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay, IC50 = 19.76 μM. 30045621
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human p53-null PC3 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 20.04 μM. 23601819
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human p53 deficient PC3 cells after 72 hrs by SRB assay, IC50 = 20.04 μM. 23611770
A2780/CP70 Growth inhibition assay Growth inhibition of human A2780/CP70 cells expressing isogenically paired p53 mutant by SRB assay, GI50 = 20.4 μM. 21875801
NCI-H1299 Antiproliferative assay 72 hrs Antiproliferative activity against human p53-deficient NCI-H1299 cells after 72 hrs by MTT assay, IC50 = 20.4 μM. 22940704
NCI-H1299 Antiproliferative assay 72 hrs Antiproliferative activity against p53 deficient human NCI-H1299 cells after 72 hrs by MTT assay, IC50 = 20.48 μM. 23046248
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human p53-null HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 21.5 μM. 27101893
SJSA1 Cytotoxicity assay 24 hrs Cytotoxicity in human SJSA1 cells over expressing human DM2 after 24 hrs by CellTiter-Glo assay, EC50 = 22.8 μM. 29150077
C643 Cytotoxicity assay 24 hrs Cytotoxicity against human C643 cells after 24 hrs by MTT assay, IC50 = 23 μM. 23802716
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 23.5 μM. 25618595
U2OS Antitumor assay 72 hrs Antitumor activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay, IC50 = 24.61 μM. 21996465
HCT116 Growth inhibition assay Growth inhibition of p53 deficient human HCT116 cells expressing MDM2 by SRB assay, GI50 = 25.6 μM. 21875801
HCT116 Growth inhibition assay 48 hrs Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay, GI50 = 27 μM. 29089230
Calu Cytotoxicity assay 24 hrs Cytotoxicity against human Calu cells after 24 hrs by MTT assay, IC50 = 27.2 μM. 23802716
HCT116 Antiproliferative assay 24 hrs Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis, GI50 = 29 μM. 29691156
MDA-MB-435S Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-435S cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 29.6 μM. 27101893
PC3 Cytotoxicity assay 24 hrs Cytotoxicity against human PC3 cells after 24 hrs by MTT assay, IC50 = 30.3 μM. 23802716
Saos2 Antiproliferative assay 72 hrs Antiproliferative activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay, IC50 = 31.62 μM. 23046248
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells expressing wild type p53 after 48 hrs by MTT assay, GI50 = 32.11 μM. 24852275
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by sulforhodamine B assay, GI50 = 34 μM. 21314128
HCT116 Antiproliferative assay 24 hrs Antiproliferative activity against human HCT116 cells expressing p53 after 24 hrs by MTS assay, GI50 = 39.65 μM. 24268795
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, GI50 = 47.59 μM. 24852275
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity in p53 (-/-) human HCT116 cells incubated for 72 hrs by MTS assay, IC50 = 47.8 μM. 28987608
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, GI50 = 48.74 μM. 24852275
SJSA1 Function assay 10 uM Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as p53 activation at 10 uM by Western blot 19928922
MCF7 Cell cycle assay 4 uM 14 days Induction of cell cycle arrest in human MCF7 cells transfected with p53-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay 16474381
MCF7 Cell cycle assay 4 uM 14 days Induction of cell cycle arrest in human MCF7 cells transfected hnRNPK-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay 16474381
MCF7 Antiproliferative assay 4 uM 14 days Antiproliferative activity against human MCF7 cells at 4 uM after 14 days by coomassie staining 16474381
MCF7 Antiproliferative assay 4 uM 14 days Antiproliferative activity against human MCF7 cells assessed as appearance of flattened phenotype at 4 uM after 14 days by coomassie staining 16474381
MCF7 Function assay Induction of p53 expression in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA by Western blot analysis 16474381
MCF7 Function assay Induction of p53 expression in human MCF7 cells by Western blot analysis 16474381
MCF7 Function assay 18 hrs Induction of p53 accumulation in human MCF7 cells after 18 hrs by Western blot analysis in presence of 2.5 mM caffeine 16474381
BJ Function assay 3 uM Induction of p21CIP1 expression in irradiated human BJ cells at 3 uM by Western blot analysis 16474381
MCF7 Cell cycle assay 4 uM 14 days Induction of cell cycle arrest in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay 16474381
BJ Function assay 3 uM Induction of p21 expression in irradiated human BJ cells at 3 uM by Western blot analysis 16474381
SNJSA1 Function assay 1 to 10 uM 6 hrs Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of p21 protein at 1 to 10 uM after 6 hrs by Western blot analysis 21314128
SNJSA1 Function assay 1 to 10 uM 6 hrs Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of p53 protein at 1 to 10 uM after 6 hrs by Western blot analysis 21314128
SNJSA1 Function assay 1 to 10 uM 6 hrs Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of MDM2 protein at 1 to 10 uM after 6 hrs by Western blot analysis 21314128
MCF7 Function assay 24 hrs Upregulation of p53 in human MCF7 cells after 24 hrs by Western blot analysis 27010502
MCF7 Function assay 24 hrs Upregulation of Mdm2 in human MCF7 cells after 24 hrs by Western blot analysis 27010502
MCF7 Function assay 24 hrs Increase in p53 expression in human MCF7 cells nuclei after 24 hrs by DAPI staining based immunofluorescence microscopy 27010502
MCF7 Function assay 24 hrs Upregulation of p21 in human MCF7 cells after 24 hrs by Western blot analysis 27010502
HCT116 Function assay 50 uM 24 hrs Inhibition of p53-MDM2 (unknown origin) interaction expressed in p53-deficient human HCT116 cells at 50 uM after 24 hrs by BiFC-based FACS flow cytometric analysis 24268795
U2OS Function assay 2.5 uM 12 hrs Stabilization of p53 in human U2OS cells assessed as intracellular p53 level at 2.5 uM after 12 hrs by Western blotting 26288684
HCT116 Function assay 10 uM 20 hrs Inhibition of V1-p53/MDM2-V2 (unknown origin) interaction expressed in human HCT116 p53-/- cells at 10 uM after 20 hrs by biomolecular fluorescence complementation-based flow cytometric analysis 28800455
IMR32 Function assay 24 hrs Increase in p53 expression in human IMR32 cells nuclei after 24 hrs by DAPI staining based immunofluorescence microscopy 27010502
MCF7 Function assay 10 uM 16 hrs Inhibition of MDM2-p53 interaction in human MCF7 cells assessed as reversal of MDM2-dependent inhibition of p53-induced transcriptional activity at 10 uM after 16 hrs by dual-luciferase reporter gene assay 23540934
MCF7 Apoptosis assay 3 uM 24 to 72 hrs Induction of apoptosis in human MCF7 cells assessed as reduction in Bcl-xL expression level at 3 uM after 24 to 72 hrs by Western blotting analysis 23802716
MCF7 Apoptosis assay 3 uM 24 to 72 hrs Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells at 3 uM after 24 to 72 hrs by annexin V-FITC/propidium iodide staining based FACS flow cytometry (Rvb = 4 %) 23802716
MCF7 Apoptosis assay 3 uM 24 to 72 hrs Induction of apoptosis in human MCF7 cells assessed as increase in p21 expression level at 3 uM after 24 to 72 hrs by Western blotting analysis 23802716
MCF7 Apoptosis assay 3 uM 24 to 72 hrs Induction of apoptosis in human MCF7 cells assessed as increase in Bcl-xS expression level at 3 uM after 24 to 72 hrs by Western blotting analysis 23802716
MCF7 Apoptosis assay 50 nM 24 to 72 hrs Induction of apoptosis in human MCF7 cells assessed as accumulation of caspase-3 cleavage product at 50 nM after 24 to 72 hrs by Western blotting analysis 23802716
MCF7 Cell cycle assay 3 uM 24 to 72 hrs Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 3 uM after 24 to 72 hrs by propidium iodide staining-based FACS analysis 23802716
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 581.49 Formula

C30H30Cl2N4O4

 Conservazione (Dalla data di ricezione)
N. CAS 675576-98-4 -- Conservazione delle soluzioni stock

Sinonimi (-)-Nutlin-3 Smiles CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 100 mg/mL (171.97 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 100 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa Concentrazione Volume Peso molecolare
Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo
Lotto:

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Caratteristiche
Highly selective MDM2 inhibitor with a much lower effect on MDMX. Most effective on tumors with wild type p53.
Targets/IC50/Ki
p53-MDM2 interaction
(Cell-free assay)
90 nM
In vitro
Nutlin-3a sposta p53 dalla tasca di legame di MDM2 e, di conseguenza, rilascia p53 dall'inibizione e dalla degradazione proteasomica, portando all'induzione dei suoi bersagli a valle, all'arresto del ciclo cellulare e all'apoptosis. Sette giorni di incubazione con 10 μM di questo composto hanno portato a >90% di inibizione della crescita delle cellule NIH3T3. Questo composto stabilizza e attiva p53 e induce l'espressione di p21 in modo dose-dipendente. Depleisce efficacemente il compartimento della fase S al 0,2-2% e aumenta i compartimenti delle fasi G1 e G2/M. Questa sostanza chimica induce l'apoptosis in circa il 60% delle cellule SJSA-1 e MHM dopo 40 h, percentuale che è ulteriormente aumentata dopo 60 h (85% e 65%, rispettivamente) .
Saggio chinasico
Studi Biacore
I saggi di competizione sono eseguiti su un Biacore S51. Un chip sensore Series S CM5 è derivatizzato per l'immobilizzazione di un anticorpo PentaHis per la cattura del p53 marcato con His. Il livello di cattura è di circa 200 unità di risposta (1 unità di risposta corrisponde a 1 pg di proteina per mm2). La concentrazione della proteina MDM2 è mantenuta costante a 300 nM. I composti di prova sono disciolti in DMSO a 10 mM e ulteriormente diluiti per creare una serie di concentrazioni di inibitore in ogni campione di prova MDM2. I saggi vengono eseguiti a 25 °C in tampone di corsa (10 mM Hepes, 0,15 M NaCl, 2% DMSO). Il legame MDM2-p53 in presenza di questo composto è calcolato come percentuale del legame in assenza di questo composto e l'IC50 è calcolato utilizzando Microsoft Excel.
In vivo
Nutlin-3a sopprime la crescita del trapianto in modo dose-dipendente, con la dose più alta (200 mg/kg) che mostra una sostanziale riduzione del tumore . Questo composto è un attivatore selettivo della via p53 in vivo e altamente efficace contro i tumori di osteosarcoma SJSA-1. I tumori con p53 wild-type e amplificazione del gene MDM2 risponderanno meglio alla terapia con questa sostanza chimica.
Riferimenti

Applicazioni (Applications)

Metodi Biomarcatori Immagini PMID
Western blot p53 / MDM2 / p21 / Bax / Bak / Noxa / cleaved caspase / pro-caspase BMI-1 p53-Ser15 / p53-Ser37 / p53-Lys382 / MDM2 / CDC2 / PLK1 / HSC70
S8059-WB1
16014563
Immunofluorescence p-p21 / β-actin P53 Ac-p300
S8059-IF1
31083332
Growth inhibition assay Cell viability
S8059-viability1
26248031

Domande Frequenti (Frequently Asked Questions)

Domanda 1:
What is the difference between S1061 (Nutlin-3) and it?

Risposta:
S1061 is a racemic mixture of Nutlin3a and Nutlin3b. Its active enantiomer is s8059.