Home PI3K/Akt/mTOR PI3K Inhibiteur Dactolisib (BEZ235)

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Dactolisib (BEZ235) PI3K Inhibiteur

Réf. Catalogue: S1009

Le Dactolisib (BEZ235, NVP-BEZ235) est un double inhibiteur compétitif de l'ATP des PI3K et mTOR pour p110α/γ/δ/β et mTOR(p70S6K) avec une IC50 de 4 nM /5 nM /7 nM /75 nM /6 nM dans les essais sans cellules, respectivement. Il inhibe l'ATR avec une IC50 de 21 nM dans les cellules 3T3TopBP1-ER, induit l'autophagie et supprime la réplication du VIH-1. Phase 2.
Dactolisib (BEZ235) PI3K Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 469.55

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Contrôle Qualité (Quality Control)

Lot : Pureté : 99.99%
99.99

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires Type d'essai Concentration Temps d'incubation Formulation Description de l'activité PMID
Trypanosoma brucei brucei Antimicrobial Assay 18 h DMSO Antitrypanosomal activity with EC50 of 0.0025 μM 24805946
MCF7 Growth Inhibition Assay 0.01-100 μM 48 h DMSO IC50=0.73 μM 23871904
HCT116 Growth Inhibition Assay 0.01-100 μM 48 h DMSO IC50=1.16 μM 23871904
U87MG Growth Inhibition Assay 0.01-100 μM 48 h DMSO IC50=1.32 μM 23871904
HBC4 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.61 M 22336246
BSY1 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.48 M 22336246
HBC5 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.87 M 22336246
MCF7 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.16 M 22336246
MDA-MB-231 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.09 M 22336246
U251 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.66 M 22336246
SF268 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.92 M 22336246
SF295 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.31 M 22336246
SF539 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.59 M 22336246
SNB75 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.58 M 22336246
SNB78 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.65 M 22336246
HCC2998 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.05 M 22336246
KM12 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.54 M 22336246
HT-29 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.75 M 22336246
HCT15 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.03 M 22336246
HCT116 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.61 M 22336246
NCI-H23 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.64 M 22336246
NCI-H226 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.44 M 22336246
NCI-H522 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.45 M 22336246
NCI-H438 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.11 M 22336246
A549 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.07 M 22336246
DMS273 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.80 M 22336246
DMS114 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.39 M 22336246
LOXIMVI Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.66 M 22336246
OVCAR3 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.17 M 22336246
OVCAR4 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.58 M 22336246
OVCAR5 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.57 M 22336246
OVCAR8 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.84 M 22336246
SKOV3 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.41 M 22336246
RXF631L Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.21 M 22336246
ACHN Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.95 M 22336246
St-4 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.47 M 22336246
MKN1 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.41 M 22336246
MKN7 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.68 M 22336246
MKN28 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.07 M 22336246
MKN45 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.34 M 22336246
MKN74 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.42 M 22336246
DU145 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.16 M 22336246
PC3 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.66 M 22336246
Trypanosoma brucei brucei Function Assay 200 nM 12 h DMSO Decrease in phosphotidyl inositol phosphate level 24805946
Trypanosoma brucei brucei Function Assay 18 h DMSO Inhibition of receptor-mediated endocytosis assessed as decrease in transferrin uptake 24805946
Trypanosoma brucei brucei Function Assay 200 nM 12 h DMSO Effect on sphingomylein level 24805946
Trypanosoma brucei brucei Function Assay 200 nM 12 h DMSO Effect on phosphatidylcholine level 24805946
UM-UC-3 Growth Inhibition Assay IC50=315 pM SANGER
SBC-1 Growth Inhibition Assay IC50=742 pM SANGER
MKN1 Growth Inhibition Assay IC50=2.8 nM SANGER
NCI-H720 Growth Inhibition Assay IC50=3.57 nM SANGER
BFTC-909 Growth Inhibition Assay IC50=3.71 nM SANGER
BPH-1 Growth Inhibition Assay IC50=4.76 nM SANGER
PC-3 Growth Inhibition Assay IC50=5.09 nM SANGER
AN3-CA Growth Inhibition Assay IC50=5.56 nM SANGER
HN Growth Inhibition Assay IC50=5.96 nM SANGER
HCC2218 Growth Inhibition Assay IC50=6.61 nM SANGER
KP-4 Growth Inhibition Assay IC50=7 nM SANGER
LU-139 Growth Inhibition Assay IC50=7.77 nM SANGER
ETK-1 Growth Inhibition Assay IC50=7.88 nM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=8.49 nM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=9.12 nM SANGER
DU-4475 Growth Inhibition Assay IC50=9.44 nM SANGER
NCI-H1666 Growth Inhibition Assay IC50=9.71 nM SANGER
CAMA-1 Growth Inhibition Assay IC50=9.8 nM SANGER
TYK-nu Growth Inhibition Assay IC50=9.94 nM SANGER
MFE-280 Growth Inhibition Assay IC50=9.99 nM SANGER
A549 Growth Inhibition Assay IC50=10.14 nM SANGER
769-P Growth Inhibition Assay IC50=10.44 nM SANGER
L-363 Growth Inhibition Assay IC50=10.69 nM SANGER
ES8 Growth Inhibition Assay IC50=10.9 nM SANGER
PA-1 Growth Inhibition Assay IC50=11.82 nM SANGER
Mewo Growth Inhibition Assay IC50=11.99 nM SANGER
HSC-3 Growth Inhibition Assay IC50=12.21 nM SANGER
H4 Growth Inhibition Assay IC50=12.67 nM SANGER
BB65-RCC Growth Inhibition Assay IC50=12.72 nM SANGER
NCI-H1793 Growth Inhibition Assay IC50=12.82 nM SANGER
KARPAS-45 Growth Inhibition Assay IC50=13.51 nM SANGER
GCT Growth Inhibition Assay IC50=13.68 nM SANGER
EoL-1 Growth Inhibition Assay IC50=13.93 nM SANGER
LB2241-RCC Growth Inhibition Assay IC50=14.01 nM SANGER
ES5 Growth Inhibition Assay IC50=14.74 nM SANGER
LOXIMVI Growth Inhibition Assay IC50=14.99 nM SANGER
COR-L105 Growth Inhibition Assay IC50=15.04 nM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=15.1 nM SANGER
CHL-1 Growth Inhibition Assay IC50=15.45 nM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=15.63 nM SANGER
HH Growth Inhibition Assay IC50=15.7 nM SANGER
NUGC-3 Growth Inhibition Assay IC50=16.34 nM SANGER
EGI-1 Growth Inhibition Assay IC50=16.43 nM SANGER
OS-RC-2 Growth Inhibition Assay IC50=16.47 nM SANGER
MOLT-16 Growth Inhibition Assay IC50=17.15 nM SANGER
NCI-H209 Growth Inhibition Assay IC50=17.29 nM SANGER
697 Growth Inhibition Assay IC50=17.43 nM SANGER
D-56MG Growth Inhibition Assay IC50=17.69 nM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=17.83 nM SANGER
EW-16 Growth Inhibition Assay IC50=18.04 nM SANGER
HGC-27 Growth Inhibition Assay IC50=18.06 nM SANGER
ES7 Growth Inhibition Assay IC50=18.09 nM SANGER
HuH-7 Growth Inhibition Assay IC50=18.4 nM SANGER
BCPAP Growth Inhibition Assay IC50=18.65 nM SANGER
SW1710 Growth Inhibition Assay IC50=18.72 nM SANGER
IST-MEL1 Growth Inhibition Assay IC50=18.77 nM SANGER
SF295 Growth Inhibition Assay IC50=18.93 nM SANGER
RPMI-7951 Growth Inhibition Assay IC50=19.28 nM SANGER
SF126 Growth Inhibition Assay IC50=19.41 nM SANGER
GAMG Growth Inhibition Assay IC50=19.48 nM SANGER
KNS-81-FD Growth Inhibition Assay IC50=19.54 nM SANGER
RT-112 Growth Inhibition Assay IC50=19.66 nM SANGER
DEL Growth Inhibition Assay IC50=20.49 nM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=20.63 nM SANGER
HOS Growth Inhibition Assay IC50=21.06 nM SANGER
ES4 Growth Inhibition Assay IC50=21.08 nM SANGER
RXF393 Growth Inhibition Assay IC50=21.45 nM SANGER
NCI-H2030 Growth Inhibition Assay IC50=21.52 nM SANGER
YH-13 Growth Inhibition Assay IC50=21.88 nM SANGER
HT-1080 Growth Inhibition Assay IC50=21.93 nM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=21.95 nM SANGER
G-402 Growth Inhibition Assay IC50=22.16 nM SANGER
786-0 Growth Inhibition Assay IC50=22.29 nM SANGER
ME-180 Growth Inhibition Assay IC50=22.43 nM SANGER
NB69 Growth Inhibition Assay IC50=22.53 nM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=22.96 nM SANGER
TGBC1TKB Growth Inhibition Assay IC50=23.05 nM SANGER
SW780 Growth Inhibition Assay IC50=23.13 nM SANGER
MG-63 Growth Inhibition Assay IC50=23.45 nM SANGER
BV-173 Growth Inhibition Assay IC50=23.87 nM SANGER
CAL-51 Growth Inhibition Assay IC50=23.89 nM SANGER
A375 Growth Inhibition Assay IC50=23.93 nM SANGER
MEL-HO Growth Inhibition Assay IC50=24.04 nM SANGER
EFO-27 Growth Inhibition Assay IC50=24.33 nM SANGER
Hs-578-T Growth Inhibition Assay IC50=24.58 nM SANGER
NBsusSR Growth Inhibition Assay IC50=24.6 nM SANGER
CTB-1 Growth Inhibition Assay IC50=24.67 nM SANGER
FTC-133 Growth Inhibition Assay IC50=25.1 nM SANGER
MOLT-4 Growth Inhibition Assay IC50=25.12 nM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=25.15 nM SANGER
ES3 Growth Inhibition Assay IC50=25.22 nM SANGER
TI-73 Growth Inhibition Assay IC50=25.28 nM SANGER
MPP-89 Growth Inhibition Assay IC50=25.32 nM SANGER
KYSE-150 Growth Inhibition Assay IC50=25.89 nM SANGER
LXF-289 Growth Inhibition Assay IC50=26.04 nM SANGER
SK-LU-1 Growth Inhibition Assay IC50=26.17 nM SANGER
HOP-92 Growth Inhibition Assay IC50=26.48 nM SANGER
HuO9 Growth Inhibition Assay IC50=26.76 nM SANGER
SW962 Growth Inhibition Assay IC50=26.76 nM SANGER
RS4-11 Growth Inhibition Assay IC50=26.91 nM SANGER
NCI-H292 Growth Inhibition Assay IC50=27 nM SANGER
DB Growth Inhibition Assay IC50=27.36 nM SANGER
SW1088 Growth Inhibition Assay IC50=28.29 nM SANGER
A204 Growth Inhibition Assay IC50=28.47 nM SANGER
A3-KAW Growth Inhibition Assay IC50=28.64 nM SANGER
MV-4-11 Growth Inhibition Assay IC50=28.7 nM SANGER
ES1 Growth Inhibition Assay IC50=28.84 nM SANGER
ONS-76 Growth Inhibition Assay IC50=29.05 nM SANGER
D-263MG Growth Inhibition Assay IC50=29.35 nM SANGER
U-2-OS Growth Inhibition Assay IC50=29.5 nM SANGER
T98G Growth Inhibition Assay IC50=29.88 nM SANGER
GI-ME-N Growth Inhibition Assay IC50=29.91 nM SANGER
BHT-101 Growth Inhibition Assay IC50=30.05 nM SANGER
NOS-1 Growth Inhibition Assay IC50=30.12 nM SANGER
AsPC-1 Growth Inhibition Assay IC50=30.2 nM SANGER
QIMR-WIL Growth Inhibition Assay IC50=30.6 nM SANGER
JVM-3 Growth Inhibition Assay IC50=30.83 nM SANGER
KU-19-19 Growth Inhibition Assay IC50=31.13 nM SANGER
OVCAR-8 Growth Inhibition Assay IC50=31.26 nM SANGER
BEN Growth Inhibition Assay IC50=31.63 nM SANGER
BE-13 Growth Inhibition Assay IC50=31.82 nM SANGER
EW-18 Growth Inhibition Assay IC50=31.86 nM SANGER
ECC10 Growth Inhibition Assay IC50=31.95 nM SANGER
CTV-1 Growth Inhibition Assay IC50=32.82 nM SANGER
COLO-800 Growth Inhibition Assay IC50=32.92 nM SANGER
A2058 Growth Inhibition Assay IC50=33.25 nM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=33.43 nM SANGER
Ca9-22 Growth Inhibition Assay IC50=33.55 nM SANGER
COLO-684 Growth Inhibition Assay IC50=33.58 nM SANGER
RPMI-8226 Growth Inhibition Assay IC50=33.82 nM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=34.15 nM SANGER
Becker Growth Inhibition Assay IC50=34.21 nM SANGER
NCI-H28 Growth Inhibition Assay IC50=34.44 nM SANGER
CAL-120 Growth Inhibition Assay IC50=34.72 nM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=35.41 nM SANGER
OVCAR-5 Growth Inhibition Assay IC50=35.47 nM SANGER
LAMA-84 Growth Inhibition Assay IC50=35.87 nM SANGER
CAKI-1 Growth Inhibition Assay IC50=36.43 nM SANGER
Daoy Growth Inhibition Assay IC50=36.7 nM SANGER
CAL-62 Growth Inhibition Assay IC50=36.86 nM SANGER
8-MG-BA Growth Inhibition Assay IC50=37.25 nM SANGER
8505C Growth Inhibition Assay IC50=37.51 nM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=37.59 nM SANGER
CAL-39 Growth Inhibition Assay IC50=37.9 nM SANGER
MN-60 Growth Inhibition Assay IC50=37.96 nM SANGER
RKO Growth Inhibition Assay IC50=38.33 nM SANGER
U251 Growth Inhibition Assay IC50=38.43 nM SANGER
SJSA-1 Growth Inhibition Assay IC50=38.54 nM SANGER
CAL-12T Growth Inhibition Assay IC50=38.6 nM SANGER
HCC1419 Growth Inhibition Assay IC50=38.71 nM SANGER
CO-314 Growth Inhibition Assay IC50=38.74 nM SANGER
LB1047-RCC Growth Inhibition Assay IC50=38.81 nM SANGER
A101D Growth Inhibition Assay IC50=38.97 nM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=39.51 nM SANGER
MZ2-MEL Growth Inhibition Assay IC50=39.66 nM SANGER
NB5 Growth Inhibition Assay IC50=40.64 nM SANGER
G-401 Growth Inhibition Assay IC50=40.82 nM SANGER
HT Growth Inhibition Assay IC50=41.02 nM SANGER
8305C Growth Inhibition Assay IC50=41.87 nM SANGER
BHY Growth Inhibition Assay IC50=42.72 nM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=43 nM SANGER
T-24 Growth Inhibition Assay IC50=43.83 nM SANGER
EPLC-272H Growth Inhibition Assay IC50=44.39 nM SANGER
PSN1 Growth Inhibition Assay IC50=44.4 nM SANGER
NCI-H2452 Growth Inhibition Assay IC50=44.58 nM SANGER
KS-1 Growth Inhibition Assay IC50=44.66 nM SANGER
HD-MY-Z Growth Inhibition Assay IC50=44.92 nM SANGER
KNS-62 Growth Inhibition Assay IC50=45.38 nM SANGER
NOMO-1 Growth Inhibition Assay IC50=45.87 nM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=46.04 nM SANGER
IGR-1 Growth Inhibition Assay IC50=46.13 nM SANGER
KYSE-180 Growth Inhibition Assay IC50=46.17 nM SANGER
EW-22 Growth Inhibition Assay IC50=46.2 nM SANGER
NCI-H1355 Growth Inhibition Assay IC50=46.34 nM SANGER
DOHH-2 Growth Inhibition Assay IC50=46.37 nM SANGER
A4-Fuk Growth Inhibition Assay IC50=46.52 nM SANGER
PC-14 Growth Inhibition Assay IC50=46.57 nM SANGER
TE-5 Growth Inhibition Assay IC50=46.84 nM SANGER
LB996-RCC Growth Inhibition Assay IC50=47.19 nM SANGER
NCI-H1623 Growth Inhibition Assay IC50=47.76 nM SANGER
NCI-H1155 Growth Inhibition Assay IC50=48.32 nM SANGER
LoVo Growth Inhibition Assay IC50=48.4 nM SANGER
MCF7 Growth Inhibition Assay IC50=48.58 nM SANGER
AGS Growth Inhibition Assay IC50=48.77 nM SANGER
PFSK-1 Growth Inhibition Assay IC50=49.06 nM SANGER
22RV1 Growth Inhibition Assay IC50=49.09 nM SANGER
COR-L23 Growth Inhibition Assay IC50=49.16 nM SANGER
D-283MED Growth Inhibition Assay IC50=49.61 nM SANGER
SW982 Growth Inhibition Assay IC50=49.91 nM SANGER
SW620 Growth Inhibition Assay IC50=50.36 nM SANGER
KYSE-140 Growth Inhibition Assay IC50=50.55 nM SANGER
GCIY Growth Inhibition Assay IC50=50.67 nM SANGER
MHH-ESS-1 Growth Inhibition Assay IC50=51.95 nM SANGER
D-423MG Growth Inhibition Assay IC50=52.08 nM SANGER
SF539 Growth Inhibition Assay IC50=52.35 nM SANGER
RPMI-2650 Growth Inhibition Assay IC50=52.69 nM SANGER
GR-ST Growth Inhibition Assay IC50=52.87 nM SANGER
YKG-1 Growth Inhibition Assay IC50=53 nM SANGER
SK-MES-1 Growth Inhibition Assay IC50=53.26 nM SANGER
HLE Growth Inhibition Assay IC50=53.47 nM SANGER
RVH-421 Growth Inhibition Assay IC50=53.67 nM SANGER
C32 Growth Inhibition Assay IC50=53.83 nM SANGER
GB-1 Growth Inhibition Assay IC50=54.2 nM SANGER
SNB75 Growth Inhibition Assay IC50=54.26 nM SANGER
EM-2 Growth Inhibition Assay IC50=54.4 nM SANGER
RH-1 Growth Inhibition Assay IC50=54.7 nM SANGER
NKM-1 Growth Inhibition Assay IC50=54.81 nM SANGER
NCI-H2405 Growth Inhibition Assay IC50=54.88 nM SANGER
KYSE-450 Growth Inhibition Assay IC50=55.16 nM SANGER
A704 Growth Inhibition Assay IC50=55.59 nM SANGER
HAL-01 Growth Inhibition Assay IC50=55.83 nM SANGER
TE-11 Growth Inhibition Assay IC50=55.99 nM SANGER
DOK Growth Inhibition Assay IC50=56.02 nM SANGER
KY821 Growth Inhibition Assay IC50=56.2 nM SANGER
KGN Growth Inhibition Assay IC50=56.32 nM SANGER
MC116 Growth Inhibition Assay IC50=57.8 nM SANGER
PANC-08-13 Growth Inhibition Assay IC50=58.01 nM SANGER
KE-37 Growth Inhibition Assay IC50=58.77 nM SANGER
KYSE-410 Growth Inhibition Assay IC50=59.47 nM SANGER
RO82-W-1 Growth Inhibition Assay IC50=59.9 nM SANGER
M14 Growth Inhibition Assay IC50=60.04 nM SANGER
GI-1 Growth Inhibition Assay IC50=60.3 nM SANGER
ML-2 Growth Inhibition Assay IC50=60.62 nM SANGER
BFTC-905 Growth Inhibition Assay IC50=60.65 nM SANGER
DMS-273 Growth Inhibition Assay IC50=60.87 nM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=61 nM SANGER
MSTO-211H Growth Inhibition Assay IC50=63.51 nM SANGER
MEG-01 Growth Inhibition Assay IC50=63.52 nM SANGER
M059J Growth Inhibition Assay IC50=63.58 nM SANGER
LN-405 Growth Inhibition Assay IC50=63.85 nM SANGER
NCI-H1581 Growth Inhibition Assay IC50=64.03 nM SANGER
TCCSUP Growth Inhibition Assay IC50=64.53 nM SANGER
SW872 Growth Inhibition Assay IC50=64.57 nM SANGER
KYSE-510 Growth Inhibition Assay IC50=65.75 nM SANGER
NCI-H1792 Growth Inhibition Assay IC50=66.15 nM SANGER
SW13 Growth Inhibition Assay IC50=66.5 nM SANGER
TE-8 Growth Inhibition Assay IC50=66.52 nM SANGER
SCH Growth Inhibition Assay IC50=67.1 nM SANGER
NEC8 Growth Inhibition Assay IC50=67.24 nM SANGER
HuO-3N1 Growth Inhibition Assay IC50=67.31 nM SANGER
EFM-19 Growth Inhibition Assay IC50=67.5 nM SANGER
HEC-1 Growth Inhibition Assay IC50=67.52 nM SANGER
T47D Growth Inhibition Assay IC50=67.87 nM SANGER
SNU-423 Growth Inhibition Assay IC50=67.98 nM SANGER
WM-115 Growth Inhibition Assay IC50=68.14 nM SANGER
CaR-1 Growth Inhibition Assay IC50=68.25 nM SANGER
KU812 Growth Inhibition Assay IC50=68.69 nM SANGER
AM-38 Growth Inhibition Assay IC50=69.31 nM SANGER
KOSC-2 Growth Inhibition Assay IC50=69.97 nM SANGER
MC-IXC Growth Inhibition Assay IC50=70.08 nM SANGER
SCC-4 Growth Inhibition Assay IC50=71.38 nM SANGER
Calu-3 Growth Inhibition Assay IC50=71.98 nM SANGER
RPMI-8866 Growth Inhibition Assay IC50=72.82 nM SANGER
OVCAR-4 Growth Inhibition Assay IC50=73.36 nM SANGER
OAW-42 Growth Inhibition Assay IC50=73.39 nM SANGER
ATN-1 Growth Inhibition Assay IC50=73.87 nM SANGER
CHP-212 Growth Inhibition Assay IC50=74.95 nM SANGER
C2BBe1 Growth Inhibition Assay IC50=75.03 nM SANGER
A498 Growth Inhibition Assay IC50=75.15 nM SANGER
SH-4 Growth Inhibition Assay IC50=75.21 nM SANGER
SNU-449 Growth Inhibition Assay IC50=75.79 nM SANGER
RD Growth Inhibition Assay IC50=75.86 nM SANGER
PANC-03-27 Growth Inhibition Assay IC50=76.25 nM SANGER
S-117 Growth Inhibition Assay IC50=76.27 nM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=76.75 nM SANGER
LK-2 Growth Inhibition Assay IC50=77.05 nM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=77.4 nM SANGER
647-V Growth Inhibition Assay IC50=78.07 nM SANGER
LU-134-A Growth Inhibition Assay IC50=79.03 nM SANGER
5637 Growth Inhibition Assay IC50=79.23 nM SANGER
NCI-H1437 Growth Inhibition Assay IC50=80.5 nM SANGER
NCI-H460 Growth Inhibition Assay IC50=81.23 nM SANGER
BxPC-3 Growth Inhibition Assay IC50=81.46 nM SANGER
CAN Growth Inhibition Assay IC50=81.84 nM SANGER
KINGS-1 Growth Inhibition Assay IC50=82.32 nM SANGER
OCUB-M Growth Inhibition Assay IC50=82.41 nM SANGER
KALS-1 Growth Inhibition Assay IC50=82.54 nM SANGER
OCI-AML2 Growth Inhibition Assay IC50=82.61 nM SANGER
A253 Growth Inhibition Assay IC50=82.65 nM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=82.86 nM SANGER
NCI-H520 Growth Inhibition Assay IC50=83.06 nM SANGER
P30-OHK Growth Inhibition Assay IC50=83.5 nM SANGER
SBC-5 Growth Inhibition Assay IC50=83.52 nM SANGER
HCE-T Growth Inhibition Assay IC50=83.74 nM SANGER
JEG-3 Growth Inhibition Assay IC50=84.1 nM SANGER
KG-1 Growth Inhibition Assay IC50=84.24 nM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=84.54 nM SANGER
CAL-33 Growth Inhibition Assay IC50=85.08 nM SANGER
639-V Growth Inhibition Assay IC50=85.42 nM SANGER
NCI-H1048 Growth Inhibition Assay IC50=86.31 nM SANGER
NCI-H1573 Growth Inhibition Assay IC50=87.48 nM SANGER
NCI-H2228 Growth Inhibition Assay IC50=88.26 nM SANGER
NB14 Growth Inhibition Assay IC50=88.3 nM SANGER
SCC-25 Growth Inhibition Assay IC50=89.82 nM SANGER
A431 Growth Inhibition Assay IC50=89.97 nM SANGER
SN12C Growth Inhibition Assay IC50=90.62 nM SANGER
HuCCT1 Growth Inhibition Assay IC50=90.76 nM SANGER
LS-123 Growth Inhibition Assay IC50=92.18 nM SANGER
CAL-85-1 Growth Inhibition Assay IC50=92.48 nM SANGER
ES6 Growth Inhibition Assay IC50=92.83 nM SANGER
NCI-H650 Growth Inhibition Assay IC50=94.09 nM SANGER
NCI-H446 Growth Inhibition Assay IC50=95.12 nM SANGER
EW-13 Growth Inhibition Assay IC50=95.75 nM SANGER
HSC-2 Growth Inhibition Assay IC50=95.89 nM SANGER
U031 Growth Inhibition Assay IC50=96.73 nM SANGER
EW-11 Growth Inhibition Assay IC50=96.88 nM SANGER
GAK Growth Inhibition Assay IC50=98.93 nM SANGER
SK-OV-3 Growth Inhibition Assay IC50=100.07 nM SANGER
OMC-1 Growth Inhibition Assay IC50=100.18 nM SANGER
TK10 Growth Inhibition Assay IC50=100.21 nM SANGER
EKVX Growth Inhibition Assay IC50=100.6 nM SANGER
Detroit562 Growth Inhibition Assay IC50=102.17 nM SANGER
SF268 Growth Inhibition Assay IC50=102.34 nM SANGER
SNU-387 Growth Inhibition Assay IC50=104.17 nM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=105.06 nM SANGER
NCI-H1563 Growth Inhibition Assay IC50=105.18 nM SANGER
D-502MG Growth Inhibition Assay IC50=105.7 nM SANGER
A2780 Growth Inhibition Assay IC50=106.47 nM SANGER
IA-LM Growth Inhibition Assay IC50=107.51 nM SANGER
D-392MG Growth Inhibition Assay IC50=107.54 nM SANGER
MS-1 Growth Inhibition Assay IC50=107.71 nM SANGER
SW1990 Growth Inhibition Assay IC50=108.54 nM SANGER
HEL Growth Inhibition Assay IC50=109.29 nM SANGER
SW1573 Growth Inhibition Assay IC50=109.31 nM SANGER
SW1783 Growth Inhibition Assay IC50=110.22 nM SANGER
COLO-680N Growth Inhibition Assay IC50=110.76 nM SANGER
NCI-N87 Growth Inhibition Assay IC50=111.04 nM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=111.55 nM SANGER
BT-20 Growth Inhibition Assay IC50=112.01 nM SANGER
NCI-H1648 Growth Inhibition Assay IC50=113 nM SANGER
no-11 Growth Inhibition Assay IC50=113.28 nM SANGER
MOLT-13 Growth Inhibition Assay IC50=113.44 nM SANGER
NCI-H2170 Growth Inhibition Assay IC50=114.51 nM SANGER
HTC-C3 Growth Inhibition Assay IC50=116.85 nM SANGER
LU-99A Growth Inhibition Assay IC50=117.21 nM SANGER
HCC2998 Growth Inhibition Assay IC50=117.92 nM SANGER
NB13 Growth Inhibition Assay IC50=117.99 nM SANGER
GT3TKB Growth Inhibition Assay IC50=118.08 nM SANGER
BT-549 Growth Inhibition Assay IC50=118.95 nM SANGER
NCI-H747 Growth Inhibition Assay IC50=119.34 nM SANGER
EW-1 Growth Inhibition Assay IC50=120.2 nM SANGER
LB831-BLC Growth Inhibition Assay IC50=120.63 nM SANGER
NMC-G1 Growth Inhibition Assay IC50=121.11 nM SANGER
COLO-679 Growth Inhibition Assay IC50=122.15 nM SANGER
HL-60 Growth Inhibition Assay IC50=123.1 nM SANGER
MKN7 Growth Inhibition Assay IC50=123.83 nM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=124.31 nM SANGER
DMS-114 Growth Inhibition Assay IC50=125.09 nM SANGER
HuP-T4 Growth Inhibition Assay IC50=126.97 nM SANGER
HCC2157 Growth Inhibition Assay IC50=127.5 nM SANGER
SKG-IIIa Growth Inhibition Assay IC50=128.8 nM SANGER
HCT-116 Growth Inhibition Assay IC50=130.64 nM SANGER
BB30-HNC Growth Inhibition Assay IC50=130.78 nM SANGER
KYSE-270 Growth Inhibition Assay IC50=130.88 nM SANGER
MFM-223 Growth Inhibition Assay IC50=131.51 nM SANGER
NH-12 Growth Inhibition Assay IC50=132.99 nM SANGER
U-118-MG Growth Inhibition Assay IC50=133.62 nM SANGER
ESS-1 Growth Inhibition Assay IC50=135.18 nM SANGER
D-247MG Growth Inhibition Assay IC50=135.21 nM SANGER
IGROV-1 Growth Inhibition Assay IC50=135.76 nM SANGER
C-33-A Growth Inhibition Assay IC50=135.97 nM SANGER
NCI-H1693 Growth Inhibition Assay IC50=136.12 nM SANGER
MLMA Growth Inhibition Assay IC50=136.58 nM SANGER
SK-N-AS Growth Inhibition Assay IC50=137.17 nM SANGER
NCI-H1755 Growth Inhibition Assay IC50=138.85 nM SANGER
CHP-134 Growth Inhibition Assay IC50=139.55 nM SANGER
LS-513 Growth Inhibition Assay IC50=140.91 pM SANGER
TE-12 Growth Inhibition Assay IC50=140.93 nM SANGER
KNS-42 Growth Inhibition Assay IC50=144.3 nM SANGER
SJRH30 Growth Inhibition Assay IC50=144.44 nM SANGER
NCI-H1092 Growth Inhibition Assay IC50=144.52 nM SANGER
H-EMC-SS Growth Inhibition Assay IC50=146.81 nM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=147.55 nM SANGER
SK-N-FI Growth Inhibition Assay IC50=147.59 nM SANGER
NCI-H2126 Growth Inhibition Assay IC50=148.15 nM SANGER
NCI-H1299 Growth Inhibition Assay IC50=150.22 nM SANGER
CFPAC-1 Growth Inhibition Assay IC50=150.66 nM SANGER
NCI-H661 Growth Inhibition Assay IC50=151.26 nM SANGER
KYSE-70 Growth Inhibition Assay IC50=151.79 nM SANGER
SW900 Growth Inhibition Assay IC50=154.65 nM SANGER
Ca-Ski Growth Inhibition Assay IC50=156.39 nM SANGER
HPAF-II Growth Inhibition Assay IC50=156.47 nM SANGER
LB2518-MEL Growth Inhibition Assay IC50=157.1 nM SANGER
LC-2-ad Growth Inhibition Assay IC50=158.62 nM SANGER
HCC1806 Growth Inhibition Assay IC50=167.88 nM SANGER
UACC-62 Growth Inhibition Assay IC50=168.09 nM SANGER
KM-H2 Growth Inhibition Assay IC50=170.58 nM SANGER
NCI-H2347 Growth Inhibition Assay IC50=172.72 nM SANGER
SCC-15 Growth Inhibition Assay IC50=173.66 nM SANGER
BB49-HNC Growth Inhibition Assay IC50=173.81 nM SANGER
GMS-10 Growth Inhibition Assay IC50=173.94 nM SANGER
NCI-H2052 Growth Inhibition Assay IC50=174.9 nM SANGER
SW626 Growth Inhibition Assay IC50=176.06 nM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=176.61 nM SANGER
Saos-2 Growth Inhibition Assay IC50=179.35 nM SANGER
DK-MG Growth Inhibition Assay IC50=180.3 nM SANGER
SNU-C2B Growth Inhibition Assay IC50=180.73 nM SANGER
A427 Growth Inhibition Assay IC50=182.57 nM SANGER
KP-N-YS Growth Inhibition Assay IC50=185 nM SANGER
J82 Growth Inhibition Assay IC50=185.18 nM SANGER
LS-411N Growth Inhibition Assay IC50=187.28 nM SANGER
HCC1937 Growth Inhibition Assay IC50=187.49 nM SANGER
OE33 Growth Inhibition Assay IC50=188.97 nM SANGER
NB7 Growth Inhibition Assay IC50=189.89 nM SANGER
SW684 Growth Inhibition Assay IC50=196.13 nM SANGER
HT-144 Growth Inhibition Assay IC50=196.15 nM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=196.2 nM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=198.47 nM SANGER
NCI-H1395 Growth Inhibition Assay IC50=198.85 nM SANGER
NCI-H2122 Growth Inhibition Assay IC50=200.59 nM SANGER
no-10 Growth Inhibition Assay IC50=201.04 nM SANGER
SW48 Growth Inhibition Assay IC50=201.31 nM SANGER
NCI-H1650 Growth Inhibition Assay IC50=204.01 nM SANGER
MZ1-PC Growth Inhibition Assay IC50=205.58 nM SANGER
U-266 Growth Inhibition Assay IC50=205.79 nM SANGER
CAS-1 Growth Inhibition Assay IC50=207.44 nM SANGER
AU565 Growth Inhibition Assay IC50=212.82 nM SANGER
UACC-257 Growth Inhibition Assay IC50=213.99 nM SANGER
CAL-27 Growth Inhibition Assay IC50=217.05 nM SANGER
NCI-H23 Growth Inhibition Assay IC50=219.33 nM SANGER
TE-6 Growth Inhibition Assay IC50=219.68 nM SANGER
TGBC24TKB Growth Inhibition Assay IC50=222.17 nM SANGER
TE-1 Growth Inhibition Assay IC50=222.88 nM SANGER
RCC10RGB Growth Inhibition Assay IC50=224.19 nM SANGER
NCI-H596 Growth Inhibition Assay IC50=228.22 nM SANGER
SW954 Growth Inhibition Assay IC50=233.83 nM SANGER
NCI-H2087 Growth Inhibition Assay IC50=234.51 nM SANGER
SK-PN-DW Growth Inhibition Assay IC50=235.19 nM SANGER
KM12 Growth Inhibition Assay IC50=235.7 nM SANGER
BT-474 Growth Inhibition Assay IC50=235.73 nM SANGER
IST-MES1 Growth Inhibition Assay IC50=236.57 nM SANGER
HT-1197 Growth Inhibition Assay IC50=238.09 nM SANGER
CAL-54 Growth Inhibition Assay IC50=238.49 nM SANGER
NB10 Growth Inhibition Assay IC50=240.06 nM SANGER
PANC-10-05 Growth Inhibition Assay IC50=245.56 nM SANGER
NCI-H522 Growth Inhibition Assay IC50=248.31 nM SANGER
A388 Growth Inhibition Assay IC50=249.82 nM SANGER
GOTO Growth Inhibition Assay IC50=250.29 nM SANGER
KLE Growth Inhibition Assay IC50=251.87 nM SANGER
KYSE-520 Growth Inhibition Assay IC50=252.86 nM SANGER
HCE-4 Growth Inhibition Assay IC50=262.5 nM SANGER
KURAMOCHI Growth Inhibition Assay IC50=265.9 nM SANGER
HCC38 Growth Inhibition Assay IC50=266.48 nM SANGER
FADU Growth Inhibition Assay IC50=266.63 nM SANGER
CW-2 Growth Inhibition Assay IC50=269.96 nM SANGER
L-428 Growth Inhibition Assay IC50=275.15 nM SANGER
HCC1569 Growth Inhibition Assay IC50=275.84 nM SANGER
NCI-H810 Growth Inhibition Assay IC50=278.31 nM SANGER
LB771-HNC Growth Inhibition Assay IC50=285.84 nM SANGER
LCLC-103H Growth Inhibition Assay IC50=285.99 nM SANGER
EFO-21 Growth Inhibition Assay IC50=287.68 nM SANGER
CAL-72 Growth Inhibition Assay IC50=293.19 nM SANGER
SCC-9 Growth Inhibition Assay IC50=293.22 nM SANGER
COLO-829 Growth Inhibition Assay IC50=296.5 nM SANGER
U-87-MG Growth Inhibition Assay IC50=300.73 nM SANGER
MZ7-mel Growth Inhibition Assay IC50=323.76 nM SANGER
NCI-H1770 Growth Inhibition Assay IC50=326.74 nM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=328.1 nM SANGER
SiHa Growth Inhibition Assay IC50=329.24 nM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=336.77 nM SANGER
DJM-1 Growth Inhibition Assay IC50=340.33 nM SANGER
OE19 Growth Inhibition Assay IC50=340.53 nM SANGER
NCI-H1651 Growth Inhibition Assay IC50=344.18 nM SANGER
COLO-792 Growth Inhibition Assay IC50=354.42 nM SANGER
ACHN Growth Inhibition Assay IC50=356.71 nM SANGER
TH-3 Growth Inhibition Assay IC50=379.95 nM SANGER
HT-1376 Growth Inhibition Assay IC50=384.88 nM SANGER
RH-18 Growth Inhibition Assay IC50=394.74 nM SANGER
NB6 Growth Inhibition Assay IC50=396.66 nM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=403.37 nM SANGER
UACC-893 Growth Inhibition Assay IC50=406.47 nM SANGER
DSH1 Growth Inhibition Assay IC50=406.91 nM SANGER
TE-10 Growth Inhibition Assay IC50=407.01 nM SANGER
HCC70 Growth Inhibition Assay IC50=409.21 nM SANGER
TGBC11TKB Growth Inhibition Assay IC50=410.33 nM SANGER
NCI-H727 Growth Inhibition Assay IC50=412.11 nM SANGER
ALL-PO Growth Inhibition Assay IC50=415.69 nM SANGER
ABC-1 Growth Inhibition Assay IC50=420.45 nM SANGER
NCI-H69 Growth Inhibition Assay IC50=426.76 nM SANGER
GP5d Growth Inhibition Assay IC50=434.41 nM SANGER
UMC-11 Growth Inhibition Assay IC50=458.36 nM SANGER
RMG-I Growth Inhibition Assay IC50=467.56 nM SANGER
YAPC Growth Inhibition Assay IC50=490.6 nM SANGER
LS-1034 Growth Inhibition Assay IC50=491.06 nM SANGER
RCM-1 Growth Inhibition Assay IC50=496.68 nM SANGER
HCC1954 Growth Inhibition Assay IC50=512.5 nM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=516.51 nM SANGER
NB12 Growth Inhibition Assay IC50=528.42 nM SANGER
SW756 Growth Inhibition Assay IC50=554.96 nM SANGER
HCC1187 Growth Inhibition Assay IC50=575.83 nM SANGER
NCI-H2342 Growth Inhibition Assay IC50=590.39 nM SANGER
NCI-H2291 Growth Inhibition Assay IC50=598.31 nM SANGER
OVCAR-3 Growth Inhibition Assay IC50=598.96 nM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=629.01 nM SANGER
SAS Growth Inhibition Assay IC50=652.67 nM SANGER
COLO-824 Growth Inhibition Assay IC50=689.37 nM SANGER
HCC1395 Growth Inhibition Assay IC50=698.5 nM SANGER
COLO-668 Growth Inhibition Assay IC50=706.1 nM SANGER
NCI-H226 Growth Inhibition Assay IC50=707.8 nM SANGER
NB17 Growth Inhibition Assay IC50=721.75 nM SANGER
SW1463 Growth Inhibition Assay IC50=739.19 nM SANGER
TGW Growth Inhibition Assay IC50=760.15 nM SANGER
NCI-H526 Growth Inhibition Assay IC50=823.53 nM SANGER
COR-L88 Growth Inhibition Assay IC50=848.12 nM SANGER
NCI-H441 Growth Inhibition Assay IC50=895.22 nM SANGER
NCI-H630 Growth Inhibition Assay IC50=912.96 nM SANGER
Mo-T Growth Inhibition Assay IC50=947.88 nM SANGER
JAR Growth Inhibition Assay IC50=956.24 nM SANGER
NCI-H1838 Growth Inhibition Assay IC50=1.02388 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=1.07376 μM SANGER
MKN28 Growth Inhibition Assay IC50=1.09024 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=1.11905 μM SANGER
TE-9 Growth Inhibition Assay IC50=1.12973 μM SANGER
NY Growth Inhibition Assay IC50=1.16792 μM SANGER
HT55 Growth Inhibition Assay IC50=1.31344 μM SANGER
SW837 Growth Inhibition Assay IC50=1.32978 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=1.41791 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=1.4424 μM SANGER
COLO-741 Growth Inhibition Assay IC50=1.49771 μM SANGER
LU-65 Growth Inhibition Assay IC50=1.62249 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=1.65498 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=1.79479 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=1.95503 μM SANGER
OAW-28 Growth Inhibition Assay IC50=2.06919 μM SANGER
C8166 Growth Inhibition Assay IC50=2.63392 μM SANGER
COLO-678 Growth Inhibition Assay IC50=2.83768 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=2.86381 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=2.90369 μM SANGER
JVM-2 Growth Inhibition Assay IC50=3.03188 μM SANGER
SW1116 Growth Inhibition Assay IC50=3.05411 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=3.10439 μM SANGER
Calu-6 Growth Inhibition Assay IC50=3.1997 μM SANGER
SHP-77 Growth Inhibition Assay IC50=3.528 μM SANGER
Capan-2 Growth Inhibition Assay IC50=4.32581 μM SANGER
SW948 Growth Inhibition Assay IC50=4.74779 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=5.07725 μM SANGER
LAN-6 Growth Inhibition Assay IC50=6.21495 μM SANGER
LU-135 Growth Inhibition Assay IC50=6.43077 μM SANGER
T84 Growth Inhibition Assay IC50=6.9864 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=7.62233 μM SANGER
SW1417 Growth Inhibition Assay IC50=7.91731 μM SANGER
BALL-1 Growth Inhibition Assay IC50=8.50409 μM SANGER
HT-29 Growth Inhibition Assay IC50=9.07599 μM SANGER
C3A Growth Inhibition Assay IC50=9.88394 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=10.5081 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=11.6289 μM SANGER
DU-145 Growth Inhibition Assay IC50=14.5052 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=14.5103 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=14.7809 μM SANGER
ZR-75-30 Growth Inhibition Assay IC50=16.3303 μM SANGER
A673 Growth Inhibition Assay IC50=20.5507 μM SANGER
K-562 Growth Inhibition Assay IC50=28.4183 μM SANGER
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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire 469.55 Formule

C30H23N5O

 Stockage (À compter de la date de réception)
N° CAS 915019-65-7 Télécharger le SDF Stockage des solutions mères

Synonymes NVP-BEZ235 Smiles CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5

Solubilité (Solubility)

In vitro
Lot:

DMSO : 9 mg/mL (19.16 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse Concentration Volume Poids moléculaire
Calculateur de dilution Calculateur de poids moléculaire

In vivo
Lot:

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

mg/kg g μL

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (Mechanism of Action)

Targets/IC50/Ki
p110α
(Cell-free assay)
4 nM
p110γ
(Cell-free assay)
5 nM
mTOR (p70S6K)
(Cell-free assay)
6 nM
p110δ
(Cell-free assay)
7 nM
ATR
(3T3TopBP1-ER cells)
21 nM
p110β
(Cell-free assay)
75 nM
In vitro
Dactolisib (BEZ235) significantly reduces the phosphorylation levels of the mTOR activated kinase p70S6K. It results in a reduction of S235/S236P-RPS6 levels with IC50 of 6.5 nM. The activity of this compound against mTOR is determined using a biochemical mTOR K-LISA assay with IC50 of 20.7 nM. It shows slightly lower activity against its β paralogue with IC50 of 75 nM. The PI3K/Akt/mTOR pathway is often constitutively activated in human tumor cells. BEZ235 blocks PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. Both PTEN-null cell lines PC3M and U87MG show a dose-dependent reduction in cell proliferation when treated with increasing concentrations of it with an average GI50 of 10-12 nM. It is an mTORC1/2 catalytic inhibitor.
Essai kinase
Dosages in vitro de la protéine kinase, PI3K et mTOR
Les protéines PI3Kα, β et δ sont composées du domaine iSH2 de p85 fusionné à l'extrémité NH2 de la protéine p110 pleine longueur, à l'exception de l'α qui ne contient pas non plus les 20 derniers acides aminés. PI3Kγ est produite comme protéine pleine longueur délétée de ses 144 premiers acides aminés. Tous les constructions sont fusionnées à une étiquette His COOH-terminale pour une purification aisée, puis clonées dans les plasmides pBlue-Bac4.5 (pour les isoformes α, β et δ) ou pVL1393 (pour l'isoforme γ). Les différents vecteurs sont ensuite cotransfectés avec de l'ADN génomique BaculoGold WT en utilisant des méthodes recommandées par le fournisseur pour la production des baculovirus et protéines recombinants respectifs. Le Dactolisib (BEZ235) est testé pour son activité contre PI3K à l'aide d'un dosage Kinase-Glo. La réaction de la kinase est effectuée dans une plaque noire de 384 puits. Chaque puits est chargé avec 50 μL d'éléments d'essai (dans 90 % de DMSO) et 5 μL de tampon de réaction contenant 10 μg/mL de substrat PI (l-α-phosphatidylinositol ; Avanti Polar Lipids ; préparé dans 3 % d'octyl-glucoside) et les protéines PI3K (10, 25, 10 et 150 nM de p110α, p110β, p110δ et p110γ, respectivement) sont ensuite ajoutées. La réaction est initiée par l'ajout de 5 μL d'ATP 1 μM préparé dans le tampon de réaction et est incubée pendant 60 (pour p110α, p110β et p110δ) ou 120 min (pour p110γ). Elle est terminée par l'ajout de 10 μL de tampon Kinase-Glo. Les plaques sont ensuite lues dans un lecteur Synergy 2 pour la détection de la luminescence.
In vivo
Dactolisib (BEZ235) induces regression of the tumors (69%) without statistically significant effect on body weight gain. Altogether, these preliminary in vivo efficacy results show that it causes disease stasis when administered orally as a single agent and can enhance the efficacy of other anticancer agents when used in combination studies.
Références
  • [4] https://pubmed.ncbi.nlm.nih.gov/20606035/
  • [5] https://pubmed.ncbi.nlm.nih.gov/21412767/
  • [6] https://pubmed.ncbi.nlm.nih.gov/22662154/
  • [7] https://pubmed.ncbi.nlm.nih.gov/20876803/
  • [8] https://pubmed.ncbi.nlm.nih.gov/21552262/

Applications (Applications)

Méthodes Biomarqueurs Images PMID
Western blot Myc / Vinculin / pT58 Myc pAkt / Akt / Skp2 / AR / pS6 / p27 p-S6K / S6K / p-Akt / Akt / p-ABL / BCR-ABL Bcl-2 / Caspase-3 / Cleaved caspase-3 Cyclin D1 / Cyclin D2 mTOR / p-mTOR / p70S6K / p-p70S6K p-EGFR-Tyr1068 / EGFR / p-HER2-Tyr1221 / p-HER2-Tyr1222 / HER2 / p-HER3-Tyr1289
S1009-WB1
25934076
Immunofluorescence SP1 p-ErbB2(Y1248) LC3
S1009-IF1
26336820
Growth inhibition assay Cell viability (P3, U87) Cell viability (breast cancer cells) Cell viability (K562, KBM7R)
S1009-viability1
27542970
ELISA VEGF
S1009-ELISA1
19671762

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT Recrutement Conditions Promoteur/Collaborateurs Date de début Phases
NCT01856101 Terminated
Carcinoma Transitional Cell
Cliniques universitaires Saint-Luc- Université Catholique de Louvain|Novartis
 February 2013 Phase 2
NCT01717898 Terminated
Castrate-resistant Prostate Cancer
Charles Ryan|Novartis Pharmaceuticals|University of California San Francisco
 January 31 2013 Phase 1|Phase 2
NCT01756118 Completed
Acute Lymphoblastic Leukemia|Leukemia Myelocytic Acute|Chronic Myelogenous Leukemia With Crisis of Blast Cells
Goethe University
 June 2012 Phase 1
NCT01290406 Withdrawn
Endometrial Cancer
Novartis Pharmaceuticals|Novartis
 March 2012 Phase 2
NCT01288092 Withdrawn
Metastatic Breast Cancer
Novartis Pharmaceuticals|Novartis
 March 2012 Phase 2

Foire aux questions (Frequently Asked Questions)

Question 1:
With difficulties in dissolving it, how can I improve its solubility?

Réponse :
For in vivo study, we suggest the vehicle solution NMP/polyethylene glycol 300 (10/90, v/v). Please dissolve it in NMP as more as possible. You can sonicate and warm this compound in water bath for a while. Then dilute with PEG 300.