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

solo per uso di ricerca

Dactolisib (BEZ235) PI3K Inibitore

N. Cat.: S1009

Dactolisib (BEZ235, NVP-BEZ235) è un doppio inibitore ATP-competitivo di PI3K e mTOR per p110α/γ/δ/β e mTOR(p70S6K) con IC50 di 4 nM /5 nM /7 nM /75 nM /6 nM in saggi acellulari, rispettivamente. Inibisce ATR con IC50 di 21 nM in cellule 3T3TopBP1-ER, induce l'autophagy e sopprime la replicazione di HIV-1. Fase 2.
Dactolisib (BEZ235) PI3K Inibitore Chemical Structure

Struttura chimica

Peso molecolare: 469.55

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.99%
99.99

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
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
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 469.55 Formula

C30H23N5O

 Conservazione (Dalla data di ricezione)
N. CAS 915019-65-7 Scarica SDF Conservazione delle soluzioni stock

Sinonimi 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

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 9 mg/mL (19.16 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : 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)

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.
Saggio chinasico
Saggi in vitro di Protein Kinase, PI3K e mTOR
Le proteine PI3Kα, β e δ sono composte dal dominio iSH2 di p85 fuso all'estremità NH2 della proteina p110 a lunghezza intera, con l'eccezione dell'α che non contiene gli ultimi 20 amminoacidi. PI3Kγ è prodotta come proteina a lunghezza intera priva dei suoi primi 144 amminoacidi. Tutte le costruzioni sono fuse a un tag His COOH-terminale per una comoda purificazione e quindi clonate nei plasmidi pBlue-Bac4.5 (per le isoforme α, β e δ) o pVL1393 (per l'isoforma γ). I diversi vettori vengono quindi cotrasfettati con DNA genomico BaculoGold WT utilizzando metodi raccomandati dal fornitore per la produzione dei rispettivi baculovirus e proteine ricombinanti. Dactolisib (BEZ235) viene testato per la sua attività contro PI3K utilizzando un saggio Kinase-Glo. La reazione chinasica viene eseguita in una piastra nera a 384 pozzetti. Ogni pozzetto viene caricato con 50 μL di elementi di prova (nel 90% di DMSO) e 5 μL di tampone di reazione contenente 10 μg/mL di substrato PI (l-α-fosfatidilinositolo; Avanti Polar Lipids; preparato in 3% di ottil-glucoside) e le proteine PI3K (10, 25, 10 e 150 nM di p110α, p110β, p110δ e p110γ, rispettivamente) vengono quindi aggiunte ad esso. La reazione viene avviata con l'aggiunta di 5 μL di ATP 1 μM preparato nel tampone di reazione e viene incubata per 60 (per p110α, p110β e p110δ) o 120 min (per p110γ). Viene terminata con l'aggiunta di 10 μL di tampone Kinase-Glo. Le piastre vengono quindi lette in un lettore Synergy 2 per la rilevazione della luminescenza.
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.
Riferimenti
  • [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/

Applicazioni (Applications)

Metodi Biomarcatori Immagini 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

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT Reclutamento Condizioni Sponsor/Collaboratori Data di inizio Fasi
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

Domande Frequenti (Frequently Asked Questions)

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

Risposta:
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.