Home PI3K/Akt/mTOR PI3K inhibitor - ATM/ATR inhibitor - mTOR inhibitor - Autophagy activator - HIV inhibitor Dactolisib (BEZ235) For research use only.

Dactolisib (BEZ235)

Synonyms: NVP-BEZ235

Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.

Dactolisib (BEZ235) Chemical Structure

Dactolisib (BEZ235) Chemical Structure

CAS No. 915019-65-7

Purity & Quality Control

Dactolisib (BEZ235) Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description 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
Click to View More Cell Line Experimental Data

Biological Activity

Description Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Targets
p110α [1]
(Cell-free assay)		 p110γ [1]
(Cell-free assay)		 mTOR (p70S6K) [1]
(Cell-free assay)		 p110δ [1]
(Cell-free assay)		 ATR [8]
(3T3TopBP1-ER cells)		 Click to View More Targets
4 nM 5 nM 6 nM 7 nM 21 nM
In vitro
In vitro BEZ235 significantly reduces the phosphorylation levels of the mTOR activated kinase p70S6K. BEZ235 results in a reduction of S235/S236P-RPS6 levels with IC50 of 6.5 nM. The activity of BEZ235 against mTOR is determined using a biochemical mTOR K-LISA assay with IC50 of 20.7 nM. BEZ235 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 BEZ235 with an average GI50 of 10-12 nM. [1] BEZ235 is an mTORC1/2 catalytic inhibitor. [2]
Kinase Assay In vitro Protein Kinase, PI3K, and mTOR Assays
PI3Kα, β, and δ proteins are composed of the iSH2 domain of p85 NH2-terminally fused to the full-length protein p110 protein, with the exception of α that also does not contain the last 20 amino acids. PI3Kγ is produced as full-length protein deleted for its first 144 amino acids. All constructs are fused to a COOH-terminal His tag for convenient purification and then cloned into the pBlue-Bac4.5 (for α, β, and δ isoforms) or pVL1393 (for γ isoform) plasmids. The different vectors are then cotransfected with BaculoGold WT genomic DNA using methods recommended by the vendor for production of the respective recombinant baculoviruses and proteins. BEZ235 are tested for their activity against PI3K using a Kinase-Glo assay. The kinase reaction is done in 384-well black plate. Each well is loaded with 50 μL of test items (in 90% DMSO) and 5 μL reaction buffer containing 10 μg/mL PI substrate (l-α-phosphatidylinositol; Avanti Polar Lipids; prepared in 3% octyl-glucoside) and the PI3K proteins (10, 25, 10, and 150 nM of p110α, p110β, p110δ, and p110γ, respectively) are then added to it. The reaction is started by the addition of 5 μL of 1 μM ATP prepared in the reaction buffer and is incubated for either 60 (for p110α, p110β, and p110δ) or 120 min (for p110γ). It is terminated by the addition of 10 μL Kinase-Glo buffer. The plates are then read in a Synergy 2 reader for luminescence detection.
Cell Research Cell lines HCT116, DLD-1 and SW480 cells
Concentrations 0-1 μM
Incubation Time 48 hours
Method

The human CRC cell lines, HCT116 (PIK3CA mutant; kinase domain at H1047R), DLD-1 (PIK3CA mutant; helical domain at E545K), and SW480 (PIK3CA wild-type) and isogenic DLD-1 PIK3CA mutant as well as wild-type cells are maintained in DMEM with 10% FBS and 1 × Penicillin/Streptomycin. Cells are plated at different initial densities (HCT116: 3 × 103 cells/well, DLD-1: 5.5 × 103 cells/well, SW480: 4.5 × 103 cells/well, DLD-1 PIK3CA mutant: 7 × 103 cells/well, and DLD-1 PIK3CA wild-type: 9 × 103 cells/well) to account for differential growth kinetics. After 16 hours, cells are incubated with increasing concentrations of BEZ235, and the drug-containing growth medium is changed every 24 hours. Cell viability is assessed 16 hours after the initial plating and 48 hours after initiation of drug treatment using the colorimetric MTS assay CellTiter 96® AQueous One Solution Cell Proliferation Assay, as per the manufacturer's instructions. Cell viability after drug treatment is normalized to that of untreated cells also grown for 48 hours. For western blot analysis, cells are plated with zero or maximum inhibitory dose (500 nM) BEZ235 for 2, 6, 24, or 48 hours.
Experimental Result Images Methods Biomarkers 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 25934076
Immunofluorescence SP1 p-ErbB2(Y1248) LC3 26336820
Growth inhibition assay Cell viability (P3, U87) Cell viability (breast cancer cells) Cell viability (K562, KBM7R) 27542970
ELISA VEGF 19671762
In Vivo
In vivo BEZ235 induces regression of the tumors (69%) without statistically significant effect on body weight gain. Altogether, these preliminary in vivo efficacy results show that BEZ235 causes disease stasis when administered orally as a single agent and can enhance the efficacy of other anticancer agents when used in combination studies. [1]
Animal Research Animal Models Female Harlan athymic nude mice
Dosages 45 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date 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

Chemical Information & Solubility

Molecular Weight 469.55 Formula

C30H23N5O
CAS No. 915019-65-7 SDF Download Dactolisib (BEZ235) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 9 mg/mL ( (19.16 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
With difficulties in dissolving BEZ235, How can I improve its solubility?

Answer:
For in vivo study, we suggest the vehicle solution NMP/polyethylene glycol 300 (10/90, v/v). Please dissolve BEZ235 in NMP as more as possible. You can sonicate and warm it in water bath for a while. Then dilute with PEG 300.

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