Dactolisib (BEZ235)

别名: NVP-BEZ235 中文名称:达克利司

Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3KmTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。

Dactolisib (BEZ235) Chemical Structure

Dactolisib (BEZ235) Chemical Structure

CAS: 915019-65-7

规格 价格 库存 购买数量
50mg 895.88 现货
100mg 1414.41 现货
200mg 2530.71 现货
1g 7944.3 现货
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Dactolisib (BEZ235)相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
Trypanosoma brucei brucei Function Assay 200 nM 12 h Effect on phosphatidylcholine level 24805946
Trypanosoma brucei brucei Function Assay 200 nM 12 h Effect on sphingomylein level 24805946
Trypanosoma brucei brucei Function Assay 200 nM 12 h Decrease in phosphotidyl inositol phosphate level 24805946
PC3 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.66 M 22336246
DU145 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.16 M 22336246
MKN74 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.42 M 22336246
MKN45 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.34 M 22336246
MKN28 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.07 M 22336246
MKN7 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.68 M 22336246
MKN1 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.41 M 22336246
St-4 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.47 M 22336246
ACHN Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.95 M 22336246
RXF631L Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.21 M 22336246
SKOV3 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.41 M 22336246
OVCAR8 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.84 M 22336246
OVCAR5 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.57 M 22336246
OVCAR4 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.58 M 22336246
OVCAR3 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.17 M 22336246
LOXIMVI Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.66 M 22336246
DMS114 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.39 M 22336246
DMS273 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.80 M 22336246
A549 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.07 M 22336246
NCI-H438 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.11 M 22336246
NCI-H522 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.45 M 22336246
NCI-H226 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.44 M 22336246
NCI-H23 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.64 M 22336246
HCT116 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.61 M 22336246
HCT15 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.03 M 22336246
HT-29 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.75 M 22336246
KM12 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.54 M 22336246
HCC2998 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.05 M 22336246
SNB78 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.65 M 22336246
SNB75 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.58 M 22336246
SF539 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.59 M 22336246
SF295 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.31 M 22336246
SF268 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.92 M 22336246
U251 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.66 M 22336246
MDA-MB-231 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.09 M 22336246
MCF7 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.16 M 22336246
HBC5 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-7.87 M 22336246
BSY1 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.48 M 22336246
HBC4 Growth Inhibition Assay 0.01-100 μM 48 h Log GI50=-8.61 M 22336246
U87MG Growth Inhibition Assay 0.01-100 μM 48 h IC50=1.32 μM 23871904
HCT116 Growth Inhibition Assay 0.01-100 μM 48 h IC50=1.16 μM 23871904
MCF7 Growth Inhibition Assay 0.01-100 μM 48 h IC50=0.73 μM 23871904
Trypanosoma brucei brucei Function Assay 18 h Inhibition of receptor-mediated endocytosis assessed as decrease in transferrin uptake 24805946
Trypanosoma brucei brucei Antimicrobial Assay 18 h Antitrypanosomal activity with EC50 of 0.0025 μM 24805946
AGS Growth Inhibition Assay IC50=48.77 nM SANGER
MCF7 Growth Inhibition Assay IC50=48.58 nM SANGER
LoVo Growth Inhibition Assay IC50=48.4 nM SANGER
NCI-H1155 Growth Inhibition Assay IC50=48.32 nM SANGER
NCI-H1623 Growth Inhibition Assay IC50=47.76 nM SANGER
LB996-RCC Growth Inhibition Assay IC50=47.19 nM SANGER
TE-5 Growth Inhibition Assay IC50=46.84 nM SANGER
PC-14 Growth Inhibition Assay IC50=46.57 nM SANGER
A4-Fuk Growth Inhibition Assay IC50=46.52 nM SANGER
DOHH-2 Growth Inhibition Assay IC50=46.37 nM SANGER
NCI-H1355 Growth Inhibition Assay IC50=46.34 nM SANGER
EW-22 Growth Inhibition Assay IC50=46.2 nM SANGER
KYSE-180 Growth Inhibition Assay IC50=46.17 nM SANGER
IGR-1 Growth Inhibition Assay IC50=46.13 nM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=46.04 nM SANGER
NOMO-1 Growth Inhibition Assay IC50=45.87 nM SANGER
KNS-62 Growth Inhibition Assay IC50=45.38 nM SANGER
HD-MY-Z Growth Inhibition Assay IC50=44.92 nM SANGER
KS-1 Growth Inhibition Assay IC50=44.66 nM SANGER
NCI-H2452 Growth Inhibition Assay IC50=44.58 nM SANGER
PSN1 Growth Inhibition Assay IC50=44.4 nM SANGER
EPLC-272H Growth Inhibition Assay IC50=44.39 nM SANGER
T-24 Growth Inhibition Assay IC50=43.83 nM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=43 nM SANGER
BHY Growth Inhibition Assay IC50=42.72 nM SANGER
8305C Growth Inhibition Assay IC50=41.87 nM SANGER
HT Growth Inhibition Assay IC50=41.02 nM SANGER
G-401 Growth Inhibition Assay IC50=40.82 nM SANGER
NB5 Growth Inhibition Assay IC50=40.64 nM SANGER
MZ2-MEL Growth Inhibition Assay IC50=39.66 nM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=39.51 nM SANGER
A101D Growth Inhibition Assay IC50=38.97 nM SANGER
LB1047-RCC Growth Inhibition Assay IC50=38.81 nM SANGER
CO-314 Growth Inhibition Assay IC50=38.74 nM SANGER
HCC1419 Growth Inhibition Assay IC50=38.71 nM SANGER
CAL-12T Growth Inhibition Assay IC50=38.6 nM SANGER
SJSA-1 Growth Inhibition Assay IC50=38.54 nM SANGER
U251 Growth Inhibition Assay IC50=38.43 nM SANGER
RKO Growth Inhibition Assay IC50=38.33 nM SANGER
MN-60 Growth Inhibition Assay IC50=37.96 nM SANGER
CAL-39 Growth Inhibition Assay IC50=37.9 nM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=37.59 nM SANGER
8505C Growth Inhibition Assay IC50=37.51 nM SANGER
8-MG-BA Growth Inhibition Assay IC50=37.25 nM SANGER
CAL-62 Growth Inhibition Assay IC50=36.86 nM SANGER
Daoy Growth Inhibition Assay IC50=36.7 nM SANGER
CAKI-1 Growth Inhibition Assay IC50=36.43 nM SANGER
LAMA-84 Growth Inhibition Assay IC50=35.87 nM SANGER
OVCAR-5 Growth Inhibition Assay IC50=35.47 nM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=35.41 nM SANGER
CAL-120 Growth Inhibition Assay IC50=34.72 nM SANGER
NCI-H28 Growth Inhibition Assay IC50=34.44 nM SANGER
Becker Growth Inhibition Assay IC50=34.21 nM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=34.15 nM SANGER
RPMI-8226 Growth Inhibition Assay IC50=33.82 nM SANGER
COLO-684 Growth Inhibition Assay IC50=33.58 nM SANGER
Ca9-22 Growth Inhibition Assay IC50=33.55 nM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=33.43 nM SANGER
A2058 Growth Inhibition Assay IC50=33.25 nM SANGER
COLO-800 Growth Inhibition Assay IC50=32.92 nM SANGER
CTV-1 Growth Inhibition Assay IC50=32.82 nM SANGER
ECC10 Growth Inhibition Assay IC50=31.95 nM SANGER
EW-18 Growth Inhibition Assay IC50=31.86 nM SANGER
BE-13 Growth Inhibition Assay IC50=31.82 nM SANGER
BEN Growth Inhibition Assay IC50=31.63 nM SANGER
OVCAR-8 Growth Inhibition Assay IC50=31.26 nM SANGER
KU-19-19 Growth Inhibition Assay IC50=31.13 nM SANGER
JVM-3 Growth Inhibition Assay IC50=30.83 nM SANGER
QIMR-WIL Growth Inhibition Assay IC50=30.6 nM SANGER
AsPC-1 Growth Inhibition Assay IC50=30.2 nM SANGER
NOS-1 Growth Inhibition Assay IC50=30.12 nM SANGER
BHT-101 Growth Inhibition Assay IC50=30.05 nM SANGER
GI-ME-N Growth Inhibition Assay IC50=29.91 nM SANGER
T98G Growth Inhibition Assay IC50=29.88 nM SANGER
U-2-OS Growth Inhibition Assay IC50=29.5 nM SANGER
D-263MG Growth Inhibition Assay IC50=29.35 nM SANGER
ONS-76 Growth Inhibition Assay IC50=29.05 nM SANGER
ES1 Growth Inhibition Assay IC50=28.84 nM SANGER
MV-4-11 Growth Inhibition Assay IC50=28.7 nM SANGER
A3-KAW Growth Inhibition Assay IC50=28.64 nM SANGER
A204 Growth Inhibition Assay IC50=28.47 nM SANGER
SW1088 Growth Inhibition Assay IC50=28.29 nM SANGER
DB Growth Inhibition Assay IC50=27.36 nM SANGER
NCI-H292 Growth Inhibition Assay IC50=27 nM SANGER
RS4-11 Growth Inhibition Assay IC50=26.91 nM SANGER
SW962 Growth Inhibition Assay IC50=26.76 nM SANGER
HuO9 Growth Inhibition Assay IC50=26.76 nM SANGER
HOP-92 Growth Inhibition Assay IC50=26.48 nM SANGER
SK-LU-1 Growth Inhibition Assay IC50=26.17 nM SANGER
LXF-289 Growth Inhibition Assay IC50=26.04 nM SANGER
KYSE-150 Growth Inhibition Assay IC50=25.89 nM SANGER
MPP-89 Growth Inhibition Assay IC50=25.32 nM SANGER
TI-73 Growth Inhibition Assay IC50=25.28 nM SANGER
ES3 Growth Inhibition Assay IC50=25.22 nM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=25.15 nM SANGER
MOLT-4 Growth Inhibition Assay IC50=25.12 nM SANGER
FTC-133 Growth Inhibition Assay IC50=25.1 nM SANGER
CTB-1 Growth Inhibition Assay IC50=24.67 nM SANGER
NBsusSR Growth Inhibition Assay IC50=24.6 nM SANGER
Hs-578-T Growth Inhibition Assay IC50=24.58 nM SANGER
EFO-27 Growth Inhibition Assay IC50=24.33 nM SANGER
MEL-HO Growth Inhibition Assay IC50=24.04 nM SANGER
A375 Growth Inhibition Assay IC50=23.93 nM SANGER
CAL-51 Growth Inhibition Assay IC50=23.89 nM SANGER
BV-173 Growth Inhibition Assay IC50=23.87 nM SANGER
MG-63 Growth Inhibition Assay IC50=23.45 nM SANGER
SW780 Growth Inhibition Assay IC50=23.13 nM SANGER
TGBC1TKB Growth Inhibition Assay IC50=23.05 nM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=22.96 nM SANGER
NB69 Growth Inhibition Assay IC50=22.53 nM SANGER
ME-180 Growth Inhibition Assay IC50=22.43 nM SANGER
786-0 Growth Inhibition Assay IC50=22.29 nM SANGER
G-402 Growth Inhibition Assay IC50=22.16 nM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=21.95 nM SANGER
HT-1080 Growth Inhibition Assay IC50=21.93 nM SANGER
YH-13 Growth Inhibition Assay IC50=21.88 nM SANGER
NCI-H2030 Growth Inhibition Assay IC50=21.52 nM SANGER
RXF393 Growth Inhibition Assay IC50=21.45 nM SANGER
ES4 Growth Inhibition Assay IC50=21.08 nM SANGER
HOS Growth Inhibition Assay IC50=21.06 nM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=20.63 nM SANGER
DEL Growth Inhibition Assay IC50=20.49 nM SANGER
RT-112 Growth Inhibition Assay IC50=19.66 nM SANGER
KNS-81-FD Growth Inhibition Assay IC50=19.54 nM SANGER
GAMG Growth Inhibition Assay IC50=19.48 nM SANGER
SF126 Growth Inhibition Assay IC50=19.41 nM SANGER
RPMI-7951 Growth Inhibition Assay IC50=19.28 nM SANGER
SF295 Growth Inhibition Assay IC50=18.93 nM SANGER
IST-MEL1 Growth Inhibition Assay IC50=18.77 nM SANGER
SW1710 Growth Inhibition Assay IC50=18.72 nM SANGER
BCPAP Growth Inhibition Assay IC50=18.65 nM SANGER
HuH-7 Growth Inhibition Assay IC50=18.4 nM SANGER
ES7 Growth Inhibition Assay IC50=18.09 nM SANGER
HGC-27 Growth Inhibition Assay IC50=18.06 nM SANGER
EW-16 Growth Inhibition Assay IC50=18.04 nM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=17.83 nM SANGER
D-56MG Growth Inhibition Assay IC50=17.69 nM SANGER
697 Growth Inhibition Assay IC50=17.43 nM SANGER
NCI-H209 Growth Inhibition Assay IC50=17.29 nM SANGER
MOLT-16 Growth Inhibition Assay IC50=17.15 nM SANGER
OS-RC-2 Growth Inhibition Assay IC50=16.47 nM SANGER
EGI-1 Growth Inhibition Assay IC50=16.43 nM SANGER
NUGC-3 Growth Inhibition Assay IC50=16.34 nM SANGER
HH Growth Inhibition Assay IC50=15.7 nM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=15.63 nM SANGER
CHL-1 Growth Inhibition Assay IC50=15.45 nM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=15.1 nM SANGER
COR-L105 Growth Inhibition Assay IC50=15.04 nM SANGER
LOXIMVI Growth Inhibition Assay IC50=14.99 nM SANGER
ES5 Growth Inhibition Assay IC50=14.74 nM SANGER
LB2241-RCC Growth Inhibition Assay IC50=14.01 nM SANGER
EoL-1 Growth Inhibition Assay IC50=13.93 nM SANGER
GCT Growth Inhibition Assay IC50=13.68 nM SANGER
KARPAS-45 Growth Inhibition Assay IC50=13.51 nM SANGER
NCI-H1793 Growth Inhibition Assay IC50=12.82 nM SANGER
BB65-RCC Growth Inhibition Assay IC50=12.72 nM SANGER
H4 Growth Inhibition Assay IC50=12.67 nM SANGER
HSC-3 Growth Inhibition Assay IC50=12.21 nM SANGER
Mewo Growth Inhibition Assay IC50=11.99 nM SANGER
PA-1 Growth Inhibition Assay IC50=11.82 nM SANGER
ES8 Growth Inhibition Assay IC50=10.9 nM SANGER
L-363 Growth Inhibition Assay IC50=10.69 nM SANGER
769-P Growth Inhibition Assay IC50=10.44 nM SANGER
A549 Growth Inhibition Assay IC50=10.14 nM SANGER
MFE-280 Growth Inhibition Assay IC50=9.99 nM SANGER
TYK-nu Growth Inhibition Assay IC50=9.94 nM SANGER
CAMA-1 Growth Inhibition Assay IC50=9.8 nM SANGER
NCI-H1666 Growth Inhibition Assay IC50=9.71 nM SANGER
DU-4475 Growth Inhibition Assay IC50=9.44 nM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=9.12 nM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=8.49 nM SANGER
ETK-1 Growth Inhibition Assay IC50=7.88 nM SANGER
LU-139 Growth Inhibition Assay IC50=7.77 nM SANGER
KP-4 Growth Inhibition Assay IC50=7 nM SANGER
HCC2218 Growth Inhibition Assay IC50=6.61 nM SANGER
HN Growth Inhibition Assay IC50=5.96 nM SANGER
AN3-CA Growth Inhibition Assay IC50=5.56 nM SANGER
PC-3 Growth Inhibition Assay IC50=5.09 nM SANGER
BPH-1 Growth Inhibition Assay IC50=4.76 nM SANGER
BFTC-909 Growth Inhibition Assay IC50=3.71 nM SANGER
NCI-H720 Growth Inhibition Assay IC50=3.57 nM SANGER
MKN1 Growth Inhibition Assay IC50=2.8 nM SANGER
SBC-1 Growth Inhibition Assay IC50=742 pM SANGER
UM-UC-3 Growth Inhibition Assay IC50=315 pM 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
点击查看更多细胞系数据

生物活性

产品描述 Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3KmTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。
靶点
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)
点击更多
4 nM 5 nM 6 nM 7 nM 21 nM
体外研究(In Vitro)
体外研究活性 BEZ235显著降低mTOR活化的激酶p70S6K的磷酸化水平。BEZ235导致S235/S236P-RPS6水平减少,IC50为6.5 nM。BEZ235抗mTOR的活性使用生化mTOR K-LISA试验测定,IC50为20.7 nM。BEZ235对其β旁系同源物的活性稍弱,IC50为75 nM。在人肿瘤细胞中,PI3K/Akt/mTOR通路经常被组成性活化。BEZ235阻断PI3K和mTOR激酶活性,通过结合于这些酶的ATP结合槽发挥作用。用逐渐增加浓度BEZ235处理PTEN-null细胞系PC3M和U87MG时,导致细胞增殖剂量依赖性减少,平均GI50为10-12 nM。[1] BEZ235是一种mTORC1/2催化抑制剂。[2]
激酶实验 体外蛋白激酶,PI3K,和mTOR实验
PI3Kα, β, δ蛋白都由与p110全长蛋白相接的p85 N端的iSH2域组成,只是PI3Kα没有最后的20个氨基酸。PI3Kγ由p110全长蛋白去掉前144个氨基酸产生而来。所有PI3K蛋白在羧基末端加组氨酸标签便于纯化,然后克隆到pBlue-Bac4.5 (用于α, β,和δ亚型) 或者pVL1393 (用于γ 亚型) 质粒中。转染BaculoGold WT基因组DNA的不同的载体按说明书推荐的方法生产各自重组体杆状病毒及重组蛋白。使用激酶发光检测试剂盒测定BEZ235 (NVP-BEZ235)作用于PI3K的活力。在384孔板上进行激酶实验。在每个孔中加入50 nl的测试项目(溶在90%DMSO中)和5ul的反应buffer,反应buffer包含10 μg/ml PI基质 (l-α-磷脂酰肌醇; 由Avanti Polar Lipids提供;预备在3%辛基葡萄糖苷中),然后加入PI3K 蛋白(p110α, p110β, p110δ,和p110γ分别为10, 25, 10,和150 nM)。加入预备在反应buffer中的5 ul 1 µM 的ATP反应开始,反应进行60分钟 (测p110α, p110β, p110δ)或者120分钟(测p110γ),随后加入10ul的荧光激酶buffer终止反应。数据用Synergy 2 阅读器阅读用于荧光测试。
细胞实验 细胞系 HCT116, DLD-1, SW480
浓度 0-1 μM
孵育时间 48小时
方法

HCT116 (PIK3CA突变型; 激酶域在H1047R), DLD-1 (PIK3CA突变型;螺旋域在E545K), SW480 (PIK3CA 野生型)人类CRC细胞系,同基因型的DLD-1 PIK3CA突变和野生型细胞培养在含10%FBS和1×青霉素/链霉素的培养基中。细胞按不同的初始密度加入(HCT116: 3000个细胞/每孔, DLD-1: 5500个细胞/每孔, SW480: 4500个细胞/每孔, DLD-1 PIK3CA突变型: 7000个细胞/每孔, DLD-1 PIK3CA野生型: 9000个细胞/每孔),用来计算不同的生长动力学。16个小时后,细胞加入浓度越来越高的BEZ235中进行温育,含有药物的培养基24小时更换一次。根据产品说明书,加入细胞16小时和药物处理48小时,使用单溶液细胞增殖检测试剂盒以比色法检测细胞活力。与没有用药物处理正在生长的细胞相比,药物处理的细胞的活力也逐渐趋于正常化。使用GraphPad Prism 5软件用4个参数的回归曲线计算IC50值。用于western blot 分析,细胞用0 nM 或者最高抑制剂量(500 nM) BEZ235处理 2, 6, 24, 或者48 小时。

实验图片 检测方法 检测指标 实验图片 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
体内研究(In Vivo)
体内研究活性 BEZ235诱导肿瘤(69%)消退,而对体重增加没有统计学上显著的作用。总之,这些初步的体内功效研究结果表明,BEZ235单一口服给药时能够阻断疾病的发展,与其他抗癌药结合使用时能够增强疗效。[1]
动物实验 Animal Models 雌性Harlan无胸腺裸鼠
Dosages 45 mg/kg
Administration 口服处理
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

化学信息&溶解度

分子量 469.55 分子式

C30H23N5O

CAS号 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
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 9 mg/mL ( (19.16 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

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操作手册

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常见问题及建议解决方法

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

回答:
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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