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Dactolisib (BEZ235) PI3K remmer

Name: Dactolisib (BEZ235)
Brand: Selleck Chemicals
SKU: S1009
Rating: 5 (503 reviews)

Cat.nr.S1009

Dactolisib (BEZ235, NVP-BEZ235) is een dubbele ATP-competitieve PI3K en mTOR remmer voor p110α/γ/δ/β en mTOR(p70S6K) met een IC50 van respectievelijk 4 nM /5 nM /7 nM /75 nM /6 nM in celvrije assays. Het remt ATR met een IC50 van 21 nM in 3T3^TopBP1-ER cellen, induceert autophagy en onderdrukt HIV-1 replicatie. Fase 2.

Dactolisib (BEZ235) PI3K remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 469.55

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Kwaliteitscontrole

Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Overig PI3K Inhibitoren	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) LY294002 XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549)

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Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	469.55	Formule	C₃₀H₂₃N₅O	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	915019-65-7	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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

Oplosbaarheid

In vitro
Batch:

DMSO : 9 mg/mL (19.16 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.205mg/ml (0.44mM)	Taking the 1 mL working solution as an example, add 50 μL 4.1 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

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 (3T3^TopBP1-ER cells) 21 nM p110β (Cell-free assay) 75 nM
In vitro	Dactolisib (BEZ235) vermindert significant de fosforyleringsniveaus van het mTOR geactiveerde kinase p70S6K. Dit resulteert in een verlaging van de S235/S236P-RPS6 niveaus met een IC50 van 6,5 nM. De activiteit van deze verbinding tegen mTOR wordt bepaald met behulp van een biochemische mTOR K-LISA assay met een IC50 van 20,7 nM. Het vertoont een iets lagere activiteit tegen zijn β-paraloog met een IC50 van 75 nM. De PI3K/Akt/mTOR route is vaak constitutief geactiveerd in menselijke tumorcellen. BEZ235 blokkeert de PI3K en mTOR kinase activiteit door te binden aan de ATP-bindingsspleet van deze enzymen. Beide PTEN-nul cellijnen PC3M en U87MG vertonen een dosisafhankelijke vermindering van celproliferatie bij behandeling met toenemende concentraties ervan met een gemiddelde GI50 van 10-12 nM. Het is een mTORC1/2 katalytische remmer.
Kinase Assay	In vitro proteïne kinase, PI3K en mTOR assays
Kinase Assay	PI3Kα, β en δ eiwitten zijn samengesteld uit het iSH2 domein van p85 NH₂-terminaal gefuseerd aan het volledige p110 eiwit, met uitzondering van α dat ook de laatste 20 aminozuren niet bevat. PI3Kγ wordt geproduceerd als volledig eiwit, zonder de eerste 144 aminozuren. Alle constructen zijn gefuseerd aan een COOH-terminale His-tag voor gemakkelijke zuivering en vervolgens gekloneerd in de pBlue-Bac4.5 (voor α, β en δ isoformen) of pVL1393 (voor γ isoform) plasmiden. De verschillende vectoren worden vervolgens gecotransfecteerd met BaculoGold WT genomisch DNA met behulp van methoden aanbevolen door de leverancier voor de productie van de respectievelijke recombinante baculovirussen en eiwitten. Dactolisib (BEZ235) wordt getest op zijn activiteit tegen PI3K met behulp van een Kinase-Glo assay. De kinase reactie wordt uitgevoerd in een 384-wells zwarte plaat. Elke put wordt geladen met 50 μL testitems (in 90% DMSO) en 5 μL reactiebuffer die 10 μg/mL PI substraat bevat (l-α-fosfatidylinositol; Avanti Polar Lipids; bereid in 3% octyl-glucoside) en de PI3K eiwitten (respectievelijk 10, 25, 10 en 150 nM van p110α, p110β, p110δ en p110γ) worden er vervolgens aan toegevoegd. De reactie wordt gestart door de toevoeging van 5 μL van 1 μM ATP bereid in de reactiebuffer en wordt geïncubeerd gedurende 60 (voor p110α, p110β en p110δ) of 120 min (voor p110γ). Het wordt beëindigd door de toevoeging van 10 μL Kinase-Glo buffer. De platen worden vervolgens afgelezen in een Synergy 2 reader voor luminescentiedetectie.
In vivo	Dactolisib (BEZ235) induceert regressie van de tumoren (69%) zonder statistisch significant effect op gewichtstoename. Al met al tonen deze voorlopige in vivo werkzaamheidsresultaten aan dat het ziektestase veroorzaakt wanneer het oraal wordt toegediend als enkelvoudig middel en de werkzaamheid van andere antikankermiddelen kan verbeteren wanneer het wordt gebruikt in combinatiestudies.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/18606717/ [2] https://pubmed.ncbi.nlm.nih.gov/21966435/ [3] https://pubmed.ncbi.nlm.nih.gov/21791089/ [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/

Toepassingen

Methoden	Biomarkers	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

Informatie over klinische proeven

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
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

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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Veelgestelde vragen

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

Antwoord:
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.

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