Home PI3K/Akt/mTOR PI3K Inhibitor Pictilisib (GDC-0941)

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Pictilisib (GDC-0941) PI3Kα/δ Inhibitor

Kat.-Nr.S1065

Pictilisib (GDC-0941, RG7321) ist ein potenter Inhibitor von PI3Kα/δ mit einer IC50 von 3 nM in zellfreien Assays, mit moderater Selektivität gegenüber p110β (11-fach) und p110γ (25-fach). Pictilisib (GDC-0941) induziert Autophagy und Apoptosis. Phase 2.
Pictilisib (GDC-0941) PI3K Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 513.64

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Qualitätskontrolle

Charge: Reinheit: 99.97%
99.97

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
Sf9 Kinase Assay 1 h DMSO Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM 18754654
Sf9 Kinase Assay 1 h DMSO Inhibition of human recombinant PI3K p110beta H1047-R mutant expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM 18754654
Sf9 Kinase Assay 1 h DMSO Inhibition of human recombinant PI3K p110beta E545-K mutant expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM 18754654
Sf9 Kinase Assay 1 h DMSO Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.033 μM 18754654
Sf9 Kinase Assay 1 h DMSO Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha 18754654
MDA-MB-361 Function Assay 2 h DMSO Inhibition of Akt Ser473 phosphorylation in human MDA-MB-361 cells with PIK3CA E545-K mutation with IC50 of 0.028 μM 18754654
PC3 Function Assay 2 h DMSO Inhibition of Akt Ser473 phosphorylation in PTEN-null human PC3 cells with IC50 of 0.037 μM 18754654
U87MG Function Assay 2 h DMSO Inhibition of Akt Ser473 phosphorylation in PTEN-null human U87MG cells with IC50 of 0.046 μM 18754654
MDA-MB-361 Growth Inhibition Assay 96 h DMSO Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation with IC50 of 0.72 μM 18754654
A2780 Growth Inhibition Assay 96 h DMSO Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation with IC50 of 0.14 μM 18754654
PC3 Growth Inhibition Assay 96 h DMSO IC50=0.28 μM 18754654
U87MG Growth Inhibition Assay 96 h DMSO IC50=0.95 μM 18754654
Sf9 Kinase Assay 30 min DMSO Inhibition of human PI3Kgamma expressed assessed as amount of ATP consumed with IC50 of 0.042 μM 22548342
RAW 264.7 Kinase Assay 90 min DMSO Inhibition of human PI3Kgamma expressed assessed as inhibition of AKT phosphorylation with IC50 of 0.298 μM 22548342
Sf9 Kinase Assay 1 h Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells with IC50 of 0.017 μM 23540645
Sf9 Kinase Assay 1 h Inhibition of GST-fused human recombinant PI3Kdelta expressed 23540645
Sf9 Kinase Assay 1 h Inhibition of GST-fused human recombinant PI3Kgamma expressed 23540645
Sf9 Kinase Assay 1 h Inhibition of GST-fused human recombinant PI3Kalpha expressed 23540645
SKOV3 Kinase Assay 1 μM 1 h DMSO Inhibition of PI3Kalpha assessed as inhibition of Akt Ser473 phosphorylation 23360348
MCF7 Growth Inhibition Assay 1 μM 96 h DMSO GI50=0.0702 μM 23360348
SKOV3 Growth Inhibition Assay 1 μM 96 h DMSO GI50=0.1476 μM 23360348
PC3 Growth Inhibition Assay 72 h DMSO IC50=0.28 μM 21981714
MCF7.1 Growth Inhibition Assay 72 h DMSO Antiproliferative activity against human MCF7.1 cells expressing HER2 gene with IC50 of 0.28 μM 21981714
MCF7-neo/Her2 Growth Inhibition Assay 72 h DMSO IC50=0.29 μM 23662903
MCF7-neo/Her2 Kinase Assay Inhibition of PI3Kalpha assessed as reduction of AKT phosphorylation at S473 with IC50 of 0.007 μM 23662903
PC3 Growth Inhibition Assay 72 h DMSO EC50=0.34 μM 21985639
MCF7.1 Growth Inhibition Assay 72 h DMSO Antiproliferative activity against human MCF7.1 cells expressing PI3Kalpha mutant with EC50 of 0.39 μM 21985639
PC3 Growth Inhibition Assay 72 h DMSO Antiproliferative activity against human PC3 cells deficient in PTEN with IC50 of 0.39 μM 20050669
MCF7.1 Growth Inhibition Assay 72 h DMSO Antiproliferative activity against human MCF7.1 cells expressing PI3Kalpha mutant with IC50 of 0.34 μM 20050669
MCF7.1 Growth Inhibition Assay 72 h EC50=0.72 μM 20346656
NCI-H1975 Cytotoxic Assay 72 h IC50=0.27 μM 23059545
H460 Cytotoxic Assay 72 h IC50=0.87 μM 23059545
HT-29 Cytotoxic Assay 72 h IC50=0.66 μM 23059545
HepG2 Cytotoxic Assay 72 h IC50=1 μM 23059545
SGC7901 Cytotoxic Assay 72 h IC50=1.8 μM 23059545
NCI-H226 Cytotoxic Assay 72 h IC50=2.9 μM 23059545
A549 Cytotoxic Assay 72 h IC50=6.9 μM 23059545
U87MG Cytotoxic Assay 72 h IC50=7.77 μM 23059545
HBC4 Growth Inhibition Assay logGI50=-6.03 M 22336246
BSY1 Growth Inhibition Assay logGI50=-6.90 M 22336246
HBC5 Growth Inhibition Assay logGI50=-6.60 M 22336246
MCF7 Growth Inhibition Assay logGI50=-7.33 M 22336246
MDA-MB-231 Growth Inhibition Assay logGI50=-5.46 M 22336246
U251 Growth Inhibition Assay logGI50=-5.50 M 22336246
SF268 Growth Inhibition Assay logGI50=-5.39 M 22336246
SF295 Growth Inhibition Assay logGI50=-6.37 M 22336246
SF539 Growth Inhibition Assay logGI50=-6.50 M 22336246
SNB75 Growth Inhibition Assay logGI50=-7.10 M 22336246
SNB78 Growth Inhibition Assay logGI50=-6.52 M 22336246
HCC2998 Growth Inhibition Assay logGI50=-6.29 M 22336246
KM12 Growth Inhibition Assay logGI50=-5.76 M 22336246
HT-29 Growth Inhibition Assay logGI50=-6.30 M 22336246
HCT15 Growth Inhibition Assay logGI50=-6.12 M 22336246
HCT116 Growth Inhibition Assay logGI50=-5.87 M 22336246
NCI-H23 Growth Inhibition Assay logGI50=-5.73 M 22336246
NCI-H226 Growth Inhibition Assay logGI50=-6.21 M 22336246
NCI-H522 Growth Inhibition Assay logGI50=-6.58 M 22336246
NCI-H483 Growth Inhibition Assay logGI50=-6.56 M 22336246
A549 Growth Inhibition Assay logGI50=-6.15 M 22336246
DMS273 Growth Inhibition Assay logGI50=-6.43 M 22336246
DMS114 Growth Inhibition Assay logGI50=-5.92 M 22336246
LOXIMVI Growth Inhibition Assay logGI50=-6.29 M 22336246
OVCAR3 Growth Inhibition Assay logGI50=-6.71 M 22336246
OVCAR4 Growth Inhibition Assay logGI50=-5.76 M 22336246
OVCAR5 Growth Inhibition Assay logGI50=-6.26 M 22336246
OVCAR8 Growth Inhibition Assay logGI50=-5.73 M 22336246
SKOV3 Growth Inhibition Assay logGI50=-6.52 M 22336246
RXF631L Growth Inhibition Assay logGI50=-6.88 M 22336246
ACHN Growth Inhibition Assay logGI50=-6.07 M 22336246
St-4 Growth Inhibition Assay logGI50=-5.56 M 22336246
MKN1 Growth Inhibition Assay logGI50=-7.08 M 22336246
MKN7 Growth Inhibition Assay logGI50=-6.50 M 22336246
MKN28 Growth Inhibition Assay logGI50=-5.52 M 22336246
MKN45 Growth Inhibition Assay logGI50=-6.55 M 22336246
MKN74 Growth Inhibition Assay logGI50=-6.02 M 22336246
DU145 Growth Inhibition Assay logGI50=-5.85 M 22336246
PC3 Growth Inhibition Assay logGI50=-6.66 M 22336246
ES5 Growth Inhibition Assay IC50=50.21 nM SANGER
HH Growth Inhibition Assay IC50=111.08 nM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=114.3 nM SANGER
NCI-H1770 Growth Inhibition Assay IC50=123.86 nM SANGER
HuO9 Growth Inhibition Assay IC50=206.02 nM SANGER
HAL-01 Growth Inhibition Assay IC50=206.73 nM SANGER
NOS-1 Growth Inhibition Assay IC50=211.82 nM SANGER
HGC-27 Growth Inhibition Assay IC50=212.57 nM SANGER
NB69 Growth Inhibition Assay IC50=245.27 nM SANGER
RS4-11 Growth Inhibition Assay IC50=261.76 nM SANGER
DOK Growth Inhibition Assay IC50=301.7 nM SANGER
LB2241-RCC Growth Inhibition Assay IC50=303.84 nM SANGER
NCI-H1623 Growth Inhibition Assay IC50=304.08 nM SANGER
YH-13 Growth Inhibition Assay IC50=304.32 nM SANGER
BPH-1 Growth Inhibition Assay IC50=314 nM SANGER
AN3-CA Growth Inhibition Assay IC50=340.37 nM SANGER
ES7 Growth Inhibition Assay IC50=341.99 nM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=352.92 nM SANGER
GAMG Growth Inhibition Assay IC50=370.85 nM SANGER
CHL-1 Growth Inhibition Assay IC50=378.65 nM SANGER
NB7 Growth Inhibition Assay IC50=389.83 nM SANGER
MFE-280 Growth Inhibition Assay IC50=418.2 nM SANGER
HL-60 Growth Inhibition Assay IC50=425.75 nM SANGER
GCIY Growth Inhibition Assay IC50=433.8 nM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=439.13 nM SANGER
LXF-289 Growth Inhibition Assay IC50=448.27 nM SANGER
NBsusSR Growth Inhibition Assay IC50=488.85 nM SANGER
KU-19-19 Growth Inhibition Assay IC50=516.07 nM SANGER
A204 Growth Inhibition Assay IC50=522.33 nM SANGER
LB1047-RCC Growth Inhibition Assay IC50=522.93 nM SANGER
COLO-684 Growth Inhibition Assay IC50=523.11 nM SANGER
PA-1 Growth Inhibition Assay IC50=532.41 nM SANGER
MG-63 Growth Inhibition Assay IC50=541.11 nM SANGER
BHT-101 Growth Inhibition Assay IC50=544.94 nM SANGER
NKM-1 Growth Inhibition Assay IC50=593.09 nM SANGER
T47D Growth Inhibition Assay IC50=597.56 nM SANGER
MOLT-4 Growth Inhibition Assay IC50=623.62 nM SANGER
IGROV-1 Growth Inhibition Assay IC50=634.31 nM SANGER
ES4 Growth Inhibition Assay IC50=639.54 nM SANGER
HuO-3N1 Growth Inhibition Assay IC50=642.38 nM SANGER
NEC8 Growth Inhibition Assay IC50=653.57 nM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=659.17 nM SANGER
EPCL-272H Growth Inhibition Assay IC50=687.21 nM SANGER
D-263MG Growth Inhibition Assay IC50=718.1 nM SANGER
MV-4-11 Growth Inhibition Assay IC50=724.31 nM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=725.94 nM SANGER
SW872 Growth Inhibition Assay IC50=727.89 nM SANGER
P30-OHK Growth Inhibition Assay IC50=730.71 nM SANGER
OMC-1 Growth Inhibition Assay IC50=751.09 nM SANGER
LoVo Growth Inhibition Assay IC50=777.9 nM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=796.34 nM SANGER
L-363 Growth Inhibition Assay IC50=798.42 nM SANGER
ES8 Growth Inhibition Assay IC50=810.52 nM SANGER
697 Growth Inhibition Assay IC50=831.55 nM SANGER
HSC-3 Growth Inhibition Assay IC50=839.54 nM SANGER
H4 Growth Inhibition Assay IC50=850.85 nM SANGER
QIMR-WIL Growth Inhibition Assay IC50=865.2 nM SANGER
OAW-42 Growth Inhibition Assay IC50=872.19 nM SANGER
MCF7 Growth Inhibition Assay IC50=898.59 nM SANGER
SCC-25 Growth Inhibition Assay IC50=914.19 nM SANGER
NCI-H1563 Growth Inhibition Assay IC50=915.99 nM SANGER
OVCAR-5 Growth Inhibition Assay IC50=940.17 nM SANGER
HDLM-2 Growth Inhibition Assay IC50=949.2 nM SANGER
NB5 Growth Inhibition Assay IC50=956.6 nM SANGER
NCI-H292 Growth Inhibition Assay IC50=974.32 nM SANGER
A101D Growth Inhibition Assay IC50=990.19 nM SANGER
NCI-H1648 Growth Inhibition Assay IC50=998.51 nM SANGER
EKVX Growth Inhibition Assay IC50=1.0129 μM SANGER
SW1710 Growth Inhibition Assay IC50=1.04233 μM SANGER
WM-115 Growth Inhibition Assay IC50=1.06656 μM SANGER
CAL-54 Growth Inhibition Assay IC50=1.07081 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=1.08045 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=1.08967 μM SANGER
D-423MG Growth Inhibition Assay IC50=1.09962 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=1.13449 μM SANGER
HT Growth Inhibition Assay IC50=1.13478 μM SANGER
CTB-1 Growth Inhibition Assay IC50=1.14293 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=1.19565 μM SANGER
HuH-7 Growth Inhibition Assay IC50=1.20949 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=1.22177 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=1.29734 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=1.29993 μM SANGER
A498 Growth Inhibition Assay IC50=1.30474 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=1.30679 μM SANGER
AU565 Growth Inhibition Assay IC50=1.31863 μM SANGER
Saos-2 Growth Inhibition Assay IC50=1.33205 μM SANGER
A549 Growth Inhibition Assay IC50=1.3997 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=1.43305 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=1.48692 μM SANGER
639-V Growth Inhibition Assay IC50=1.50245 μM SANGER
A704 Growth Inhibition Assay IC50=1.50785 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=1.51408 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=1.56085 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=1.60746 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=1.60778 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=1.6127 μM SANGER
EFM-19 Growth Inhibition Assay IC50=1.6181 μM SANGER
G-401 Growth Inhibition Assay IC50=1.62164 μM SANGER
D-566MG Growth Inhibition Assay IC50=1.6253 μM SANGER
JVM-3 Growth Inhibition Assay IC50=1.64875 μM SANGER
TK10 Growth Inhibition Assay IC50=1.67083 μM SANGER
BT-20 Growth Inhibition Assay IC50=1.68902 μM SANGER
EGI-1 Growth Inhibition Assay IC50=1.84701 μM SANGER
EW-16 Growth Inhibition Assay IC50=1.85182 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=1.85203 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=1.88692 μM SANGER
G-402 Growth Inhibition Assay IC50=1.89797 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=1.9139 μM SANGER
ME-180 Growth Inhibition Assay IC50=1.93477 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=1.94458 μM SANGER
TYK-nu Growth Inhibition Assay IC50=1.95823 μM SANGER
HOS Growth Inhibition Assay IC50=1.97948 μM SANGER
T98G Growth Inhibition Assay IC50=1.99006 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=2.01332 μM SANGER
SNB75 Growth Inhibition Assay IC50=2.01541 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=2.02689 μM SANGER
CAL-39 Growth Inhibition Assay IC50=2.0328 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=2.04084 μM SANGER
NH-12 Growth Inhibition Assay IC50=2.05424 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=2.1052 μM SANGER
KS-1 Growth Inhibition Assay IC50=2.11001 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=2.13384 μM SANGER
CHP-212 Growth Inhibition Assay IC50=2.18442 μM SANGER
HCC1419 Growth Inhibition Assay IC50=2.21115 μM SANGER
ES1 Growth Inhibition Assay IC50=2.21326 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=2.24123 μM SANGER
EW-22 Growth Inhibition Assay IC50=2.25067 μM SANGER
A431 Growth Inhibition Assay IC50=2.27354 μM SANGER
SF126 Growth Inhibition Assay IC50=2.30625 μM SANGER
SF295 Growth Inhibition Assay IC50=2.31524 μM SANGER
D-502MG Growth Inhibition Assay IC50=2.32461 μM SANGER
HCC2157 Growth Inhibition Assay IC50=2.32927 μM SANGER
D-283MED Growth Inhibition Assay IC50=2.35926 μM SANGER
SNU-423 Growth Inhibition Assay IC50=2.40171 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=2.44586 μM SANGER
22RV1 Growth Inhibition Assay IC50=2.45617 μM SANGER
SW1088 Growth Inhibition Assay IC50=2.49213 μM SANGER
HT-3 Growth Inhibition Assay IC50=2.49259 μM SANGER
NCI-H1666 Growth Inhibition Assay IC50=2.51104 μM SANGER
EM-2 Growth Inhibition Assay IC50=2.51169 μM SANGER
SNU-449 Growth Inhibition Assay IC50=2.57014 μM SANGER
786-0 Growth Inhibition Assay IC50=2.59238 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=2.65939 μM SANGER
MEL-HO Growth Inhibition Assay IC50=2.67634 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=2.69267 μM SANGER
MKN7 Growth Inhibition Assay IC50=2.70754 μM SANGER
5637 Growth Inhibition Assay IC50=2.71035 μM SANGER
HOP-92 Growth Inhibition Assay IC50=2.74717 μM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=2.82023 μM SANGER
NB12 Growth Inhibition Assay IC50=2.84914 μM SANGER
DMS-273 Growth Inhibition Assay IC50=2.8647 μM SANGER
HCC70 Growth Inhibition Assay IC50=2.86589 μM SANGER
YKG-1 Growth Inhibition Assay IC50=3.03787 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=3.05291 μM SANGER
HN Growth Inhibition Assay IC50=3.06636 μM SANGER
HT-1080 Growth Inhibition Assay IC50=3.08606 μM SANGER
HPAF-II Growth Inhibition Assay IC50=3.10068 μM SANGER
U-2-OS Growth Inhibition Assay IC50=3.13782 μM SANGER
SNU-387 Growth Inhibition Assay IC50=3.16364 μM SANGER
Becker Growth Inhibition Assay IC50=3.16808 μM SANGER
BHY Growth Inhibition Assay IC50=3.25571 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=3.29352 μM SANGER
M14 Growth Inhibition Assay IC50=3.30663 μM SANGER
COR-L23 Growth Inhibition Assay IC50=3.37279 μM SANGER
C32 Growth Inhibition Assay IC50=3.41508 μM SANGER
Mewo Growth Inhibition Assay IC50=3.42182 μM SANGER
TE-8 Growth Inhibition Assay IC50=3.48259 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=3.60637 μM SANGER
AGS Growth Inhibition Assay IC50=3.62464 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=3.66138 μM SANGER
Calu-3 Growth Inhibition Assay IC50=3.71287 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=3.71315 μM SANGER
SW962 Growth Inhibition Assay IC50=3.72636 μM SANGER
PC-14 Growth Inhibition Assay IC50=3.73222 μM SANGER
SW1573 Growth Inhibition Assay IC50=3.75348 μM SANGER
769-P Growth Inhibition Assay IC50=3.82743 μM SANGER
KNS-62 Growth Inhibition Assay IC50=3.92338 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=4.05638 μM SANGER
LN-405 Growth Inhibition Assay IC50=4.15728 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=4.22543 μM SANGER
DMS-114 Growth Inhibition Assay IC50=4.23891 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=4.24558 μM SANGER
TCCSUP Growth Inhibition Assay IC50=4.24788 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=4.25332 μM SANGER
HCE-4 Growth Inhibition Assay IC50=4.27197 μM SANGER
DK-MG Growth Inhibition Assay IC50=4.3039 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=4.32584 μM SANGER
A2780 Growth Inhibition Assay IC50=4.36682 μM SANGER
ETK-1 Growth Inhibition Assay IC50=4.37052 μM SANGER
FADU Growth Inhibition Assay IC50=4.37467 μM SANGER
CAL-12T Growth Inhibition Assay IC50=4.41413 μM SANGER
647-V Growth Inhibition Assay IC50=4.44022 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=4.45113 μM SANGER
LU-99A Growth Inhibition Assay IC50=4.4606 μM SANGER
CAL-33 Growth Inhibition Assay IC50=4.52456 μM SANGER
LU-134-A Growth Inhibition Assay IC50=4.52745 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=4.55146 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=4.57002 μM SANGER
TE-1 Growth Inhibition Assay IC50=4.66143 μM SANGER
OE33 Growth Inhibition Assay IC50=4.70511 μM SANGER
CAL-51 Growth Inhibition Assay IC50=4.71082 μM SANGER
SW1783 Growth Inhibition Assay IC50=4.75308 μM SANGER
BT-474 Growth Inhibition Assay IC50=4.76384 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=4.87392 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=4.88557 μM SANGER
IA-LM Growth Inhibition Assay IC50=4.99435 μM SANGER
SW954 Growth Inhibition Assay IC50=4.99443 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=5.05461 μM SANGER
MKN1 Growth Inhibition Assay IC50=5.07927 μM SANGER
A375 Growth Inhibition Assay IC50=5.09256 μM SANGER
8305C Growth Inhibition Assay IC50=5.09887 μM SANGER
CAL-62 Growth Inhibition Assay IC50=5.18259 μM SANGER
NB10 Growth Inhibition Assay IC50=5.22744 μM SANGER
OC-314 Growth Inhibition Assay IC50=5.37444 μM SANGER
PSN1 Growth Inhibition Assay IC50=5.38286 μM SANGER
GR-ST Growth Inhibition Assay IC50=5.38322 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=5.401 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=5.41148 μM SANGER
SCC-4 Growth Inhibition Assay IC50=5.41355 μM SANGER
TE-6 Growth Inhibition Assay IC50=5.41816 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=5.42248 μM SANGER
SW684 Growth Inhibition Assay IC50=5.66385 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=5.68684 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=5.72231 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=5.78251 μM SANGER
PC-3 Growth Inhibition Assay IC50=5.91615 μM SANGER
CAN Growth Inhibition Assay IC50=5.9282 μM SANGER
ESS-1 Growth Inhibition Assay IC50=5.97869 μM SANGER
ATN-1 Growth Inhibition Assay IC50=6.05568 μM SANGER
BxPC-3 Growth Inhibition Assay IC50=6.08219 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=6.12476 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=6.19163 μM SANGER
SW780 Growth Inhibition Assay IC50=6.2042 μM SANGER
A388 Growth Inhibition Assay IC50=6.23115 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=6.24073 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=6.36612 μM SANGER
LS-123 Growth Inhibition Assay IC50=6.40521 μM SANGER
CaR-1 Growth Inhibition Assay IC50=6.46373 μM SANGER
RT-112 Growth Inhibition Assay IC50=6.60338 μM SANGER
CGT Growth Inhibition Assay IC50=6.73681 μM SANGER
SW626 Growth Inhibition Assay IC50=6.73946 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=6.74507 μM SANGER
SBC-5 Growth Inhibition Assay IC50=6.97297 μM SANGER
SF539 Growth Inhibition Assay IC50=6.99333 μM SANGER
TI-73 Growth Inhibition Assay IC50=7.06285 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=7.07762 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=7.08432 μM SANGER
EW-1 Growth Inhibition Assay IC50=7.36996 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=7.39432 μM SANGER
MC-IXC Growth Inhibition Assay IC50=7.41972 μM SANGER
HSC-2 Growth Inhibition Assay IC50=7.42705 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=7.5149 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=7.51711 μM SANGER
HT-1376 Growth Inhibition Assay IC50=7.87778 μM SANGER
EW-13 Growth Inhibition Assay IC50=7.89977 μM SANGER
no-11 Growth Inhibition Assay IC50=7.90174 μM SANGER
Daoy Growth Inhibition Assay IC50=7.94321 μM SANGER
COLO-800 Growth Inhibition Assay IC50=8.04162 μM SANGER
GB-1 Growth Inhibition Assay IC50=8.06565 μM SANGER
SJRH30 Growth Inhibition Assay IC50=8.15878 μM SANGER
NCI-H2291 Growth Inhibition Assay IC50=8.29187 μM SANGER
J82 Growth Inhibition Assay IC50=8.29491 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=8.31453 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=8.34856 μM SANGER
RH-18 Growth Inhibition Assay IC50=8.35046 μM SANGER
SW48 Growth Inhibition Assay IC50=8.59453 μM SANGER
RD Growth Inhibition Assay IC50=8.59391 μM SANGER
MS-1 Growth Inhibition Assay IC50=8.61387 μM SANGER
ES6 Growth Inhibition Assay IC50=8.73119 μM SANGER
TE-12 Growth Inhibition Assay IC50=8.77505 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=8.91217 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=8.92938 μM SANGER
HLE Growth Inhibition Assay IC50=8.93785 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=9.01839 μM SANGER
U-87-MG Growth Inhibition Assay IC50=9.24321 μM SANGER
MN-60 Growth Inhibition Assay IC50=9.24542 μM SANGER
SAS Growth Inhibition Assay IC50=9.25581 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=9.361 μM SANGER
C-33-A Growth Inhibition Assay IC50=9.43988 μM SANGER
RXF393 Growth Inhibition Assay IC50=9.47002 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=9.49384 μM SANGER
RCM-1 Growth Inhibition Assay IC50=9.63801 μM SANGER
SN12C Growth Inhibition Assay IC50=9.65338 μM SANGER
KLE Growth Inhibition Assay IC50=9.70009 μM SANGER
EFO-21 Growth Inhibition Assay IC50=9.77382 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=9.88011 μM SANGER
D-247MG Growth Inhibition Assay IC50=10.0568 μM SANGER
MPP-89 Growth Inhibition Assay IC50=10.0946 μM SANGER
RVH-421 Growth Inhibition Assay IC50=10.1505 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=10.2806 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=10.3532 μM SANGER
DEL Growth Inhibition Assay IC50=10.3794 μM SANGER
HT55 Growth Inhibition Assay IC50=10.6205 μM SANGER
MC116 Growth Inhibition Assay IC50=10.6655 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=10.669 μM SANGER
DJM-1 Growth Inhibition Assay IC50=10.6949 μM SANGER
ZR-75-30 Growth Inhibition Assay IC50=10.9441 μM SANGER
U-118-MG Growth Inhibition Assay IC50=10.9896 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=11.0716 μM SANGER
SW837 Growth Inhibition Assay IC50=11.0949 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=11.1281 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=11.135 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=11.1493 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=11.3794 μM SANGER
HEC-1 Growth Inhibition Assay IC50=11.4328 μM SANGER
DU-4475 Growth Inhibition Assay IC50=11.7393 μM SANGER
DSH1 Growth Inhibition Assay IC50=11.7606 μM SANGER
HCC1569 Growth Inhibition Assay IC50=11.7678 μM SANGER
HCC1187 Growth Inhibition Assay IC50=11.8588 μM SANGER
EW-11 Growth Inhibition Assay IC50=11.9474 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=12.059 μM SANGER
KALS-1 Growth Inhibition Assay IC50=12.8553 μM SANGER
8505C Growth Inhibition Assay IC50=12.885 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=13.0453 μM SANGER
CHP-134 Growth Inhibition Assay IC50=13.1158 μM SANGER
HCE-T Growth Inhibition Assay IC50=13.2364 μM SANGER
LB-831-BLC Growth Inhibition Assay IC50=13.6246 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=13.6524 μM SANGER
SW756 Growth Inhibition Assay IC50=13.7246 μM SANGER
OCUB-M Growth Inhibition Assay IC50=13.8156 μM SANGER
SW982 Growth Inhibition Assay IC50=13.8276 μM SANGER
DB Growth Inhibition Assay IC50=13.8384 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=13.9139 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=14.0015 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=14.0132 μM SANGER
GI-1 Growth Inhibition Assay IC50=14.0658 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=14.6054 μM SANGER
TE-5 Growth Inhibition Assay IC50=14.7208 μM SANGER
EFO-27 Growth Inhibition Assay IC50=14.7622 μM SANGER
CAL-72 Growth Inhibition Assay IC50=14.7783 μM SANGER
GP5d Growth Inhibition Assay IC50=15.0474 μM SANGER
CAS-1 Growth Inhibition Assay IC50=15.066 μM SANGER
A2058 Growth Inhibition Assay IC50=15.5638 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=15.6859 μM SANGER
Detroit562 Growth Inhibition Assay IC50=15.9139 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=16.0821 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=16.1125 μM SANGER
GT3TKB Growth Inhibition Assay IC50=16.1981 μM SANGER
KM-H2 Growth Inhibition Assay IC50=16.3646 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=16.4422 μM SANGER
SF268 Growth Inhibition Assay IC50=16.452 μM SANGER
OE19 Growth Inhibition Assay IC50=16.524 μM SANGER
MLMA Growth Inhibition Assay IC50=16.5571 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=16.7136 μM SANGER
TGW Growth Inhibition Assay IC50=16.8102 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=17.0003 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=17.0237 μM SANGER
A427 Growth Inhibition Assay IC50=17.2334 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=17.3213 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=17.3897 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=17.9182 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=18.1581 μM SANGER
HCC1395 Growth Inhibition Assay IC50=18.5611 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=18.6584 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=18.669 μM SANGER
RMG-I Growth Inhibition Assay IC50=18.7382 μM SANGER
LS-513 Growth Inhibition Assay IC50=18.9228 μM SANGER
MFM-223 Growth Inhibition Assay IC50=19.0716 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=19.3295 μM SANGER
KP-4 Growth Inhibition Assay IC50=19.8531 μM SANGER
NB13 Growth Inhibition Assay IC50=19.8839 μM SANGER
UACC-893 Growth Inhibition Assay IC50=19.9757 μM SANGER
HT-1197 Growth Inhibition Assay IC50=20.2958 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=20.3266 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=20.3373 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=20.5822 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=21.3696 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=21.6722 μM SANGER
SCH Growth Inhibition Assay IC50=22.496 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=23.3887 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=23.9241 μM SANGER
ACHN Growth Inhibition Assay IC50=24.4656 μM SANGER
M059J Growth Inhibition Assay IC50=24.5634 μM SANGER
AM-38 Growth Inhibition Assay IC50=25.481 μM SANGER
KG-1 Growth Inhibition Assay IC50=25.5494 μM SANGER
COLO-824 Growth Inhibition Assay IC50=25.5599 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=25.5847 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=25.7465 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=26.3027 μM SANGER
JEG-3 Growth Inhibition Assay IC50=26.6805 μM SANGER
RKO Growth Inhibition Assay IC50=26.7632 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=27.2118 μM SANGER
CAL-120 Growth Inhibition Assay IC50=27.6914 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=27.7716 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=27.7833 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=27.9862 μM SANGER
S-117 Growth Inhibition Assay IC50=29.3857 μM SANGER
SW13 Growth Inhibition Assay IC50=29.8519 μM SANGER
ES3 Growth Inhibition Assay IC50=30.3733 μM SANGER
HCT-116 Growth Inhibition Assay IC50=30.5554 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=30.5942 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=30.6413 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=31.5784 μM SANGER
ALL-PO Growth Inhibition Assay IC50=31.8428 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=32.0623 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=32.4837 μM SANGER
FTC-133 Growth Inhibition Assay IC50=32.706 μM SANGER
COLO-829 Growth Inhibition Assay IC50=33.3467 μM SANGER
GOTO Growth Inhibition Assay IC50=33.5258 μM SANGER
YAPC Growth Inhibition Assay IC50=33.8159 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=34.1624 μM SANGER
SiHa Growth Inhibition Assay IC50=34.3817 μM SANGER
LK-2 Growth Inhibition Assay IC50=34.5708 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=34.7202 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=35.179 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=35.663 μM SANGER
SCC-9 Growth Inhibition Assay IC50=36.7146 μM SANGER
SH-4 Growth Inhibition Assay IC50=36.73 μM SANGER
HCC-1954 Growth Inhibition Assay IC50=37.2729 μM SANGER
BALL-1 Growth Inhibition Assay IC50=37.5316 μM SANGER
BE-13 Growth Inhibition Assay IC50=37.7018 μM SANGER
COLO-678 Growth Inhibition Assay IC50=37.9437 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=38.2397 μM SANGER
OAW-28 Growth Inhibition Assay IC50=38.639 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=38.9691 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=39.818 μM SANGER
A3-KAW Growth Inhibition Assay IC50=40.3661 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=40.5931 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=40.7165 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=41.1536 μM SANGER
CFPAC-1 Growth Inhibition Assay IC50=42.5211 μM SANGER
NB14 Growth Inhibition Assay IC50=42.7027 μM SANGER
COLO-792 Growth Inhibition Assay IC50=42.8961 μM SANGER
RH-1 Growth Inhibition Assay IC50=43.4836 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=44.3568 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=44.8114 μM SANGER
KGN Growth Inhibition Assay IC50=48.3063 μM SANGER
UACC-62 Growth Inhibition Assay IC50=48.4072 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=49.3018 μM SANGER
LS-411N Growth Inhibition Assay IC50=49.3118 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=49.5625 μM SANGER
Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen

Chemische Informationen, Lagerung & Stabilität

Molekulargewicht 513.64 Formel

C23H27N7O3S2

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 957054-30-7 SDF herunterladen Lagerung von Stammlösungen

Synonyme RG7321 Smiles CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6

Löslichkeit

In vitro
Charge:

DMSO : 100 mg/mL (194.68 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus

Targets/IC50/Ki
p110α
(Cell-free assay)
3 nM
p110δ
(Cell-free assay)
3 nM
p110β
(Cell-free assay)
33 nM
p110γ
(Cell-free assay)
75 nM
mTOR
(Cell-free assay)
0.58 μM(Ki app)
In vitro

Pictilisib (GDC-0941) ist gleich wirksam gegen PI3Kα und PI3Kδ sowie gegen PI3Kα-Mutanten E545-K und H1047-R und zeigt eine moderate Selektivität gegenüber PI3Kβ (10-fach) und PI3Kγ (25-fach) sowie eine höhere Selektivität gegenüber Mitgliedern der PI3K-Klasse II, III und IV, einschließlich C2β, Vps34, DNA-PK und mTOR. Es hemmt potent die Phosphorylierung von Akt in U87MG-, PC3- und MDA-MB-361-Zellen mit einer IC50 von 46 nM, 37 nM bzw. 28 nM. Diese Verbindung hemmt die Proliferation von U87MG-, A2780-, PC3- und MDA-MB-361-Zellen mit einer IC50 von 0,95 μM, 0,14 μM, 0,28 μM bzw. 0,72 μM.  Es hemmt die Proliferation von HER2-amplifizierten Zellen, die PIK3CA-Mutationen aufweisen, mit einer IC50 von <500 nM und hemmt effektiv sowohl die Proliferation als auch die Viabilität von HER2-amplifizierten Brustkrebszellen. Es hemmt signifikant das Wachstum von HCT116-, DLD1- und HT29-Zellen mit einer GI50 von 1081 nM, 1070 nM bzw. 157 nM. Es hemmt auch die Proliferation von Tumorzellen, induziert Apoptose und unterdrückt die Keimzellpopulation.

Kinase-Assay
Szintillationsnäherungsassay
Rekombinante humane PI3Kα, PI3Kβ und PI3Kδ werden in einem Sf9-Baculovirus-System mit der p85α-regulatorischen Untereinheit coexprimiert und als GST-Fusionsproteine mittels Affinitätschromatographie gereinigt. Rekombinante humane PI3Kγ wird als monomeres GST-Fusionsexprimiert und ähnlich gereinigt. Pictilisib (GDC-0941) wird in DMSO gelöst und zu 20 mM Tris-HCl (pH 7,5) gegeben, das 200 μg Yttriumsilicat (Ysi) Polylysin-SPA-Beads, 4 mM MgCl2, 1 mM Dithiothreitol (DTT), 1 μM ATP, 0,125 μCi [γ-33P]-ATP und 4% (v/v) DMSO in einem Gesamtvolumen von 50 μL enthält. Die rekombinante GST-Fusion von PI3Kα (5 ng), PI3Kβ (5 ng), PI3Kδ (5 ng) oder PI3Kγ (5 ng) wird der Assay-Mischung zugesetzt, um die Kinase-Reaktion zu initiieren. Nach einstündiger Inkubation bei Raumtemperatur wird die Kinase-Reaktion mit 150 μL PBS beendet. Die Mischung wird dann 2 Minuten lang bei 2000 U/min zentrifugiert und mit einem Wallac Microbeta-Zähler ausgelesen. Die angegebenen IC50-Werte werden unter Verwendung einer sigmoidalen Dosis-Wirkungs-Kurvenanpassung in MDL Assay Explorer berechnet.
In vivo

Pictilisib (GDC-0941) zeigt einen begrenzten mikrosomalen Metabolismus, was zu einer oralen Bioverfügbarkeit von 78% führt . Die Verabreichung dieser Verbindung in einer Dosis von 75 mg/kg/Tag zeigt eine signifikante hemmende Wirkung gegen etablierte humane U87MG-Glioblastom-Xenotransplantate in weiblichen NCr-athymischen Mäusen, mit einer Tumorwachstumshemmung von 83%. Die orale Verabreichung von 150 mg/kg/Tag hemmt das Wachstum von HER2-amplifizierten MDA-MB-361.1-Xenotransplantaten in Mäusen und verzögert signifikant die Tumorprogression, verbunden mit einer potent induzierten Apoptose in Tumoren. Die Behandlung damit (75 mg/kg/Tag) über 2 Wochen führt zu einer Reduktion des Tumorvolumens von spontanen B-Zell-Follikulären Lymphomen, die sich in PTEN+/-LKB1+/hypo-Mäusen entwickeln, um ca. 40%, begleitet von einer Ablation der Phosphorylierung von Akt-, S6K- und SGK-Proteinkinasen (Serum- und Glukokortikoid-Proteinkinase).

Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/21407213/
  • [5] https://pubmed.ncbi.nlm.nih.gov/19584227/

Anwendungen

Methoden Biomarker Bilder PMID
Western blot p-AKT / AKT / p-FoxO3a / FoxO3a / PUMA p-S6RP / S6RP p-4EBP1 / 4EBP1 p-LRP6 / LRP6 p-PAK / PAK1 / p-CRAF / RAF / p-MEK / MEK / p-ERK / ERK
S1065-WB1
29137323
Immunofluorescence p65 beta-catenin
S1065-IF1
30042442
Growth inhibition assay Cell viability
S1065-viability1
27117832

Klinische Studieninformationen

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
NCT02092831 Completed
Healthy Volunteer
Genentech Inc.
 April 2014 Phase 1
NCT01740336 Completed
Breast Cancer
Genentech Inc.
 February 6 2013 Phase 2
NCT01474668 Completed
Healthy Volunteer
Genentech Inc.
 October 2011 Phase 1
NCT01240226 Completed
Healthy Volunteer
Genentech Inc.
 November 2010 Phase 1

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