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Pictilisib (GDC-0941)

別名: RG7321

Pictilisib (GDC-0941, RG7321) 是一種有效的PI3Kα/δ抑制劑，在無細(xì)胞試驗中IC50為 3 nM，對p110β (11倍)和p110γ (25倍)具有適度的選擇性。Pictilisib (GDC-0941) 可誘導(dǎo)自噬和凋亡。Phase 2。

Pictilisib (GDC-0941) Chemical Structure

Pictilisib (GDC-0941) Chemical Structure

CAS: 957054-30-7

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1203.93 現(xiàn)貨
5mg 986.88 現(xiàn)貨
50mg 3026.17 現(xiàn)貨
200mg 7926.11 現(xiàn)貨
1g 24488.1 現(xiàn)貨
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400-668-6834

info@selleck.cn
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Pictilisib (GDC-0941)相關(guān)產(chǎn)品

相關(guān)信號通路圖

PI3K Signaling Pathways

PI3K信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
SKOV3 Growth Inhibition Assay 1 μM 96 h GI50=0.1476 μM 23360348
MCF7 Growth Inhibition Assay 1 μM 96 h GI50=0.0702 μM 23360348
SKOV3 Kinase Assay 1 μM 1 h Inhibition of PI3Kalpha assessed as inhibition of Akt Ser473 phosphorylation 23360348
U87MG Cytotoxic Assay 72 h IC50=7.77 μM 23059545
A549 Cytotoxic Assay 72 h IC50=6.9 μM 23059545
NCI-H226 Cytotoxic Assay 72 h IC50=2.9 μM 23059545
SGC7901 Cytotoxic Assay 72 h IC50=1.8 μM 23059545
HepG2 Cytotoxic Assay 72 h IC50=1 μM 23059545
HT-29 Cytotoxic Assay 72 h IC50=0.66 μM 23059545
H460 Cytotoxic Assay 72 h IC50=0.87 μM 23059545
NCI-H1975 Cytotoxic Assay 72 h IC50=0.27 μM 23059545
MCF7.1 Growth Inhibition Assay 72 h EC50=0.72 μM 20346656
MCF7.1 Growth Inhibition Assay 72 h Antiproliferative activity against human MCF7.1 cells expressing PI3Kalpha mutant with IC50 of 0.34 μM 20050669
PC3 Growth Inhibition Assay 72 h Antiproliferative activity against human PC3 cells deficient in PTEN with IC50 of 0.39 μM 20050669
MCF7.1 Growth Inhibition Assay 72 h Antiproliferative activity against human MCF7.1 cells expressing PI3Kalpha mutant with EC50 of 0.39 μM 21985639
PC3 Growth Inhibition Assay 72 h EC50=0.34 μM 21985639
MCF7-neo/Her2 Growth Inhibition Assay 72 h IC50=0.29 μM 23662903
MCF7.1 Growth Inhibition Assay 72 h Antiproliferative activity against human MCF7.1 cells expressing HER2 gene with IC50 of 0.28 μM 21981714
PC3 Growth Inhibition Assay 72 h IC50=0.28 μM 21981714
Sf9 Kinase Assay 1 h Inhibition of GST-fused human recombinant PI3Kalpha 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 PI3Kdelta expressed 23540645
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
RAW 264.7 Kinase Assay 90 min Inhibition of human PI3Kgamma expressed assessed as inhibition of AKT phosphorylation with IC50 of 0.298 μM 22548342
Sf9 Kinase Assay 30 min Inhibition of human PI3Kgamma expressed assessed as amount of ATP consumed with IC50 of 0.042 μM 22548342
U87MG Growth Inhibition Assay 96 h IC50=0.95 μM 18754654
PC3 Growth Inhibition Assay 96 h IC50=0.28 μM 18754654
A2780 Growth Inhibition Assay 96 h Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation with IC50 of 0.14 μM 18754654
MDA-MB-361 Growth Inhibition Assay 96 h Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation with IC50 of 0.72 μM 18754654
U87MG Function Assay 2 h Inhibition of Akt Ser473 phosphorylation in PTEN-null human U87MG cells with IC50 of 0.046 μM 18754654
PC3 Function Assay 2 h Inhibition of Akt Ser473 phosphorylation in PTEN-null human PC3 cells with IC50 of 0.037 μM 18754654
MDA-MB-361 Function Assay 2 h Inhibition of Akt Ser473 phosphorylation in human MDA-MB-361 cells with PIK3CA E545-K mutation with IC50 of 0.028 μM 18754654
Sf9 Kinase Assay 1 h Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha 18754654
Sf9 Kinase Assay 1 h Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.033 μM 18754654
Sf9 Kinase Assay 1 h 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 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 Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM 18754654
HCC2157 Growth Inhibition Assay IC50=2.32927 μM SANGER
D-502MG Growth Inhibition Assay IC50=2.32461 μM SANGER
SF295 Growth Inhibition Assay IC50=2.31524 μM SANGER
SF126 Growth Inhibition Assay IC50=2.30625 μM SANGER
A431 Growth Inhibition Assay IC50=2.27354 μM SANGER
EW-22 Growth Inhibition Assay IC50=2.25067 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=2.24123 μM SANGER
ES1 Growth Inhibition Assay IC50=2.21326 μM SANGER
HCC1419 Growth Inhibition Assay IC50=2.21115 μM SANGER
CHP-212 Growth Inhibition Assay IC50=2.18442 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=2.13384 μM SANGER
KS-1 Growth Inhibition Assay IC50=2.11001 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=2.1052 μM SANGER
NH-12 Growth Inhibition Assay IC50=2.05424 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=2.04084 μM SANGER
CAL-39 Growth Inhibition Assay IC50=2.0328 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=2.02689 μM SANGER
SNB75 Growth Inhibition Assay IC50=2.01541 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=2.01332 μM SANGER
T98G Growth Inhibition Assay IC50=1.99006 μM SANGER
HOS Growth Inhibition Assay IC50=1.97948 μM SANGER
TYK-nu Growth Inhibition Assay IC50=1.95823 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=1.94458 μM SANGER
ME-180 Growth Inhibition Assay IC50=1.93477 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=1.9139 μM SANGER
G-402 Growth Inhibition Assay IC50=1.89797 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=1.88692 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=1.85203 μM SANGER
EW-16 Growth Inhibition Assay IC50=1.85182 μM SANGER
EGI-1 Growth Inhibition Assay IC50=1.84701 μM SANGER
BT-20 Growth Inhibition Assay IC50=1.68902 μM SANGER
TK10 Growth Inhibition Assay IC50=1.67083 μM SANGER
JVM-3 Growth Inhibition Assay IC50=1.64875 μM SANGER
D-566MG Growth Inhibition Assay IC50=1.6253 μM SANGER
G-401 Growth Inhibition Assay IC50=1.62164 μM SANGER
EFM-19 Growth Inhibition Assay IC50=1.6181 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=1.6127 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=1.60778 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=1.60746 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=1.56085 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=1.51408 μM SANGER
A704 Growth Inhibition Assay IC50=1.50785 μM SANGER
639-V Growth Inhibition Assay IC50=1.50245 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=1.48692 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=1.43305 μM SANGER
A549 Growth Inhibition Assay IC50=1.3997 μM SANGER
Saos-2 Growth Inhibition Assay IC50=1.33205 μM SANGER
AU565 Growth Inhibition Assay IC50=1.31863 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=1.30679 μM SANGER
A498 Growth Inhibition Assay IC50=1.30474 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=1.29993 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=1.29734 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=1.22177 μM SANGER
HuH-7 Growth Inhibition Assay IC50=1.20949 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=1.19565 μM SANGER
CTB-1 Growth Inhibition Assay IC50=1.14293 μM SANGER
HT Growth Inhibition Assay IC50=1.13478 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=1.13449 μM SANGER
D-423MG Growth Inhibition Assay IC50=1.09962 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=1.08967 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=1.08045 μM SANGER
CAL-54 Growth Inhibition Assay IC50=1.07081 μM SANGER
WM-115 Growth Inhibition Assay IC50=1.06656 μM SANGER
SW1710 Growth Inhibition Assay IC50=1.04233 μM SANGER
EKVX Growth Inhibition Assay IC50=1.0129 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=998.51 nM SANGER
A101D Growth Inhibition Assay IC50=990.19 nM SANGER
NCI-H292 Growth Inhibition Assay IC50=974.32 nM SANGER
NB5 Growth Inhibition Assay IC50=956.6 nM SANGER
HDLM-2 Growth Inhibition Assay IC50=949.2 nM SANGER
OVCAR-5 Growth Inhibition Assay IC50=940.17 nM SANGER
NCI-H1563 Growth Inhibition Assay IC50=915.99 nM SANGER
SCC-25 Growth Inhibition Assay IC50=914.19 nM SANGER
MCF7 Growth Inhibition Assay IC50=898.59 nM SANGER
OAW-42 Growth Inhibition Assay IC50=872.19 nM SANGER
QIMR-WIL Growth Inhibition Assay IC50=865.2 nM SANGER
H4 Growth Inhibition Assay IC50=850.85 nM SANGER
HSC-3 Growth Inhibition Assay IC50=839.54 nM SANGER
697 Growth Inhibition Assay IC50=831.55 nM SANGER
ES8 Growth Inhibition Assay IC50=810.52 nM SANGER
L-363 Growth Inhibition Assay IC50=798.42 nM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=796.34 nM SANGER
LoVo Growth Inhibition Assay IC50=777.9 nM SANGER
OMC-1 Growth Inhibition Assay IC50=751.09 nM SANGER
P30-OHK Growth Inhibition Assay IC50=730.71 nM SANGER
SW872 Growth Inhibition Assay IC50=727.89 nM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=725.94 nM SANGER
MV-4-11 Growth Inhibition Assay IC50=724.31 nM SANGER
D-263MG Growth Inhibition Assay IC50=718.1 nM SANGER
EPCL-272H Growth Inhibition Assay IC50=687.21 nM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=659.17 nM SANGER
NEC8 Growth Inhibition Assay IC50=653.57 nM SANGER
HuO-3N1 Growth Inhibition Assay IC50=642.38 nM SANGER
ES4 Growth Inhibition Assay IC50=639.54 nM SANGER
IGROV-1 Growth Inhibition Assay IC50=634.31 nM SANGER
MOLT-4 Growth Inhibition Assay IC50=623.62 nM SANGER
T47D Growth Inhibition Assay IC50=597.56 nM SANGER
NKM-1 Growth Inhibition Assay IC50=593.09 nM SANGER
BHT-101 Growth Inhibition Assay IC50=544.94 nM SANGER
MG-63 Growth Inhibition Assay IC50=541.11 nM SANGER
PA-1 Growth Inhibition Assay IC50=532.41 nM SANGER
COLO-684 Growth Inhibition Assay IC50=523.11 nM SANGER
LB1047-RCC Growth Inhibition Assay IC50=522.93 nM SANGER
A204 Growth Inhibition Assay IC50=522.33 nM SANGER
KU-19-19 Growth Inhibition Assay IC50=516.07 nM SANGER
NBsusSR Growth Inhibition Assay IC50=488.85 nM SANGER
LXF-289 Growth Inhibition Assay IC50=448.27 nM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=439.13 nM SANGER
GCIY Growth Inhibition Assay IC50=433.8 nM SANGER
HL-60 Growth Inhibition Assay IC50=425.75 nM SANGER
MFE-280 Growth Inhibition Assay IC50=418.2 nM SANGER
NB7 Growth Inhibition Assay IC50=389.83 nM SANGER
CHL-1 Growth Inhibition Assay IC50=378.65 nM SANGER
GAMG Growth Inhibition Assay IC50=370.85 nM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=352.92 nM SANGER
ES7 Growth Inhibition Assay IC50=341.99 nM SANGER
AN3-CA Growth Inhibition Assay IC50=340.37 nM SANGER
BPH-1 Growth Inhibition Assay IC50=314 nM SANGER
YH-13 Growth Inhibition Assay IC50=304.32 nM SANGER
NCI-H1623 Growth Inhibition Assay IC50=304.08 nM SANGER
LB2241-RCC Growth Inhibition Assay IC50=303.84 nM SANGER
DOK Growth Inhibition Assay IC50=301.7 nM SANGER
RS4-11 Growth Inhibition Assay IC50=261.76 nM SANGER
NB69 Growth Inhibition Assay IC50=245.27 nM SANGER
HGC-27 Growth Inhibition Assay IC50=212.57 nM SANGER
NOS-1 Growth Inhibition Assay IC50=211.82 nM SANGER
HAL-01 Growth Inhibition Assay IC50=206.73 nM SANGER
HuO9 Growth Inhibition Assay IC50=206.02 nM SANGER
NCI-H1770 Growth Inhibition Assay IC50=123.86 nM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=114.3 nM SANGER
HH Growth Inhibition Assay IC50=111.08 nM SANGER
ES5 Growth Inhibition Assay IC50=50.21 nM SANGER
PC3 Growth Inhibition Assay logGI50=-6.66 M 22336246
DU145 Growth Inhibition Assay logGI50=-5.85 M 22336246
MKN74 Growth Inhibition Assay logGI50=-6.02 M 22336246
MKN45 Growth Inhibition Assay logGI50=-6.55 M 22336246
MKN28 Growth Inhibition Assay logGI50=-5.52 M 22336246
MKN7 Growth Inhibition Assay logGI50=-6.50 M 22336246
MKN1 Growth Inhibition Assay logGI50=-7.08 M 22336246
St-4 Growth Inhibition Assay logGI50=-5.56 M 22336246
ACHN Growth Inhibition Assay logGI50=-6.07 M 22336246
RXF631L Growth Inhibition Assay logGI50=-6.88 M 22336246
SKOV3 Growth Inhibition Assay logGI50=-6.52 M 22336246
OVCAR8 Growth Inhibition Assay logGI50=-5.73 M 22336246
OVCAR5 Growth Inhibition Assay logGI50=-6.26 M 22336246
OVCAR4 Growth Inhibition Assay logGI50=-5.76 M 22336246
OVCAR3 Growth Inhibition Assay logGI50=-6.71 M 22336246
LOXIMVI Growth Inhibition Assay logGI50=-6.29 M 22336246
DMS114 Growth Inhibition Assay logGI50=-5.92 M 22336246
DMS273 Growth Inhibition Assay logGI50=-6.43 M 22336246
A549 Growth Inhibition Assay logGI50=-6.15 M 22336246
NCI-H483 Growth Inhibition Assay logGI50=-6.56 M 22336246
NCI-H522 Growth Inhibition Assay logGI50=-6.58 M 22336246
NCI-H226 Growth Inhibition Assay logGI50=-6.21 M 22336246
NCI-H23 Growth Inhibition Assay logGI50=-5.73 M 22336246
HCT116 Growth Inhibition Assay logGI50=-5.87 M 22336246
HCT15 Growth Inhibition Assay logGI50=-6.12 M 22336246
HT-29 Growth Inhibition Assay logGI50=-6.30 M 22336246
KM12 Growth Inhibition Assay logGI50=-5.76 M 22336246
HCC2998 Growth Inhibition Assay logGI50=-6.29 M 22336246
SNB78 Growth Inhibition Assay logGI50=-6.52 M 22336246
SNB75 Growth Inhibition Assay logGI50=-7.10 M 22336246
SF539 Growth Inhibition Assay logGI50=-6.50 M 22336246
SF295 Growth Inhibition Assay logGI50=-6.37 M 22336246
SF268 Growth Inhibition Assay logGI50=-5.39 M 22336246
U251 Growth Inhibition Assay logGI50=-5.50 M 22336246
MDA-MB-231 Growth Inhibition Assay logGI50=-5.46 M 22336246
MCF7 Growth Inhibition Assay logGI50=-7.33 M 22336246
HBC5 Growth Inhibition Assay logGI50=-6.60 M 22336246
BSY1 Growth Inhibition Assay logGI50=-6.90 M 22336246
HBC4 Growth Inhibition Assay logGI50=-6.03 M 22336246
MCF7-neo/Her2 Kinase Assay Inhibition of PI3Kalpha assessed as reduction of AKT phosphorylation at S473 with IC50 of 0.007 μM 23662903
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
點擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述 Pictilisib (GDC-0941, RG7321) 是一種有效的PI3Kα/δ抑制劑，在無細(xì)胞試驗中IC50為 3 nM，對p110β (11倍)和p110γ (25倍)具有適度的選擇性。Pictilisib (GDC-0941) 可誘導(dǎo)自噬和凋亡。Phase 2。
靶點
p110α [1]
(Cell-free assay)		 p110δ [1]
(Cell-free assay)		 p110β [1]
(Cell-free assay)		 p110γ [1]
(Cell-free assay)		 mTOR [1]
(Cell-free assay)
3 nM 3 nM 33 nM 75 nM 0.58 μM(Ki app)
體外研究(In Vitro)
體外研究活性

GDC-0941也等效作用于PI3Kα和 PI3Kδ和PI3Kα突變型E545-K和H1047-R,也選擇性作用于PI3Kβ(10倍)和 PI3Kγ(25倍), 選擇性更高地作用于PI3K II, III, 和IV類成員，包括, C2β, Vps34, DNA-PK和mTOR。GDC-0941 作用于U87MG, PC3, 和 MDA-MB-361 細(xì)胞，有效抑制Akt磷酸化，IC50分別為46 nM, 37 nM,和 28 nM。GDC-0941抑制U87MG, A2780, PC3, 和MDA-MB-361細(xì)胞增殖，IC50分別為 0.95 μM, 0.14 μM, 0.28 μM, 和0.72 μM。[1]GDC-0941抑制含PIK3CA突變的HER2擴(kuò)增的細(xì)胞增殖，IC50<500 nM, 且有效抑制HER2 擴(kuò)增乳腺癌細(xì)胞增殖和活力。[2]GDC-0941 顯著抑制HCT116, DLD1和 HT29細(xì)胞生長，GI50分別為1081 nM, 1070 nM 和157 nM。[4]
激酶實驗 閃爍接近檢測
使用p85α調(diào)節(jié)亞基，使重組人PI3Kα, PI3Kβ, 和PI3Kδ在 Sf9 桿狀病毒系統(tǒng)中共表達(dá)，在谷胱甘肽-瓊脂糖凝膠上進(jìn)行親和層析而純化GST-融合蛋白。重組人 PI3Kγ表達(dá)作為單體 GST融合，也想上述相似方法純化。GDC-0941 溶于DMSO，加到含200 μg硅酸釔(Ysi) 聚賴氨酸SPA 磁珠, 4 mM MgCl2, 1 mM 二硫蘇糖醇 (DTT), 1 μM ATP, 0.125 μCi [γ-33P]-ATP, 和4% (v/v) DMSO的20 mM Tris-HCl (pH 7.5)上，總體積為 50 μL。PI3Kα (5 ng), PI3Kβ(5 ng), PI3Kδ(5 ng), 或PI3Kγ(5 ng)的重組GST-融合 ，加到實驗混合物中，開始激酶反應(yīng)。在室溫下溫育1小時后, 加入150 μL PBS終止反應(yīng)。混合物在2000 rpm 轉(zhuǎn)速下離心2分鐘，然后使用Wallac Microbeta計數(shù)器讀數(shù)。在 MDL Assay Explorer系統(tǒng)中使用S型，劑量-反應(yīng)曲線，計算進(jìn)行至少2次獨立重復(fù)實驗，取平均值，作為IC50值。
細(xì)胞實驗 細(xì)胞系 SKBR-3, BT474-M1, AU-565, HCC-1419, ZR75-30, KPL-4, JIMT-1, BT474-EEI, HCC-1954, MCF-7, CALU-3, SKOV-3, 和MKN-7
濃度 溶于DMSO,終濃度為~10 μM
孵育時間 48,和72小時
方法

使用不同濃度 GDC-0941處理細(xì)胞48,和 72小時。通過CellTiter-Glo Luminescent細(xì)胞活性檢測實驗測定細(xì)胞增殖/活力。通過Western Blot分析pAKT (Ser473), cleaved caspase-3, 和cleaved PARP通過 Caspase-Glo 3/7實驗和細(xì)胞死亡檢測 ELISAplus 實驗分別測定caspase 3/7活性, 和凋亡。
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 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 29137323
Immunofluorescence p65 beta-catenin 30042442
Growth inhibition assay Cell viability 27117832
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

在微粒體中，GDC-0941僅有有限的代謝，其口服生物利用度為78%[5]。GDC-0941 每天按 75 mg/kg劑量處理攜帶人U87MG 惡性膠質(zhì)移植瘤的雌性NCr無胸腺小鼠，顯著抑制生長，腫瘤生長抑制率為 83%。[1]GDC-0941 每天按 150 mg/kg劑量口服處理攜帶HER2擴(kuò)增的MDA-MB-361.1移植瘤 的小鼠，抑制腫瘤生長，且顯著延遲腫瘤衰退，與腫瘤中強(qiáng)誘導(dǎo)型凋亡相關(guān)。[2] GDC-0941 每天按75 mg/kg劑量處理攜帶自發(fā)性B細(xì)胞濾泡性淋巴瘤的PTEN+/-LKB1+/hypo小鼠，持續(xù)2周，誘導(dǎo)腫瘤體積下降~40%，伴隨著AKT, S6K 和SGK(血清和糖皮質(zhì)激素蛋白激酶)蛋白激酶的磷酸化被切除。GDC-0941抑制腫瘤細(xì)胞增殖，誘導(dǎo)凋亡和抑制中心母細(xì)胞數(shù)。[3]
動物實驗 Animal Models 移植MDA-MB-361.1細(xì)胞的NCR裸鼠, 皮下移植BT474-M1 細(xì)胞的SCID, C.B-17/IcrHsd-Prkdcscid 小鼠
Dosages ~150 mg/kg/day
Administration 口服飼喂
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

化學(xué)信息&溶解度

分子量 513.64 分子式

C23H27N7O3S2
CAS號 957054-30-7 SDF Download Pictilisib (GDC-0941) SDF
Smiles CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (194.68 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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