Akti-1/2

别名: Akt Inhibitor VIII

Akti-1/2 (Akt Inhibitor VIII)是高度选择性的Akt1/Akt2抑制剂,IC50分别为58 nM/210 nM,对Akt1的选择性比对Akt3高36倍。Akti-1/2 可诱导凋亡。

Akti-1/2 Chemical Structure

Akti-1/2 Chemical Structure

CAS: 612847-09-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1367.73 现货
5mg 1218.79 现货
25mg 4055.73 现货
100mg 9582.3 现货
1g 32678.1 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

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Akti-1/2相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
ME-180 cell Growth inhibition assay Inhibition of human ME-180 cell growth in a cell viability assay, IC50=3.15011 Μm SANGER
NCI-H526 cells Growth inhibition assay Inhibition of Akt-mediated antiapoptotic activity in human NCI-H526 cells assessed as disruption of protein-Apaf-1 complex at 50 uM after 24 hrs by Western blot analysis 17603540
MDA-MB-415 cell Growth inhibition assay Inhibition of human MDA-MB-415 cell growth in a cell viability assay, IC50=1.73449 μM SANGER
MDA-MB-468 cell Growth inhibition assay Inhibition of human MDA-MB-468 cell growth in a cell viability assay, IC50=3.70773 μM SANGER
IGROV-1 cell Growth inhibition assay Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=0.72328 Μm SANGER
MDA-MB-361 cell Growth inhibition assay Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=0.48995 μM SANGER
HCC70 cell Growth inhibition assay Inhibition of human HCC70 cell growth in a cell viability assay, IC50=0.75078 μM SANGER
HGC-27 cell Growth inhibition assay Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=0.15033 μM SANGER
ETK-1 Growth inhibition assay Inhibition of human ETK-1 cell growth in a cell viability assay, IC50=4.57383 μM SANGER
EFM-19 cell Growth inhibition assay Inhibition of human EFM-19 cell growth in a cell viability assay, IC50=0.56408 μM SANGER
EFO-21 cell Growth inhibition assay Inhibition of human EFO-21 cell growth in a cell viability assay, IC50=4.43468 μM SANGER
ECC12 cell Growth inhibition assay Inhibition of human ECC12 cell growth in a cell viability assay, IC50=8.88569 μM SANGER
DSH1 cell Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay, IC50=0.98722 μM SANGER
DOK cell Growth inhibition assay Inhibition of human DOK cell growth in a cell viability assay, IC50=4.15134 μM SANGER
DMS-273 cell Growth inhibition assay Inhibition of human DMS-273 cell growth in a cell viability assay, IC50=4.15134 μM SANGER
Calu-3 cell Growth inhibition assay Inhibition of human Calu-3 cell growth in a cell viability assay, IC50=3.65321 μM SANGER
Calu-1 cell Growth inhibition assay Inhibition of human Calu-1 cell growth in a cell viability assay, IC50=7.25613 μM SANGER
Ca9-22 cell Growth inhibition assay Inhibition of human Ca9-22 cell growth in a cell viability assay, IC50=5.97333 μM SANGER
Ca-Ski cell Growth inhibition assay Inhibition of human Ca-Ski cell growth in a cell viability assay, IC50=5.3411 μM SANGER
CTB-1 cell Growth inhibition assay Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=7.59751 μM SANGER
COR-L279 cell Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay, IC50=1.68064 μM SANGER
COLO-205 cell Growth inhibition assay Inhibition of human COLO-205 cell growth in a cell viability assay, IC50=1.99706 μM SANGER
CHP-212 cell Growth inhibition assay Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=4.55867 μM SANGER
CESS cell Growth inhibition assay Inhibition of human CESS cell growth in a cell viability assay, IC50=2.70089 μM SANGER
CCRF-CEM cell Growth inhibition assay Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=4.93541 μM SANGER
CCF-STTG1 cell Growth inhibition assay Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=6.81501 μM SANGER
YKG-1 cell Growth inhibition assay Inhibition of human YKG-1 cell growth in a cell viability assay, IC50=1.01806 μM SANGER
VMRC-RCZ cell Growth inhibition assay Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=3.70955 μM SANGER
UACC-893 cell Growth inhibition assay Inhibition of human UACC-893 cell growth in a cell viability assay, IC50=5.29339 μM SANGER
UACC-62 cell Growth inhibition assay Inhibition of human UACC-62 cell growth in a cell viability assay, IC50=27.0545 μM SANGER
U251 cell Growth inhibition assay Inhibition of human U251 cell growth in a cell viability assay, IC50=19.204 μM SANGER
U-698-M cell Growth inhibition assay Inhibition of human U-698-M cell growth in a cell viability assay, IC50=39.0015 μM SANGER
U-118-MG cell Growth inhibition assay Inhibition of human U-118-MG cell growth in a cell viability assay, IC50=9.90258 μM SANGER
TT cell Growth inhibition assay Inhibition of human TT cell growth in a cell viability assay, IC50=5.32724 μM SANGER
TE-8 cell Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=24.5243 μM SANGER
TE-5 cell Growth inhibition assay Inhibition of human TE-5 cell growth in a cell viability assay, IC50=4.82452 μM SANGER
TE-15 cell Growth inhibition assay Inhibition of human TE-15 cell growth in a cell viability assay, IC50=6.49393 μM SANGER
TE-10 cell Growth inhibition assay Inhibition of human TE-10 cell growth in a cell viability assay, IC50=9.04225 μM SANGER
CAL-85-1 cell Growth inhibition assay Inhibition of human CAL-85-1 cell growth in a cell viability assay, IC50=5.95309 μM SANGER
CAL-54 cell Growth inhibition assay Inhibition of human CAL-54 cell growth in a cell viability assay, IC50=4.88625 μM SANGER
CAL-51 cell Growth inhibition assay Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=7.62841 Μm SANGER
CAL-33 cell Growth inhibition assay Inhibition of human CAL-33 cell growth in a cell viability assay, IC50=3.43125 μM SANGER
C3A cell Growth inhibition assay Inhibition of human C3A cell growth in a cell viability assay, IC50=4.42192 μM SANGER
C2BBe1 cell Growth inhibition assay Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50=13.6679 μM SANGER
C-33-A cell Growth inhibition assay Inhibition of human C-33-A cell growth in a cell viability assay, IC50=12.4783 μM SANGER
BxPC-3 cell Growth inhibition assay Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=2.22442 μM SANGER
BB30-HNC cell Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=2.86449 μM SANGER
AU565 cell Growth inhibition assay Inhibition of human AU565 cell growth in a cell viability assay, IC50=1.23917 μM SANGER
AN3-CA cell Growth inhibition assay Inhibition of human AN3-CA cell growth in a cell viability assay, IC50=1.65611 μM SANGER
A498 cell Growth inhibition assay Inhibition of human A498 cell growth in a cell viability assay, IC50=1.08134 μM SANGER
A427 cell Growth inhibition assay Inhibition of human A427 cell growth in a cell viability assay, IC50=3.07693 μM SANGER
A4-Fuk cell Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=1.8583 μM SANGER
8-MG-BA cell Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=8.63401 μM SANGER
769-P cell Growth inhibition assay Inhibition of human 769-P cell growth in a cell viability assay, IC50=1.10483 μM SANGER
697 cell Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=7.17746 μM SANGER
639-V cell Growth inhibition assay Inhibition of human 639-V cell growth in a cell viability assay, IC50=5.8773 μM SANGER
23132-87 cell Growth inhibition assay Inhibition of human 23132-87 cell growth in a cell viability assay, IC50=0.75938 μM SANGER
22RV1 cell Growth inhibition assay Inhibition of human 22RV1 cell growth in a cell viability assay, IC50=6.61424 μM SANGER
T47D cell Growth inhibition assay Inhibition of human T47D cell growth in a cell viability assay, IC50=0.5162 μM SANGER
SW954 cell Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay, IC50=5.85783 μM SANGER
SW872 cell Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay, IC50=14.1435 μM SANGER
SW780 cell Growth inhibition assay Inhibition of human SW780 cell growth in a cell viability assay, IC50=4.89358 μM SANGER
SW1710 cell Growth inhibition assay Inhibition of human SW1710 cell growth in a cell viability assay, IC50=1.38892 μM SANGER
SU-DHL-1 cell Growth inhibition assay Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=6.81543 μM SANGER
SR cell Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay, IC50=13.0746 μM SANGER
SNU-C2B cell Growth inhibition assay Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=22.2673 μM SANGER
SNU-C1 cell Growth inhibition assay Inhibition of human SNU-C1 cell growth in a cell viability assay, IC50=2.00948 μM SANGER
SNU-423 cell Growth inhibition assay Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=5.94933 μM SANGER
SNU-387 cell Growth inhibition assay Inhibition of human SNU-387 cell growth in a cell viability assay, IC50=4.19544 μM SANGER
SNB75 cell Growth inhibition assay Inhibition of human SNB75 cell growth in a cell viability assay, IC50=7.8297 μM SANGER
human SN12C cell Growth inhibition assay Inhibition of human SN12C cell growth in a cell viability assay, IC50=17.1967 μM SANGER
SK-MES-1 cell Growth inhibition assay Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50=2.10096 μM SANGER
SK-MEL-3 cell Growth inhibition assay Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=21.4696 μM SANGER
SK-MEL-24 cell Growth inhibition assay Inhibition of human SK-MEL-24 cell growth in a cell viability assay, IC50=13.1675 μM SANGER
SK-LU-1 cell Growth inhibition assay Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=42.043 μM SANGER
SK-LMS-1 cell Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=8.76452 μM SANGER
SK-CO-1 cell Growth inhibition assay Inhibition of human SK-CO-1 cell growth in a cell viability assay, IC50=10.6394 μM SANGER
SJSA-1 cell Growth inhibition assay Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50=36.9072 μM SANGER
SIG-M5 cell Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=12.6604 μM SANGER
SF295 cell Growth inhibition assay Inhibition of human SF295 cell growth in a cell viability assay, IC50=13.6183 μM SANGER
SF268 cell Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50=15.1387 μM SANGER
SF126 cell Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50=10.6746 μM SANGER
SCC-9 cell Growth inhibition assay Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=3.08536 μM SANGER
SCC-4 cell Growth inhibition assay Inhibition of human SCC-4 cell growth in a cell viability assay, IC50=9.59283 μM SANGER
SCC-25 cell Growth inhibition assay Inhibition of human SCC-25 cell growth in a cell viability assay, IC50=15.8179 μM SANGER
SBC-5 cell Growth inhibition assay Inhibition of human SBC-5 cell growth in a cell viability assay, IC50=20.8325 μM SANGER
RXF393 cell Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay, IC50=20.5863 μM SANGER
RVH-421 cell Growth inhibition assay Inhibition of human RVH-421 cell growth in a cell viability assay, IC50=32.3606 μM SANGER
RT-112 cell Growth inhibition assay Inhibition of human RT-112 cell growth in a cell viability assay, IC50=6.71952 μM SANGER
RS4-11 cell Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=6.68645 μM SANGER
RPMI-8402 cell Growth inhibition assay Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=16.343 μM SANGER
RPMI-2650 cell Growth inhibition assay Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50=5.77947 μM SANGER
RO82-W-1 cell Growth inhibition assay Inhibition of human RO82-W-1 cell growth in a cell viability assay, IC50=47.2783 μM SANGER
RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=19.4439 μM SANGER
RERF-LC-MS cell Growth inhibition assay Inhibition of human RERF-LC-MS cell growth in a cell viability assay, IC50=26.1347 μM SANGER
REH cell Growth inhibition assay Inhibition of human REH cell growth in a cell viability assay, IC50=11.4883 μM SANGER
RD cell Growth inhibition assay Inhibition of human RD cell growth in a cell viability assay, IC50=20.6036 μM SANGER
RCC10RGB cell Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=8.6567 μM SANGER
PF-382 cell Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay, IC50=11.6828 μM SANGER
PC-3 cell Growth inhibition assay Inhibition of human PC-3 cell growth in a cell viability assay, IC50=10.5135 μM SANGER
PANC-10-05 cell Growth inhibition assay Inhibition of human PANC-10-05 cell growth in a cell viability assay, IC50=14.9959 μM SANGER
PANC-03-27 cell Growth inhibition assay Inhibition of human PANC-03-27 cell growth in a cell viability assay, IC50=8.71082 μM SANGER
PA-1 cell Growth inhibition assay Inhibition of human PA-1 cell growth in a cell viability assay, IC50=9.07615 μM SANGER
P30-OHK cell Growth inhibition assay Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=4.536 μM SANGER
P12-ICHIKAWA cell Growth inhibition assay Inhibition of human P12-ICHIKAWA cell growth in a cell viability assay, IC50=14.7683 μM SANGER
OVCAR-4 cell Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=30.466 μM SANGER
OVCAR-3 cell Growth inhibition assay Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=1.84415 μM SANGER
OS-RC-2 cell Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=8.52307 μM SANGER
OMC-1 cell Growth inhibition assay Inhibition of human OMC-1 cell growth in a cell viability assay, IC50=9.25098 μM SANGER
OE33 cell Growth inhibition assay Inhibition of human OE33 cell growth in a cell viability assay, IC50=1.88926 μM SANGER
OE19 cell Growth inhibition assay Inhibition of human OE19 cell growth in a cell viability assay, IC50=7.76684 μM SANGER
OCUB-M cell Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=7.72152 μM SANGER
OCI-AML2 cell Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50=33.2531 μM SANGER
OAW-42 cell Growth inhibition assay Inhibition of human OAW-42 cell growth in a cell viability assay, IC50=7.31565 μM SANGER
NY cell Growth inhibition assay Inhibition of human NY cell growth in a cell viability assay, IC50=31.1864 μM SANGER
NUGC-3 cell Growth inhibition assay Inhibition of human NUGC-3 cell growth in a cell viability assay, IC50=16.5906 μM SANGER
NOS-1 cell Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=1.36953 μM SANGER
NMC-G1 cell Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=42.6693 μM SANGER
NKM-1 cell Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=2.75923 μM SANGER
NH-12 cell Growth inhibition assay Inhibition of human NH-12 cell growth in a cell viability assay, IC50=0.60864 μM SANGER
NCI-N87 cell Growth inhibition assay Inhibition of human NCI-N87 cell growth in a cell viability assay, IC50=29.3042 μM SANGER
NCI-H838 cell Growth inhibition assay Inhibition of human NCI-H838 cell growth in a cell viability assay, IC50=31.4118 μM SANGER
NCI-H747 cell Growth inhibition assay Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=7.62799 μM SANGER
NCI-H661 cell Growth inhibition assay Inhibition of human NCI-H661 cell growth in a cell viability assay, IC50=5.42326 μM SANGER
NCI-H650 cell Growth inhibition assay Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=7.59877 μM SANGER
NCI-H64 cell Growth inhibition assay Inhibition of human NCI-H64 cell growth in a cell viability assay, IC50=12.5431 μM SANGER
NCI-H630 cell Growth inhibition assay Inhibition of human NCI-H630 cell growth in a cell viability assay, IC50=5.51055 μM SANGER
NCI-H596 Growth inhibition assay Inhibition of human NCI-H596 cell growth in a cell viability assay, IC50=17.5708 μM SANGER
NCI-H526 cell Growth inhibition assay Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50=22.8873μM SANGER
NCI-H522 cell Growth inhibition assay Inhibition of human NCI-H522 cell growth in a cell viability assay, IC50=11.0874 μM SANGER
NCI-H520 cell Growth inhibition assay Inhibition of human NCI-H520 cell growth in a cell viability assay, IC50=1.13303 μM SANGER
NCI-H460 cell Growth inhibition assay Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=4.62993 μM SANGER
NCI-H358 cell Growth inhibition assay Inhibition of human NCI-H358 cell growth in a cell viability assay, IC50=19.7233 μM SANGER
NCI-H345 cell Growth inhibition assay Inhibition of human NCI-H345 cell growth in a cell viability assay, IC50=16.2706 μM SANGER
NCI-H292 cell Growth inhibition assay Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50=6.04837 μM SANGER
NCI-H2452 cell Growth inhibition assay Inhibition of human NCI-H2452 cell growth in a cell viability assay, IC50=26.6594 μM SANGER
NCI-H2405 cell Growth inhibition assay Inhibition of human NCI-H2405 cell growth in a cell viability assay, IC50=10.4212 μM SANGER
NCI-H2347 cell Growth inhibition assay Inhibition of human NCI-H2347 cell growth in a cell viability assay, IC50=16.1581 μM SANGER
NCI-H2342 cell Growth inhibition assay Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=0.93779 μM SANGER
NCI-H2228 cell Growth inhibition assay Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50=2.28604 μM SANGER
NCI-H2196 cell Growth inhibition assay Inhibition of human NCI-H2196 cell growth in a cell viability assay, IC50=24.8003 μM SANGER
NCI-H2170 cell Growth inhibition assay Inhibition of human NCI-H2170 cell growth in a cell viability assay, IC50=18.1028 μM SANGER
NCI-H2126 cell Growth inhibition assay Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=12.3371 μM SANGER
NCI-H2122 cell Growth inhibition assay Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=10.1385 μM SANGER
NCI-H2030 cell Growth inhibition assay Inhibition of human NCI-H2030 cell growth in a cell viability assay, IC50=1.94483 μM SANGER
NCI-H2009 cell Growth inhibition assay Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=7.39019 μM SANGER
NCI-H1993 cell Growth inhibition assay Inhibition of human NCI-H1993 cell growth in a cell viability assay, IC50=22.615 μM SANGER
NCI-H1963 cell Growth inhibition assay Inhibition of human NCI-H1963 cell growth in a cell viability assay, IC50=19.7494 μM SANGER
NCI-H1792 cell Growth inhibition assay Inhibition of human NCI-H1792 cell growth in a cell viability assay, IC50=29.8379 μM SANGER
NCI-H1770 cell Growth inhibition assay Inhibition of human NCI-H1770 cell growth in a cell viability assay, IC50=34.1793 μM SANGER
NCI-H1755 cell Growth inhibition assay Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=1.05531 μM SANGER
NCI-H1734 cell Growth inhibition assay Inhibition of human NCI-H1734 cell growth in a cell viability assay, IC50=10.7788 μM SANGER
NCI-H1703 cell Growth inhibition assay Inhibition of human NCI-H1703 cell growth in a cell viability assay, IC50=15.577 μM SANGER
NCI-H1651 cell Growth inhibition assay Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50=16.4338 μM SANGER
NCI-H1650 cell Growth inhibition assay Inhibition of human NCI-H1650 cell growth in a cell viability assay, IC50=11.5134 μM SANGER
NCI-H1648 cell Growth inhibition assay Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=5.7551 μM SANGER
NCI-H1623 cell Growth inhibition assay Inhibition of human NCI-H1623 cell growth in a cell viability assay, IC50=15.0596 μM SANGER
NCI-H1618 cel Growth inhibition assay Inhibition of human NCI-H1618 cell growth in a cell viability assay, IC50=21.9982 μM SANGER
ES7 cell Growth inhibition assay Inhibition of human ES7 cell growth in a cell viability assay, IC50=1.34511 μM SANGER
EW-3 cell Growth inhibition assay Inhibition of human EW-3 cell growth in a cell viability assay, IC50=5.64414 μM SANGER
EB2 cell Growth inhibition assay Inhibition of human EB2 cell growth in a cell viability assay, IC50=7.75468 μM SANGER
DoTc2-4510 cell Growth inhibition assay Inhibition of human DoTc2-4510 cell growth in a cell viability assay, IC50=3.43202 μM SANGER
Detroit562 cell Growth inhibition assay Inhibition of human Detroit562 cell growth in a cell viability assay, IC50=4.79465 μM SANGER
DV-90 cell Growth inhibition assay Inhibition of human DV-90 cell growth in a cell viability assay, IC50=6.03122 μM SANGER
NCI-H1563 cell Growth inhibition assay Inhibition of human NCI-H1563 cell growth in a cell viability assay, IC50=0.54246 μM SANGER
点击查看更多细胞系数据

生物活性

产品描述 Akti-1/2 (Akt Inhibitor VIII)是高度选择性的Akt1/Akt2抑制剂,IC50分别为58 nM/210 nM,对Akt1的选择性比对Akt3高36倍。Akti-1/2 可诱导凋亡。
靶点
Akt1 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
Akt3 [1]
(Cell-free assay)
58 nM 210 nM 2119 nM
体外研究(In Vitro)
体外研究活性

在基于细胞的IPKA (C33A)试验中,Akti-1/2抑制Akt1和Akt2,IC50分别为305 nM和2086 nM。在HT29,MCF7,和A2780细胞中,Akti-1/2通过急剧增加caspase-3活性诱导细胞凋亡。[1]

在肝细胞中,Akti-1/2阻断胰岛素调节PEPCK,G6Pase表达,和FOXO1活性。[2]

Akti-1/2也会通过阻断PKB强烈增强PAR-1-介导的血小板聚集。[3]

在HCC827,NCI-H522,NCI-1651,和PC-9细胞中,Akti-1/2抑制细胞生长,IC50 为4.7 μM,7.25 μM,和9.5 μM,结合时,Akti-1/2会增强细胞生长和凋亡的抑制。[4]

激酶实验 激酶筛选
简而言之,所有试验(25.5 μl在21°C下进行30 min)使用Biomek 2000实验室自动化工作站在96孔格式中进行。反应包含5–20 mU纯化的激酶和底物肽或蛋白质,通过加入10 mM 乙酸镁和5,20,或50 μM ATP ([γ-33P]-ATP, 800 cpm/pmol)起始。
细胞实验 细胞系 HCC827,NCI-H522,NCI-1651,和 PC-9 细胞
浓度 ~10 μM
孵育时间 96小时
方法

AKTi-1/2的细胞生长抑制作用使用96小时磺酰罗丹明B试验(SRB)研究。每个化合物抑制50%细胞生长的浓度(IC50)在GraphPad Prism 6.0中使用非线性回归分析和S形剂量-反应(可变斜率)方程计算。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-AKT / AKT / p-Foxo3a / p-GSK3β / p-p70S6K / p-S6 / p-4EBP1 / Cyclin D1 / Cyclin D2 / Cyclin D3 / p-Rb / p27 18725974
Immunofluorescence MCM2 / H3K9me2 / CD63 26637368
体内研究(In Vivo)
体内研究活性

在小鼠中,Akti-1/2 (50 mg/kg, i.p.)抑制肺中基底和IGF-刺激的Akt1和 Akt2磷酸化作用。[1]

化学信息&溶解度

分子量 551.64 分子式

C34H29N7O

CAS号 612847-09-3 SDF Download Akti-1/2 SDF
Smiles C1CN(CCC1N2C3=CC=CC=C3NC2=O)CC4=CC=C(C=C4)C5=C(N=C6C=C7C(=NC=N7)C=C6N5)C8=CC=CC=C8
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 22 mg/mL ( (39.88 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

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

mg/kg g μL

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

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

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

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

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

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

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