연구용

Akti-1/2 Akt 억제제

제품 번호S7776

Akti-1/2 (Akt Inhibitor VIII)는 IC50이 각각 58 nM/210 nM인 고도로 선택적인 Akt1/Akt2 억제제로, Akt3에 비해 Akt1에 대해 약 36배의 선택성을 갖습니다. 이 화합물은 apoptosis를 유도합니다.
Akti-1/2 Akt 억제제 Chemical Structure

화학 구조

분자량: 551.64

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품질 관리

배치: 순도: 99.11%
99.11

세포 배양, 처리 및 작업 농도

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

화학 정보, 보관 및 안정성

분자량 551.64 화학식

C34H29N7O

보관 (수령일로부터)
CAS 번호 612847-09-3 SDF 다운로드 원액 보관

동의어 Akt Inhibitor VIII 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

용해도

In vitro
배치:

DMSO : 22 mg/mL (39.88 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

Targets/IC50/Ki
Akt1
(Cell-free assay)
58 nM
Akt2
(Cell-free assay)
210 nM
Akt3
(Cell-free assay)
2119 nM
시험관 내(In vitro)

세포 기반 IPKA(C33A) 분석에서 Akti-1/2는 Akt1과 Akt2를 각각 305 nM 및 2086 nM의 IC50으로 억제합니다. HT29, MCF7 및 A2780 세포에서 이 화합물은 caspase-3 활성을 극적으로 증가시켜 세포 apoptosis를 유도합니다.

간세포에서 이 화학물질은 PEPCK, G6Pase 발현 및 FOXO1 활성 조절을 차단합니다.

또한 PKB를 차단하여 PAR-1 매개 혈소판 응집을 강력하게 증강합니다.

HCC827, NCI-H522, NCI-1651 및 PC-9 세포에서 이 억제제는 4.7 μM, 7.25 μM 및 9.5 μM의 IC50으로 세포 성장을 억제하며, 병용 시 세포 성장 및 apoptosis의 향상된 억제를 유발합니다.

키나아제 분석
카이네이즈 스크리닝
간략하게, 모든 분석(21°C에서 30분 동안 25.5 μl)은 Biomek 2000 실험실 자동화 워크스테이션을 사용하여 96웰 형식으로 수행됩니다. 반응물은 기질 펩타이드 또는 단백질과 함께 5 –20 mU의 정제된 키나아제를 포함하며, 10 mM MgAcetate와 5, 20 또는 50 μM ATP([γ-33P]-ATP, 800 cpm/pmol)의 첨가로 시작됩니다.
생체 내(In vivo)

생쥐에서 Akti-1/2 (50 mg/kg, i.p.)는 폐에서 기저 및 IGF-자극 Akt1 및 Akt2 인산화를 억제합니다.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/24957682/
  • [5] https://pubmed.ncbi.nlm.nih.gov/34285232/

적용 분야

방법 바이오마커 이미지 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
S7776-WB1
18725974
Immunofluorescence MCM2 / H3K9me2 / CD63
S7776-IF1
26637368

기술 지원

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