연구용

Oridonin Akt 억제제

제품 번호S2335

Oridonin은 Rabdosia rubescens에서 정제된 디테르페노이드로, 항종양, 항-Bacterial 및 항염증 효과를 가진 전통적인 약물입니다. 이 화합물은 AKT1AKT2 키나아제 활성을 각각 8.4 μM 및 8.9 μM의 IC50으로 억제합니다.
Oridonin Akt 억제제 Chemical Structure

화학 구조

분자량: 364.43

바로가기

품질 관리

배치: 순도: 99.99%
99.99

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
HL60 Cytotoxicity assay 48 hrs Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50=2.5μM 23819871
RAW264.7 Antiinflammatory assay 18 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess method, IC50=5.2μM 23819871
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50=4.33μM 28165738
Bel7402 Antiproliferative assay 72 hrs Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay, IC50=5.41μM 28165738
MGC803 Antiproliferative assay 72 hrs Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay, IC50=9.06μM 28165738
KB/CP4 Antiproliferative assay 48 hrs Antiproliferative activity against human KB/CP4 cells after 48 hrs by MTT assay, IC50=10.8μM 28165738
KB-3-1 Antiproliferative assay 48 hrs Antiproliferative activity against human KB-3-1 cells after 48 hrs by MTT assay, IC50=13.24μM 28165738
BEL7404/CP20 Antiproliferative assay 48 hrs Antiproliferative activity against human BEL7404/CP20 cells after 48 hrs by MTT assay, IC50=17.17μM 28165738
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=17.89μM 28165738
Bel7404 Antiproliferative assay 48 hrs Antiproliferative activity against human Bel7404 cells after 48 hrs by MTT assay, IC50=17.92μM 28165738
NCI-H460 Antiproliferative assay 48 hrs Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay, IC50=20.51μM 28165738
NCI-H460/MX20 Antiproliferative assay 48 hrs Antiproliferative activity against human NCI-H460/MX20 cells after 48 hrs by MTT assay, IC50=25.86μM 28165738
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=4.64μM 30921757
SGC7901 Antiproliferative assay 72 hrs Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=7.13μM 30921757
Bel7402 Antiproliferative assay 72 hrs Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=7.85μM 30921757
HL60 Antiproliferative assay 72 hrs Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=9.46μM 30921757
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=10.07μM 30921757
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=18.15μM 30921757
L02 Cytotoxicity assay 72 hrs Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=19.53μM 30921757
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=6.84μM 30981113
L02 Cytotoxicity assay 48 hrs Cytotoxicity in human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=6.97μM 30981113
Bel7402 Antiproliferative assay 48 hrs Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=9.59μM 30981113
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=17.56μM 30981113
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay, EC50=29.4μM 30981113
HCT116 Cell cycle arrest assay 3 uM 24 hrs Induction in cell cycle arrest in human HCT116 cells assessed as inhibition in cyclin A protein expression level at 3 uM incubated for 24 hrs by Western blot analysis 30981113
HCT116 Cell cycle arrest assay 3 uM 24 hrs Induction in cell cycle arrest in human HCT116 cells assessed as inhibition in cyclin B1 protein expression level at 3 uM incubated for 24 hrs by Western blot analysis 30981113
HCT116 Apoptotic assay 1 uM 24 hrs Induction of apoptotic morphological change in human HCT116 cells assessed as loss of original morphology at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method 30981113
HCT116 Apoptotic assay 1 uM 24 hrs Induction of apoptotic morphological change in human HCT116 cells assessed as formation of unstructured state at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method 30981113
HCT116 Apoptotic assay 1 uM 24 hrs Induction of apoptotic morphological change in human HCT116 cells assessed as formation of volume swelling at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method 30981113
HCT116 Apoptotic assay 1 uM 24 hrs Induction of apoptotic morphological change in human HCT116 cells assessed as formation of condensed nuclei at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method 30981113
HCT116 Apoptotic assay 1 uM 24 hrs Induction of apoptotic morphological change in human HCT116 cells assessed as cell lysis at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method 30981113
HCT116 Apoptotic assay 1 uM 24 hrs Induction of apoptotic morphological change in human HCT116 cells assessed as membrane shrinkage at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method 30981113
PLC/PRF/5 Antiproliferative assay 72 hrs Antiproliferative activity against human PLC/PRF/5 cells incubated for 72 hrs by CCK8 cells, IC50=7.41μM 31200238
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells incubated for 72 hrs by CCK8 cells, IC50=8.12μM 31200238
RPMI8226 Antiproliferative assay 72 hrs Antiproliferative activity against human RPMI8226 cells incubated for 72 hrs by CCK8 cells, IC50=9.25μM 31200238
LO2 Cytotoxicity assay 72 hrs Cytotoxicity against human LO2 cells incubated for 72 hrs by CCK8 cells, IC50=17.47μM 31200238
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK8 cells, IC50=30.4μM 31200238
HepG2 Function assay 0.1 to 1 uM 10 days Inhibition of colony formation in human HepG2 cells at 0.1 to 1 uM incubated for 10 days by crystal violet staining based microscopic method 31200238
PLC/PRF/5 Function assay 0.001 to 1 uM 10 days Inhibition of colony formation in human PLC/PRF/5 cells assessed as decrease in colony size at 0.001 to 1 uM incubated for 10 days by crystal violet staining based microscopic method 31200238
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=4.79μM 31202992
SGC7901 Antiproliferative assay 72 hrs Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=7.87μM 31202992
Bel7402 Antiproliferative assay 72 hrs Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=8.31μM 31202992
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=17.8μM 31202992
L02 Cytotoxicity assay 72 hrs Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=18.68μM 31202992
TE1 Antiproliferative assay 72 hrs Antiproliferative activity against human TE1 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=12.73μM 31494472
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=13.45μM 31494472
MGC803 Antiproliferative assay 72 hrs Antiproliferative activity against human MGC803 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=14.13μM 31494472
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=21.97μM 31494472
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 364.43 화학식

C20H28O6

보관 (수령일로부터)
CAS 번호 28957-04-2 SDF 다운로드 원액 보관

용해도

In vitro
배치:

DMSO : 72 mg/mL (197.56 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 34 mg/mL

Water : 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)
8.4 μM
Akt2
(Cell-free assay)
8.9 μM
시험관 내(In vitro)

Oridonin은 전립선 (LNCaP, DU145, PC3), 유방 (MCF-7, MDA-MB231), 비소세포폐암 (NSCL) (NCI-H520, NCI-H460, NCI-H1299), 급성 전골수성 백혈병 (NB4) 및 교모세포종 (U118, U138)을 포함한 다양한 암세포의 증식을 ED50이 1.8 내지 7.5 μg/ml 범위로 효과적으로 억제합니다. 이 화합물의 항종양 활성은 NF-kappaB 및 MAPKs 신호 경로에 대한 억제 효과 때문일 수 있습니다.

생체 내(In vivo)

LD50: 마우스 35-40mg/kg.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/1269612/
  • [5] https://pubmed.ncbi.nlm.nih.gov/29695636/

적용 분야

방법 바이오마커 이미지 PMID
Western blot BCR-ABL / Myc p-AMPK / AMPK / Glut1 / LC3
S2335-WB1
28128329
Immunofluorescence HSF1 p65
S2335-IF1
28128329
Growth inhibition assay Cell viability
S2335-viability1
26496199

기술 지원

취급 설명서

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

다른 문의사항이 있으시면 메시지를 남겨주세요.

이름을 입력해주세요.
이메일을 입력해주세요. 유효한 이메일 주소를 입력해주세요.
저희에게 무엇이든 작성해주세요.