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Oridonin

別名: NSC-250682, Isodonol, Rubescenin 中文名稱:冬凌草甲素,東凌草素

Oridonin是從Rabdosia rubescens中分離的對映貝殼杉烷二萜,是一種具有抗腫瘤、抗細(xì)菌和抗感染效果的傳統(tǒng)中藥。Oridonin 抑制AKT1AKT2的激酶活性,對應(yīng)的IC50值分別為8.4 μM 和 8.9 μM。

Oridonin Chemical Structure

Oridonin Chemical Structure

CAS: 28957-04-2

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 730.05 現(xiàn)貨
10mg 582.66 現(xiàn)貨
50mg 2191.33 現(xiàn)貨
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Oridonin相關(guān)產(chǎn)品

相關(guān)信號通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
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
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
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
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
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
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生物活性

產(chǎn)品描述 Oridonin是從Rabdosia rubescens中分離的對映貝殼杉烷二萜,是一種具有抗腫瘤、抗細(xì)菌和抗感染效果的傳統(tǒng)中藥。Oridonin 抑制AKT1AKT2的激酶活性,對應(yīng)的IC50值分別為8.4 μM 和 8.9 μM。
靶點(diǎn)
Akt1 [5]
(Cell-free assay)
Akt2 [5]
(Cell-free assay)
8.4 μM 8.9 μM
體外研究(In Vitro)
體外研究活性

Oridonin有效抑制各種癌細(xì)胞的增殖,包括來自前列腺癌 (LNCaP, DU145, PC3),乳腺癌(MCF-7, MDA-MB231),非小細(xì)胞肺癌 (NSCL) (NCI-H520, NCI-H460, NCI-H1299),急性早幼粒細(xì)胞白血病(NB4),以及膠質(zhì)母細(xì)胞瘤(U118, U138)的細(xì)胞增殖,ED50s的范圍為1.8 to 7.5 μ克/毫升。[1] Oridonin的抗腫瘤活性可能是由于它對NF-κB和MAPKs信號通路的抑制作用。[2] [3]

實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot BCR-ABL / Myc p-AMPK / AMPK / Glut1 / LC3 28128329
Immunofluorescence HSF1 p65 28128329
Growth inhibition assay Cell viability 26496199
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

LD50:小鼠35-40毫克/千克。[4]

化學(xué)信息&溶解度

分子量 364.43 分子式

C20H28O6

CAS號 28957-04-2 SDF Download Oridonin SDF
儲存條件(自收到貨起)

體外溶解度
批次:

DMSO : 72 mg/mL ( (197.56 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO)

Ethanol : 34 mg/mL (93.29 mM)

Water : Insoluble

摩爾濃度計(jì)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(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計(jì)算器(澄清溶液)

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

mg/kg g μL

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(jì)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,: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: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: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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