土木香内酯作用机制 - Medchemexpress - MCE中国

1、Product Data SheetAlantolactoneCat. No.: HY-N0038CAS No.: 546-43-0分式: CHO分量: 232.32作靶点: STAT; Apoptosis; TGF-beta/Smad作通路: JAK/STAT Signaling; Stem Cell/Wnt; Apoptosis; TGF-beta/Smad储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (430.44 mM)* means so

2、luble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 4.3044 mL 21.5220 mL 43.0441 mL5 mM 0.8609 mL 4.3044 mL 8.6088 mL10 mM 0.4304 mL 2.1522 mL 4.3044 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时

3、，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (10.76 mM); Clear solution此案可获得 2.5

4、mg/mL (10.76 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (10.76 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (10.76 mM，饱和度未知) 的澄清溶

5、液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (10.76 mM); Clear solution此案可获得 2.5 mg/mL (10.76 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性

6、Alantolactone是STAT3 的选择性抑制剂，并具有抗肿瘤活性。Alantolactone 可诱导癌症相关的凋亡。IC & Target STAT3体外研究 Alantolactone induces apoptosis in HepG2 cells in a dose-dependent manner. This Alantolactone-induced apoptosisis found to be associated with GSH depletion, inhibition of STAT3 activation, ROS generation, mitochondri

7、altransmembrane potential dissipation, and increased Bax/Bcl-2 ratio and caspase-3 activation1. Alantolactonedecreases STAT3 translocation to the nucleus, its DNA-binding, and STAT3 target gene expression. Alantolactonesignificantly inhibits STAT3 activation with a marginal effect on MAPKs and on NF

8、-B transcription; however, thiseffect is not mediated by inhibiting STAT3 upstream kinases2.Alantolactone induces activin/SMAD3 signaling in human colon adenocarcinoma HCT-8 cells. Alantolactone performsits antitumor effect by interrupting the interaction between Cripto-1 and the activin receptor ty

9、pe IIA in the activinsignaling pathway4.Alantolactone (5 g/mL, 24 h) inhibits cell proliferation in colon adenocarcinoma HCT-8 cells4.Cell Viability Assay4Cell Line: HCT-8 cells.Concentration: 5 g/mL (21.6 M).Incubation Time: 24 h.Result: Activated the activin signaling pathway in HCT-8 cells.体内研究 I

10、t is found that the average tumor volume in the Alantolactone-treated mice is approximately 2.17-fold lowercompared with that in the control mice. However the administration of Alantolactone does not affect the overallbodyweight during the experimental period, suggesting no apparent toxicity. Additi

11、onally, the average tumor weightis significantly lower in the Alantolactone-treated mice compared with the control mice. Whats more, theadministration of Alantolactone results in a significant decrease in p-STAT3 and cyclin D1 expression in the tumortissues2.Animal Model: Female athymic BALB/c nude

12、mice at the age of 6 weeks2.Dosage: 2.5 mg/kg.Administration: I.P. injection every 2 days.Result: Exhibited anti-cancer activity.Page 2 of 3 www.MedChemE户使本产品发表的科研献 Stem Cells. 2019 Feb;37(2):190-201. Pharmacol Res. 2020 Mar.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFEREN

13、CES1. Khan M, et al. Alantolactone induces apoptosis in HepG2 cells through GSH depletion, inhibition of STAT3 activation, and mitochondrial dysfunction.Biomed Res Int. 2013;2013:719858.2. Chun J, et al. Alantolactone selectively suppresses STAT3 activation and exhibits potent anticancer activity in MDA-MB-231 cells. Cancer Lett. 2015 Feb1;357(1):393-403.McePdfHeightCaution: Pro