染料木素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetGenisteinCat. No.: HY-14596CAS No.: 446-72-0分式: CHO分量: 270.24作靶点: EGFR; Autophagy; Apoptosis; Endogenous Metabolite作通路: JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Autophagy; Apoptosis;Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mo

2、nth溶解性数据体外实验 DMSO : 100 mg/mL (370.04 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 3.7004 mL 18.5021 mL 37.0041 mL5 mM 0.7401 mL 3.7004 mL 7.4008 mL10 mM 0.3700 mL 1.8502 mL 3.7004 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,

3、 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，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% salineSolubil

4、ity: 3.75 mg/mL (13.88 mM); Clear solution此案可获得 3.75 mg/mL (13.88 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 37.5 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: 3 mg/mL (11.10 mM); Clear solutionPage 1 of

5、2 www.MedChemE此案可获得 3 mg/mL (11.10 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 30.0 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: 3 mg/mL (11.10 mM); Clear solution此案可获得 3 mg/mL (11.10 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 30.0 mg/mL 的澄 DMS

6、O 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Genistein种异 酮， 种多重 的酪氨酸激酶 (tyrosine kinases，如 EGFR) 抑制剂，是对多种癌症的化疗剂，主 通过改变细胞凋亡 (apoptosis)，细胞周 期和管成以及抑制转移。IC & Target EGFR Human Endogenous Metabolite0.6 M (IC50, Cell Assay)(批量添加)体外研究 Genistein inhibits serum-stimulated growth of MCF-7 and T47D ER+ cells

7、with IC50 values of 7.6 and 8.7 g/mL bydye exclusion, respectively, and 8.7 and 10.6 g/mL by 3Hthymidmne incorporation, respectively. These values aresimilar to the IC50 values of 9.4 and 7 g/mL for MCF-7 and T47D ER+ cells, respectively, obtained with the MTT assay.Additionally, Genistein at concen

8、trations up to 20 g/mL does not alter MTT mitochondrial reduction when comparedto control cells in an 8 h incubation period. Furthermore, neither biochanin A or daidzein are found to interfere withthe MTT assay at IC50 concentrations. Therefore, the MTT assay is valid for determining growth inhibiti

9、on by Genisteinat concentrations under 20 g/mL in the systems studied1.体内研究 In the present study, the effective dose of morphine caused a significant decrease in testis weight of mice comparedto Saline group (p=0.00). Moreover, testis weight are significantly increase in treated animals with Geniste

10、in andGenistein plus morphine in all doses in comparison with morphine group (p=0.028). Morphine caused a significantdecrease in the testosterone, LH and FSH hormones compared to saline group (p=0.00). In addition, the testosterone,LH and FSH hormones increased significantly in Genistein (p0.05; P0.

11、05). Significant decreasing of the protein expression of PPAR in liver is observed when Genistein isadded to rats, compared to either HFD group or HFD-BPA group3.PROTOCOLCell Assay 1 The IC50 values for Genistein are determined by the MTT assay. Briefly, the MTT assay is a colorimetric assay that is

12、based on the ability of living but not dead cells to reduce a tetrazolium-based compound to a blue formazanproduct. The formazan crystals are solubilized in DMSO, and the absorbance is measured at 540 nm. The absorbanceat 540 nm is proportional to the number of viable cells. The lC50 values obtained

13、 with the MTT assay are comparedwith the lC50 values obtained by counting viable cells using trypan blue dye exclusion and by tritiated thymidineincorporation into DNA1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice2Administration 23 Balb/c

14、 male mice are used. Genistein is administered as follows: On days 1-30, Genistein once daily, interaperitoneallyinjecting. Morphine plus Genistein is administered as follows: On days 1-30, Genistein once daily plus morphine,Page 2 of 3 www.MedChemEinteraperitoneally injecting (17, 18). The same vol

15、ume of saline is administered. Mice are randomly divided into 8groups (n=6). 1) Normal saline group (1 mL DW/daily); 2) Morphine treated group; 3) Genistein 1 mg/kg treatedgroup; 4) Genistein 2 mg/kg treated group 5) Genistein 4 mg/kg treated group; 6) Morphine plus Genistein 1 mg/kgtreated group; 7

16、) Morphine plus Genistein 2 mg/kg treated group; 8) Morphine plus Genistein 4 mg/kg treatedgroup.Rats3Male 8-week-old Wistar rats (150-180g) are used. After one week acclimation, all rats are randomly divided into 8groups with 10 rats per group and treated for 35 weeks as follows: (1) STD group is f

17、ed with rodent standard chowdiet (STD); (2) STD-BPA group is fed with STD and administered with BPA (50 g/kg/day); (3) STD-(BPA+G) group isfed with STD and administered with BPA (50 g/kg/day) plus Genistein (10 mg/kg/day); (4) STD-G group is fed withSTD and administered with Genistein (10 mg/kg/day)

18、; (5) HFD group received high-fat diet (HFD); (6) HFD-BPA groupis fed with HFD and administered with BPA (50 g/kg/day); (7) STD-(BPA+G) group is fed with HFD and administeredwith BPA (50 g/kg/day) plus Genistein (10 mg/kg/day); (8) HFD-G group is fed with HFD and administrated withGenistein (10 mg/k

19、g/day). All the male genitors are treated for 35 weeks consecutively. The details of BPA (50 g/kg/day) and Genistein (10 mg/kg/day) treatment methods have been described previously: BPA is dissolved in cornoil and diluted with three stock solutions (20, 40, 80, and 120 g/mL).MCE has not independentl

20、y confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 ACS Nano. 2020 Apr 20. ACS Appl Mater Interfaces. 2020 Jan 8;12(1):1707-1720. Theranostics. 2019 May 31;9(13):3732-3753. Br J Pharmacol. 2020 Apr 15. J Mol Med (Berl). 2019 Apr;97(4):541-552.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Peterson G, et al. Genistein inhibits both estrogen and growth factor-stimulated proliferation of human breast cance