冬凌草甲素 促销 ≥98%(HPLC),分析标准品
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| 包装规格: | 20mg in glass bottle |
| 产品描述: | 基本信息 产品编号: O10037 产品名称: Oridonin CAS: 28957-04-2 储存条件 粉末 2-8℃ 四年 分子式: C20H28O6364.43 溶于液体 -80℃ 两年 分子量 364.43 -20℃ 一个月 化学名: (14R)-7-alpha,20-Epoxy-1-alpha,6-beta,7,14-tetrahydroxykaur-16-en-15-one Solubility (25°C): 体外: DMSO 73mg/mL (200.31mM) Ethanol 28mg/mL (76.83mM) Water Insoluble 体内(现配现用): 1.请依序添加每种溶剂:10% 1-Methyl-2-pyrrolidinone→90% PEG300 Solubility: ≥ 5mg/mL (13.72mM); Clear solution 2.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.08mg/mL (5.71mM); Clear solution 此⽅案可获得 ≥ 2.08mg/mL (5.71mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中,混合均匀;向上述体系中加⼊ 50μL Tween-80,混合均匀;然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 3.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.08mg/mL (5.71mM); Clear solution 此⽅案可获得 ≥ 2.08mg/mL (5.71mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均匀。 4.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility: ≥ 2.08mg/mL (5.71mM); Clear solution 此⽅案可获得 ≥ 2.08mg/mL (5.71mM,饱和度未知) 的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例,取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中,混合均匀。 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 2.7440mL 13.7201mL 27.4401mL 5mM 0.5488mL 2.7440mL 5.4880mL 10mM 0.2744mL 1.3720mL 2.7440mL 50mM 0.0549mL 0.2744mL 0.5488mL 生物活性 产品描述 Oridonin (Isodonol, Rubescenin, NSC-250682) 是从Rabdosia rubescens中分离的对映贝壳杉烷二萜,是一种具有抗肿瘤、抗细菌和抗感染效果的传统中药。Oridonin 抑制AKT1 和 AKT2的激酶活性,对应的IC50值分别为8.4μM 和 8.9μM。 靶点 Akt1 (Cell-free assay) 8.4μM Akt2 (Cell-free assay) 8.9μM 体外研究 Oridonin有效抑制各种癌细胞的增殖,包括来自前列腺癌 (LNCaP, DU145, PC3),乳腺癌(MCF-7, MDA-MB231),非小细胞肺癌 (NSCL) (NCI-H520, NCI-H460, NCI-H1299),急性早幼粒细胞白血病(NB4),以及胶质母细胞瘤(U118, U138)的细胞增殖,ED50s的范围为1.8 to 7.5 μ克/毫升。Oridonin的抗肿瘤活性可能是由于它对NF-κB和MAPKs信号通路的抑制作用。 体内研究 LD50:小鼠35-40毫克/千克。 推荐实验方法(仅供参考) Kinase Assay For the AKT kinase assay, the ADP-Glo™ Kinase Assay Kit is used. Active AKT1 or AKT2 kinase and inactive GSK-3β as substrate are mixed by 1× reaction buffer and then added to a white 96-well plate. Pure ATP provided in the kit is serially diluted obtain a final concentration of 0, 1, 10, 50, and 100μM. GSK-3β is added to reach a final concentration of 2.5, 5, 10 or 20μM and DMSO is used as a control. The mixed solution is incubated at room temperature and luciferase activity is measured using the Luminoskan Ascent plate reader Cell Assay Cells are seeded (6×103 cells/well for KYSE70; 2.5×103 cells/well for KYSE410; 2×103 cells/well for KYSE450) in 96-well plates and incubated for 24 h and then treated with different amounts of Oridonin or vehicle. After incubation for 24, 48 or 72 h, cell proliferation is measured by the MTT assay. For anchorage-independent cell growth assessment, cells (2.5, 5 or 10μM Oridonin) suspended in complete medium are added to 0.3% agar with vehicle, 2.5, 5 or 10μM Oridonin in a top layer over a base layer of 0.5% agar with vehicle, 2.5, 5 or 10μM Oridonin. The cultures are maintained at 37°C in a 5% CO2 incubator for 3 weeks and then colonies are visualized under a microscope and counted using the Image-Pro Plus software program Animal Administration Mice Breast cancer cells are harvested and resuspended in 40% Matrigel-Basement Membrane Matrix, LDEV-free, and then injected (100μL per site) into the fourth pair of mammary fat pads of nude mice (CrTac: NCr-Foxn1nu). Tumors are measured in two dimensions using manual calipers. Tumor volume is calculated using the formula: Volume = 0.5 × length × width × width. Tumor volume is measured every 2-3 days. Upon harvesting, tumors are fixed in formalin overnight and then in 70% ethanol for histopathology analysis. Mice are treated with Oridonin (15mg/kg) in 1% Pluronic F68 or vehicle (1% Pluronic F68) daily by intraperitoneal (IP) injection. BEZ235 is reconstituted 1:9 in 1-methyl-2 pyrolidone and polyethylene glycol 300 (PEG300) Mice are treated with this compound formulation at 45mg/kg daily (QD) by oral gavage |
| 保存条件: | 2-8℃ |
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