1. Apoptosis
  2. Apoptosis
  3. Adarotene

Adarotene  (Synonyms: ST1926)

目录号: HY-14808 纯度: 99.18%
COA 产品使用指南

Adarotene 是一种有效的 apoptosis 诱导剂,通过产生 DNA 损伤,来阻止人类肿瘤细胞的增殖。

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Adarotene Chemical Structure

Adarotene Chemical Structure

CAS No. : 496868-77-0

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10 mM * 1 mL in DMSO ¥716
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5 mg ¥651
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10 mg ¥1209
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50 mg ¥3813
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Top Publications Citing Use of Products

    Adarotene purchased from MCE. Usage Cited in: Biomed Pharmacother. 2020 Aug;128:110291.  [Abstract]

    Western blot analysis of p-AMPKα, p-mTOR and p-P70S6K in ST1962 (2.5, 5 and 10 μM)-treated glioma cell lines for 24 h. AMPKα activation is markedly induced by ST1926 in a dose-dependent manner; phosphorylated mechanistic target of rapamycin (mTOR) and P70S6K expression levels are obviously down-regulated.

    Adarotene purchased from MCE. Usage Cited in: Biomed Pharmacother. 2020 Aug;128:110291.  [Abstract]

    Effects of ST1926 on retinoic acid (RA) pathway. Glioma cells are treated with ST1926 (2.5, 5 and 10 μM) for 24 h, immunofluorescence staining of CRABP2.

    Adarotene purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017;41(2):519-529.  [Abstract]

    Arithmetic means±SEM (n=10) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) Adarotene (3-9 µM) or solvant DMSO alone (grey bar).
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Adarotene is an effective apoptosis inducer, which surprisingly produces DNA damage and exhibites a potent antiproliferative activity on a large panel of human tumor cells.

    体外研究
    (In Vitro)

    Adarotene causes a dose-dependent growth inhibition in a large panel of human tumor cell lines with IC50 ranging from 0.1 to 0.3 µM. Adarotene causes cell accumulation in G1/S or S phase of cell cycle depending on tumor cells IGROV-1 and DU145[1]. Adarotene is apoptotic and cytotoxic on a large spectrum of cancerous and leukemic cells, including freshly isolated AML blasts in primary culture. The molecular target of ST1926 apoptotic activity in myeloid leukemia cells is similar to the ligand-binding domain of RARγ. Adarotene treatment of cells results in rapid accumulation of intracellular calcium[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Adarotene (15, 20 mg/kg, p.o.) causes a significant tumor growth inhibition in a human ovarian carcinoma, A2780/DX, and in a human melanoma, MeWo, growing in nude mice[1]. Adarotene (30, 40 mg/kg, p.o.) results in a significant and dose-dependent increase in the life span of NB4-bearing SCID mice without overt toxicity[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    374.47

    Formula

    C25H26O3

    CAS 号
    性状

    固体

    颜色

    White to green

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 25 mg/mL (66.76 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6704 mL 13.3522 mL 26.7044 mL
    5 mM 0.5341 mL 2.6704 mL 5.3409 mL
    查看完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方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,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.68 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.68 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.18%

    参考文献
    Cell Assay
    [2]

    Briefly, cells (1×107/mL) are loaded with 1 μM FURA-2 at 37°C in the dark for 30 minutes, washed twice, resuspended in phosphate-buffered saline (PBS) containing 1.26 mM CaCl2 at 106 cells/mL and then used for the experiments. Dual excitation, alternating at 340 nm and 380 nm, is provided by a spectrophotofluorometer equipped with 2 excitation monochromators, and emission is fixed at 480 nm. The temperature is set at 37°C±1°C. In some experiments, to eliminate extracellular calcium, cells preloaded with FURA-2 are resuspended in PBS without Ca2+, and 0.5 mM EGTA (ethylene glycol tetraacetic acid) is added to each sample prior to addition of the appropriate stimulus.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    NB4 cells (3×106) are intraperitoneally inoculated in SCID mice (8 mice/group). ST1926 is dissolved in cremophor/ethanol 1:1 solution, and diluted 1:10 in PBS at the concentration of 50 mg/kg; the doses of 30 mg/kg and 40 mg/kg are then prepared by appropriate dilutions in the same vehicle. ATRA is dissolved in the dark in Cremophor EL and kept magnetically stirred; the solution is then diluted 1:10 in PBS at the final concentration of 40 mg/kg. Both compounds are administered intraperitoneally and orally twice per day for 3 weeks starting from the day after cell inoculation, in a volume of 10 mL/kg. During treatments body weight and lethality are registered.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    Adarotene 相关分类

    完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6704 mL 13.3522 mL 26.7044 mL 66.7610 mL
    5 mM 0.5341 mL 2.6704 mL 5.3409 mL 13.3522 mL
    10 mM 0.2670 mL 1.3352 mL 2.6704 mL 6.6761 mL
    15 mM 0.1780 mL 0.8901 mL 1.7803 mL 4.4507 mL
    20 mM 0.1335 mL 0.6676 mL 1.3352 mL 3.3381 mL
    25 mM 0.1068 mL 0.5341 mL 1.0682 mL 2.6704 mL
    30 mM 0.0890 mL 0.4451 mL 0.8901 mL 2.2254 mL
    40 mM 0.0668 mL 0.3338 mL 0.6676 mL 1.6690 mL
    50 mM 0.0534 mL 0.2670 mL 0.5341 mL 1.3352 mL
    60 mM 0.0445 mL 0.2225 mL 0.4451 mL 1.1127 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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