2. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  3. Topoisomerase ADC Cytotoxin
  4. Daun02

Daun02是拓扑异构酶抑制剂Daunorubicin的前体。

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Daun02 Chemical Structure

Daun02 Chemical Structure

CAS No. : 290304-24-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4857
In-stock
2 mg ￥1800
In-stock
5 mg ￥2800
In-stock
10 mg ￥4990
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Daun02 相关抗体

Top Publications Citing Use of Products

    Daun02 purchased from MCE. Usage Cited in: Sci Rep. 2017 Jan 3;7:39817.  [Abstract]

    Photomicrographs represent cFos in the MePD after Meth and hormone administration following DAUN02 or vehicle infusions. A student’s t-test show DAUN02 significantly reduces Fos-ir cells in the MePD compared to the vehicle-treated cohort.

    查看 Topoisomerase 亚型特异性产品:

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    Topoisomerase Topo I Topo II

    查看 ADC Cytotoxin 亚型特异性产品:

    查看所有亚型
    Auristatin Calicheamicins Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Daun02 is a proagent of the topoisomerase inhibitor Daunorubicin.

    IC50 & Target[2]

    Topoisomerase

     

    Daunorubicins/Doxorubicins

     

    体外研究
    (In Vitro)

    Daun02 is a prodrug, which is converted by β-galactosidase to Daunorubicin, which has been shown to reduce calcium ion (Ca2+)-dependent action potentials in neuroblastoma cells[1]. Daunorubicin is a topoisomerase inhibitor[2]. Daun02 is a good substrate for β-galactosidase (β-gal). The concentration of Daun02 producing 50% (EC50) decrease in cell viability is 0.5 μM, 1.5 μM, and 3.5 μM for T47-D, Panc02, and MCF-7, respectively[3].

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

    Daun02 相关抗体:
    体内研究
    (In Vivo)

    Daun02 is a good substrate for β-gal with Km and Vmax values of 0.37 mM and 8.6 μmol/min/mg protein. At a concentration of 10-5 M, Daun02 is 79% bound to plasma protein compares to 94% for Daunomycin[3].

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

    884.79

    Formula

    C41H44N2O20
    CAS 号
    性状

    固体

    颜色

    Brown to wine

    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 6 months
    -20°C 1 month
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (113.02 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.1302 mL 5.6511 mL 11.3021 mL
    5 mM 0.2260 mL 1.1302 mL 2.2604 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 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

    动物实验：

    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 (2.83 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。

      以 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。
    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

    只
    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: 98.72%

    COA (268 KB) LCMS (95 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [3]

    Murine Panc02 cells are maintained as exponentiallygrowing monolayer cultures in DMEM/F12 or RPMI-1640 medium supplemented with 10% FBS, 1% glutamine, penicillin, and streptomycin at 37°C. For cytotoxicity assay, the cells are seeded into 96-well microplates and incubated overnight. Initial experiments indicate that FBS contains low levels of intrinsic β-gal activity as evidenced by the slow conversion of Daun02 to Daunomycin; however, this is not evident for human serum. Therefore, prior to addition of Daun02, the FBS concentration is reduced from 10% to 1% for Panc02 cells. Human serum (10%) is used for the transduced human cell lines. The cells are incubated for 24 h and then MTT is added. Lysis buffer (20% SDS dissolved in 50% DMF) is added 4 h after the addition of MTT and the cells are incubated overnight. The optical density at 570 nm is determined using a BIO-RAD microplate reader. Cytotoxicity is expressed as the concentration of drug or prodrug that produced a 50% (EC50) reduction in cell viability[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3]
    Male athymic BALB/c mice (nu/nu genotype, 18-20 g) are used. Daunomycin is administered at a dose of 20 mg/kg in 100 μL normal saline solution into the tail vein. Daun02 is administered intraperitoneallyat a dose of 200 mg/kg in 200 μL vehicle. (This route is selected because the volume of drug solution, 200 μL, is too great for tail vein administration.) Tumor volume is determined bycaliper measurement in two dimensions and converted to tumor mass. Tumor growth is monitored over a period of 30 days or until the tumors has reached a mass of 5% of bodyweight (about 1 g). The animals are then killed bycarbon dioxide asphyxiation.

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

    Daun02 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.1302 mL 5.6511 mL 11.3021 mL 28.2553 mL
    5 mM 0.2260 mL 1.1302 mL 2.2604 mL 5.6511 mL
    10 mM 0.1130 mL 0.5651 mL 1.1302 mL 2.8255 mL
    15 mM 0.0753 mL 0.3767 mL 0.7535 mL 1.8837 mL
    20 mM 0.0565 mL 0.2826 mL 0.5651 mL 1.4128 mL
    25 mM 0.0452 mL 0.2260 mL 0.4521 mL 1.1302 mL
    30 mM 0.0377 mL 0.1884 mL 0.3767 mL 0.9418 mL
    40 mM 0.0283 mL 0.1413 mL 0.2826 mL 0.7064 mL
    50 mM 0.0226 mL 0.1130 mL 0.2260 mL 0.5651 mL
    60 mM 0.0188 mL 0.0942 mL 0.1884 mL 0.4709 mL
    80 mM 0.0141 mL 0.0706 mL 0.1413 mL 0.3532 mL
    100 mM 0.0113 mL 0.0565 mL 0.1130 mL 0.2826 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.

    Keywords:

    Daun02290304-24-4Daun 02Daun-02TopoisomeraseADC CytotoxinADC PayloadInhibitorinhibitorinhibit

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    目录号：
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