1. Cell Cycle/DNA Damage Autophagy Apoptosis
  2. Topoisomerase Autophagy Apoptosis
  3. Topotecan hydrochloride

Topotecan hydrochloride  (Synonyms: 盐酸拓扑替康; SKF 104864A hydrochloride; NSC 609669 hydrochloride)

目录号: HY-13768A 纯度: 99.76%
COA 产品使用指南

Topotecan Hydrochloride (SKF 104864A Hydrochloride) 是具有抗癌活性的 拓扑异构酶I 抑制剂。

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Topotecan hydrochloride Chemical Structure

Topotecan hydrochloride Chemical Structure

CAS No. : 119413-54-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
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5 mg ¥312
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10 mg ¥500
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50 mg ¥1326
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100 mg ¥2238
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500 mg   询价  

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Other Forms of Topotecan hydrochloride:

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Top Publications Citing Use of Products

    Topotecan hydrochloride purchased from MCE. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761.  [Abstract]

    WDR5 inhibitor OICR-9429 enhances the sensitivity of ovarian cancer to genotoxic chemotherapeutics in vivo. Representative images and the apoptotic rate the indicated chemotherapy-treated xenograft tumors.

    Topotecan hydrochloride purchased from MCE. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761.  [Abstract]

    IB analysis of the level of cleaved-caspase 3 and cleaved-PARP1 in the indicated chemotherapy-treated xenograft tumors. GAPDH served as the loading control.

    查看 Topoisomerase 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

    IC50 & Target[1]

    Topoisomerase I

     

    体外研究
    (In Vitro)

    Topotecan Hydrochloride (SKF 104864A Hydrochloride) 以剂量和时间依赖性方式明显抑制人神经胶质瘤细胞和神经胶质瘤干细胞 (GSC) 的增殖。根据24 h的IC50值,选择 3 μM 的盐酸 Topotecan Hydrochloride 作为最佳给药浓度。此外,Topotecan Hydrochloride 诱导细胞周期停滞在 G0/G1 和 S 期并促进细胞凋亡。
    Topotecan Hydrochloride 以剂量依赖的方式抑制细胞活力。与对照组相比,2、20和40 μM的盐酸 Topotecan Hydrochloride 明显抑制细胞活力。Topotecan Hydrochloride 24 h 的IC50值为U251细胞2.73±0.25 μM,U87细胞2.95±0.23 μM,GSCs-U251 5.46±0.41 μM,GSCs-5.95±0.24 μM U87。故选择 3 μM盐酸托泊替康作为后续实验的最佳给药浓度[1]

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

    体内研究
    (In Vivo)

    NUB-7 转移模型,处理 14 天后处死 4 组动物。与对照组相比,与 PZ 相比,TP+PZ 处理的动物的低剂量节律性 (LDM) 盐酸 Topotecan Hydrochloride 和 TP+帕唑帕尼 (PZ) 肝脏重量显著降低。在属于除 TP+PZ 之外的所有组的小鼠的肝脏中可见微观肿瘤,证实了盐酸托泊替康+PZ 控制肝转移的能力。在之前的一项剂量反应研究中,与每周最大耐受剂量方案 (7.5 和 15 mg/kg) 相比,口服节律性托泊替康盐酸盐的每日剂量 (0.5、1.0 和 1.5 mg/kg) 导致微血管密度降低更多一种卵巢癌模型,但每天口服 1.5 mg/kg 盐酸托泊替康处理的小鼠表现出摄食量减少,抗肿瘤作用较弱[2]

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

    Clinical Trial
    分子量

    457.91

    Formula

    C23H24ClN3O5

    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    中文名称

    盐酸托泊替康;盐酸拓扑替康

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (218.38 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)

    H2O 中的溶解度 : 33.33 mg/mL (72.79 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1838 mL 10.9192 mL 21.8384 mL
    5 mM 0.4368 mL 2.1838 mL 4.3677 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 (sealed storage, away from moisture and light)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.46 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,此方案实验周期在半个月以上的动物实验酌情使用。

      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玉米油中,混合均匀。

    • 方案 二

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

      Solubility: ≥ 2.08 mg/mL (4.54 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 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

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.76%

    参考文献
    Cell Assay
    [1]

    The U251, U87, GSCs-U251 and GSCs-U87 cells are seeded at a density of 2×104 cells per well in 96-well plates separately, and incubated for 24 h. Cells are administered with Shikonin and Topotecan Hydrochloride (0.02, 0.2, 2, 20, 40 μM). After the treatment, 10 μL of cell counting kit-8 (CCK-8) is added into each well for additional 1-hour incubation at 37°C. The optical density (OD) is read with a microplate reader at 450 nm[1].

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

    Animal Administration
    [2]

    Mice[2]
    For subcutaneous xenograft studies, we used SK-N-BE, SH-SY5Y, KHOS, and RH30. 1×106 cells are implanted subcutaneously into the inguinal fat pad of each of nonobese diabetic/severe combined immune deficient (NOD/SCID) mice. When tumors reached 0.5 cm in diameter, the animals are randomized into 4 groups and treated daily by oral gavage. The animals are grouped as: Control group, LDM Topotecan group or LDM TP (1 mg/kg Topotecan), Pazopanib group or PZ (150 mg/kg Pazopanib) and combination group or TP + PZ (1 mg/kg Topotecan Hydrochloride + 150 mg/kg Pazopanib). To compare pulse Topotecan with LDM TP in KHOS osteosarcoma model, PZ is replaced by weekly oral dose of pulse Topotecan or Pulse TP (15 mg/kg Topotecan). The criteria for endpoint are tumor sizes exceeding 2.0 cm in diameter or animals showing signs of morbidity. The tumor sizes are measured on a daily basis until the endpoint or sacrifice. The long (D) and short diameters (d) are measured with calipers. Tumor volume (cm3) is calculated as V=0.5×D×d2. When the endpoint is reached or at the end of the treatment, the animals are sacrificed by cervical dislocation.

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

    参考文献

    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 (sealed storage, away from moisture and light)。-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
    H2O / DMSO 1 mM 2.1838 mL 10.9192 mL 21.8384 mL 54.5959 mL
    5 mM 0.4368 mL 2.1838 mL 4.3677 mL 10.9192 mL
    10 mM 0.2184 mL 1.0919 mL 2.1838 mL 5.4596 mL
    15 mM 0.1456 mL 0.7279 mL 1.4559 mL 3.6397 mL
    20 mM 0.1092 mL 0.5460 mL 1.0919 mL 2.7298 mL
    25 mM 0.0874 mL 0.4368 mL 0.8735 mL 2.1838 mL
    30 mM 0.0728 mL 0.3640 mL 0.7279 mL 1.8199 mL
    40 mM 0.0546 mL 0.2730 mL 0.5460 mL 1.3649 mL
    50 mM 0.0437 mL 0.2184 mL 0.4368 mL 1.0919 mL
    60 mM 0.0364 mL 0.1820 mL 0.3640 mL 0.9099 mL
    DMSO 80 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6824 mL
    100 mM 0.0218 mL 0.1092 mL 0.2184 mL 0.5460 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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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    目录号:
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