2. Cell Cycle/DNA Damage
  3. G-quadruplex
  4. Nemorubicin

Nemorubicin  (Synonyms: 奈莫柔比星; Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243)

目录号: HY-15794 纯度: 96.84%
COA 产品使用指南

摩尔计算器

Nemorubicin (Methoxymorpholinyl doxorubicin) 是一种具有有效抗肿瘤活性的 Doxorubicin 衍生物。Nemorubicin 对多药耐药表型的多种肿瘤细胞系具有细胞毒性。 Nemorubicin 不仅插入到双链 DNA 中，而且产生 G-四联体 G-quadruplex 重要的配体，使其结构稳定。 Nemorubicin 需要完整的核苷酸切除修复系统才能发挥其活性。

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Nemorubicin Chemical Structure

Nemorubicin Chemical Structure

CAS No. : 108852-90-0

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规格 价格 是否有货 数量
1 mg ￥590
In-stock
5 mg ￥1450
In-stock
10 mg ￥2320
In-stock
25 mg ￥3980
In-stock
50 mg ￥5850
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Other Forms of Nemorubicin:

Nemorubicin 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity[1][2][3][4].

体外研究
(In Vitro)

Nemorubicin has antitumor activity, with IC70s of 578 nM, 468 nM, 193 nM, 191 nM, 68 nM, and 131 ± 9 nM for HT-29, A2780, DU145, EM-2, Jurkat and CEM cell lines, respectively[1].
Nemorubicin is CYP3A-activated anticancer prodrug, which can produce a more cytotoxic metabolite, PNU-159682[1][2].
Nemorubicin acts through nucleotide excision repair (NER) system to exert its activity. Nemorubicin (0-0.3 μM) is more active in the L1210/DDP cells with intact NER than in the XPG-deficient L1210/0 cells. Cells resistant to nemorubicin show increased sensitivity to UV damage[3].
Nemorubicin is cytotoxic to 9L/3A4 cells, with an IC50 of 0.2 nM, 120-fold lower than that of P450-deficient 9L cells (IC50, 23.9 nM). Nemorubicin also potently inhibits Adeno-3A4 infected U251 cells with IC50 of 1.4 nM. P450 reductase overexpression enhances cytotoxicity of Nemorubicin[4].

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

Nemorubicin 相关抗体:
体内研究
(In Vivo)

Nemorubicin is converted to PNU-159682 by human liver cytochrome P450 (CYP) 3A4 in rat, mouse, and dog liver microsomes[2]. Nemorubicin (60 µg/kg) induces sifnificant tumor growth delay in scid mice bearing 9L/3A4 tumors, but shows no obvious effect on the tumor growth delay of 9L tumors in mice by i.v. or intratumoral injection (i.t.). Nemorubicin (40 µg/kg, i.p.) exhibits no antitumor activity and no host toxicity in mice bearing 9L/3A4 tumors[4].

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

643.64

Formula

C32H37NO13
CAS 号
性状

固体

颜色

Orange to reddish brown

中文名称

奈莫柔比星
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 65 mg/mL (100.99 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 1.5537 mL 7.7683 mL 15.5366 mL
5 mM 0.3107 mL 1.5537 mL 3.1073 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 (protect from light)。-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

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: ≥ 3.25 mg/mL (5.05 mM); 澄清溶液

    此方案可获得 ≥ 3.25 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 32.5 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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 97.80% ee.: 100.00%

COA (276 KB) HNMR (218 KB) LCMS (329 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[4]

9L and CHO cells are plated in triplicate wells of a 96-well plate at 3000 cells per well 24 hr prior to drug treatment. Cells are treated with various concentrations of Nemorubicin or IFA for 4d. Cells are then stained with crystal violet (A595) and relative cell survival is calculated. IC50 values are determined from a semi-logarithmic graph of the data points using Prism 4[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4]

9L and 9L/3A4 cells are grown as solid tumors in male ICR/Fox Chase SCID mice. Cells cultured in DMEM medium to 75% confluence are trypsinized and washed in PBS and then adjusted to 2 × 107 cells/mL of FBS-free DMEM. Four-week-old SCID mice (18-20 g) are implanted with either 9L or 9L/3A4 tumor cells by injection of 4 × 106 cells/0.2 mL of cell suspension, s.c. on each hind flank. Tumor sizes (length and width) are measured twice a week using Vernier calipers beginning 7d after tumor implantation. When the average tumor size reach 300 to 400 mm3, Nemorubicin dissolved in PBS is administered by tail vein injection (i.v.) or by direct intratumoral (i.t.) injection (three injections spaced 7 d apart, each at 60 µg Nemorubicin per kg body weight). Intratumoral injections are performed using a syringe pump set a 1 µL/s with a 30-gauge needle. Each i.t. treatment dose is divided into three injections per tumor, with the injected volume set at 50 µL per tumor per 25 g mouse. Thus, for a 30 g mouse, a total of 120 µL of 15 µg/mL of Nemorubicin solution is administered: 20 µL per site × 3 sites per tumor × 2 tumors/mouse. Drug-free controls are injected i.t. with the same vol of PBS. In some experiments, Nemorubicin is administered by i.p. injection at 40 or 60 µg/kg body weight. Tumor sizes and body weights are measured twice/wk for the duration of the study. Tumor volumes are calculated using the formula: V = π/6 (L × W)3/2. Percent tumor regression is calculated as 100 × (V1-V2)/V1, where V1 is the tumor vol on the day of drug treatment and V2 is the vol on the day when the largest the decrease in tumor size is seen following drug treatment. Tumor doubling time is calculated as the time required for tumors to double in vol after drug treatment[4].

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

Nemorubicin 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 (protect from light)。-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 1.5537 mL 7.7683 mL 15.5366 mL 38.8416 mL
5 mM 0.3107 mL 1.5537 mL 3.1073 mL 7.7683 mL
10 mM 0.1554 mL 0.7768 mL 1.5537 mL 3.8842 mL
15 mM 0.1036 mL 0.5179 mL 1.0358 mL 2.5894 mL
20 mM 0.0777 mL 0.3884 mL 0.7768 mL 1.9421 mL
25 mM 0.0621 mL 0.3107 mL 0.6215 mL 1.5537 mL
30 mM 0.0518 mL 0.2589 mL 0.5179 mL 1.2947 mL
40 mM 0.0388 mL 0.1942 mL 0.3884 mL 0.9710 mL
50 mM 0.0311 mL 0.1554 mL 0.3107 mL 0.7768 mL
60 mM 0.0259 mL 0.1295 mL 0.2589 mL 0.6474 mL
80 mM 0.0194 mL 0.0971 mL 0.1942 mL 0.4855 mL
100 mM 0.0155 mL 0.0777 mL 0.1554 mL 0.3884 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:

Nemorubicin108852-90-0Methoxymorpholinyl doxorubicin FCE 23762 PNU 152243奈莫柔比星FCE23762FCE 23762FCE-23762PNU152243PNU 152243PNU-152243G-quadruplexInhibitorinhibitorinhibit

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