Cyclophosphamide(Synonyms: 环磷酰胺)

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Cyclophosphamide (Synonyms: 环磷酰胺) 纯度: ≥98.0%

Cyclophosphamide 是一种合成的 DNA Alkylator,在化学上与氮芥类有关,具有抗肿瘤及免疫抑制活性。

Cyclophosphamide(Synonyms: 环磷酰胺)

Cyclophosphamide Chemical Structure

CAS No. : 50-18-0

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Cyclophosphamide 相关产品

相关化合物库:

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  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Animal Disease Model Inducer Library

生物活性

Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic activity, a immunosuppressant.

IC50 & Target

DNA Alkylator[1]

体外研究
(In Vitro)

Cyclophosphamide induces outer membrane blebbing, leads to DNA fragmentation, as revealed by TUNEL staining of free 3′-OH DNA ends, and induces cleavage of the caspase 3 and caspase 7 substrate PARP in 9L/P450 cells. Bcl-2 expression fully blocks the activation of both initiator caspases as well as the effector caspase 3 in cells treated with activated Cyclophosphamide. Bcl-2 inhibits the cytotoxic effects but not the cytostatic effects of activated Cyclophosphamide[1]. Cyclophosphamide inhibits the AChE reversibly with an IC50 of 511 μM[2]. Carbon tetrachloride does not affect the direct cytotoxicity of cyclophosphamide or 4-hydroxycyclophosphamide to cells in culture[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Cyclophosphamide (injected i.p.;2mg/mouse in 0.1 mL PBS, in C3H mice bearing SW1 tumors) increases the percentage of cells that stained for CD3, CD4 or CD8 in both spleens and tumors[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six to eight-week old female C3H/HeN mice bearing SW1 tumors[4]
Dosage: 2 mg/mouse
Administration: Injected i.p.; 2mg/mouse in 0.1 mL PBS; 4 days
Result: Increased the percentage of cells that stained for CD3, CD4 or CD8 in both spleens and tumors.

Clinical Trial

分子量

261.09

Formula

C7H15Cl2N2O2P

CAS 号

50-18-0

中文名称

环磷酰胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

溶解性数据
In Vitro: 

DMSO : ≥ 38 mg/mL (145.54 mM)

H2O : 33.33 mg/mL (127.66 mM; Need ultrasonic)

* “≥” 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 3.8301 mL 19.1505 mL 38.3010 mL
5 mM 0.7660 mL 3.8301 mL 7.6602 mL
10 mM 0.3830 mL 1.9150 mL 3.8301 mL

*

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;该产品在溶液状态不稳定,建议您现用现配,即刻使用

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

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 50 mg/mL (191.50 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (9.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.58 mM,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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (9.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.58 mM,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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.58 mM,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 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Schwartz PS, et al. Cyclophosphamide induces caspase 9-dependent apoptosis in 9L tumor cells. Mol Pharmacol. 2001 Dec;60(6):1268-1279.

    [2]. al-Jafari AA, et al. Inhibition of human acetylcholinesterase by cyclophosphamide. Toxicology. 1995 Jan 19;96(1):1-6.

    [3]. Harris RN, et al. Carbon tetrachloride-induced increase in the antitumor activity of cyclophosphamide in mice: a pharmacokineticstudy. Cancer Chemother Pharmacol. 1984;12(3):167-72.

    [4]. Liu P, et al. Administration of cyclophosphamide changes the immune profile of tumor-bearing mice. J Immunother. 2010 Jan;33(1):53-9.

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