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    • Cyclophosphamide Monohydrate

      別名: NSC-26271 Monohydrate

      Cyclophosphamide Monohydrate是一種氮芥類烷化劑,使烷基連接到DNA的鳥嘌呤堿基。與DNA交聯(lián),造成DNA鏈斷裂,引起突變。具有細(xì)胞毒性作用。Cyclophosphamide?(NSC-26271) Monohydrate 可用于誘導(dǎo)貧血動物模型。

      Cyclophosphamide Monohydrate Chemical Structure

      Cyclophosphamide Monohydrate Chemical Structure

      CAS: 6055-19-2

      規(guī)格 價格 庫存 購買數(shù)量
      50mg 785.09 現(xiàn)貨
      200mg 2375.1 現(xiàn)貨
      1g 5487.3 現(xiàn)貨
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      Cyclophosphamide Monohydrate相關(guān)產(chǎn)品

      細(xì)胞實驗數(shù)據(jù)示例

      細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息(PMID)
      HL60 cells Cytotoxicity assay Cytotoxicity against human HL60 cells by MTT assay, IC50=8.79 μM 20850303
      K562 Antiproliferative assay 48 hr Antiproliferative activity against Homo sapiens (human) K562 cells after 48 hr by MTT assay, IC50 = 0.153 μM. ChEMBL
      MCF7 Cytotoxicity assay 48 hr Cytotoxicity against Homo sapiens (human) MCF7 cells after 48 hr by SRB assay, IC50 = 10 mM. 19372630
      HepG2 Cytotoxicity assay 48 hr Cytotoxicity against Homo sapiens (human) HepG2 cells after 48 hr by MTT assay, IC50 = 0.24 μM. ChEMBL
      U2932 Antitumor assay 50 mg/kg 5 consecutive days Antitumor activity against human U2932 cells xenografted in SCID mouse assessed as reduction in tumor burden at 50 mg/kg, ip administered for 5 consecutive days measured up to day 40 post cell injection 28605593
      MDA-MB-231 Cytotoxicity assay 48 hr Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells after 48 hr by MTT assay, IC50 = 0.09 μM. ChEMBL
      K562 Cytotoxicity assay 48 hr Cytotoxicity against Homo sapiens (human) K562 cells after 48 hr by MTT assay, IC50 = 0.15 μM. ChEMBL
      NCI-H522 Antitumor assay 50 mg/kg 28 days Antitumor activity against human NCI-H522 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 50 mg/kg, ig administered once daily for 28 days relative to control 28092860
      U87MG Anticancer assay 80 mg/kg 6 days Anticancer activity against human U87MG cells xenografted in athymic mouse assessed as tumor suppression at 80 mg/kg, iv Q2D for 6 days 21106377
      MX1 Antitumor assay 120 mg/kg up to 3 weeks Antitumor activity against human MX1 cells xenografted in nude mouse adjuvant model assessed as increase in mouse survival time at 120 mg/kg, po BID measured up to 3 weeks 20726512
      U87 MG Antitumor assay 80 mg/kg Antitumor activity in human U87 MG cells xenografted mouse at 80 mg/kg, iv administered in Q2D x 5 schedule 18450456
      B-cells Immunosuppressive assay 100 mg/kg 8 days Immunosuppressive activity against MAV-1 infected BALB/c mouse assessed as B cells suppression at 100 mg/kg, ip treated 8 days before infection for 4 weeks measured 14 days post infection by flow cytometry 18268085
      T-cells Immunosuppressive assay 100 mg/kg 8 days Immunosuppressive activity against MAV-1 infected BALB/c mouse assessed as T cells suppression at 100 mg/kg, ip treated 8 days before infection for 4 weeks measured 14 days post infection by flow cytometry 18268085
      BALB/c 3T3 Cytotoxicity assay In vitro cytotoxicity against BALB/c 3T3 cells, IC50 = 37.6 μM. 7877150
      BALB/c 3T3 cells Cytotoxicity assay In vitro cytotoxicity was evaluated in mouse embryo BALB/c 3T3 cells, IC50=37.6 μM 9873412
      點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

      生物活性

      產(chǎn)品描述 Cyclophosphamide Monohydrate是一種氮芥類烷化劑,使烷基連接到DNA的鳥嘌呤堿基。與DNA交聯(lián),造成DNA鏈斷裂,引起突變。具有細(xì)胞毒性作用。Cyclophosphamide?(NSC-26271) Monohydrate 可用于誘導(dǎo)貧血動物模型。
      體外研究(In Vitro)
      體外研究活性

      Cyclophosphamide (CY)是一種化學(xué)治療劑,對免疫系統(tǒng)具有劑量依賴性雙重作用。Cyclophosphamide治療增強(qiáng)細(xì)胞凋亡,并降低調(diào)控T細(xì)胞的穩(wěn)態(tài)增殖。Cyclophosphamide下調(diào)GITR和FoxP3的表達(dá),其涉及T(REGs)的抑制活性。[1]

      Cyclophosphamide增加原代人肝細(xì)胞培養(yǎng)物中CYP3A4,CYP2C8,和 CYP2C9蛋白水平,從而提高培養(yǎng)的肝細(xì)胞中它們自身的4-羥基化比率。[2]

      代謝活化存在下,Cyclophosphamide使Salmonella tryphimurium的堿基對取代菌株產(chǎn)生突變,但是在 E. coli顯色測試中顯示為陰性。代謝活化存在下,Cyclophosphamide能夠使各種人工培養(yǎng)的細(xì)胞中產(chǎn)生基因突變,染色體畸變,微核和姐妹染色單體互換,并且代謝活化不存在時,會產(chǎn)生姐妹染色單體互換。[3]

      實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
      Western blot PTEN / pAkt / Caspase 3 / GAPDH Caspase 3 / Cleaved-Caspase 3 / Cleaved-PARP / Tubulin Nuclear AIF / Cytosolic AIF / TBP / GAPDH LC3B I / LC3B II / GAPDH 23874108
      Growth inhibition assay Cell Viability Tumor Volume Tumor Volume 31429028
      IHC tumor cell invasion TUNEL / Caspase 3 PTEN / pAkt / PCNA ovary of mice Caspase-3 23874108
      Immunofluorescence pAKT / pERK Ki-67 / UPK3 / KRT5 / pERK Ki-67 / KRT14 / KRT5 autophagy levels 31654636
      體內(nèi)研究(In Vivo)
      體內(nèi)研究活性

      Cyclophosphamide會使大鼠,小鼠和中國倉鼠體內(nèi)產(chǎn)生染色體損傷和微核,并且在小鼠斑點(diǎn)試驗和Muta小鼠轉(zhuǎn)基因lacZ構(gòu)建體中產(chǎn)生基因突變。[3]

      Cyclophosphamide,以確定的順序加入到GM-CSF-分泌的,neu-表達(dá)的全細(xì)胞疫苗中,能夠增強(qiáng)疫苗的潛在作用以延緩neu轉(zhuǎn)基因小鼠體內(nèi)的腫瘤生長。Cyclophosphamide通過增強(qiáng)疫苗的功效,而不是通過對癌細(xì)胞的直接細(xì)胞溶解作用發(fā)揮它的作用。[4]

      NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
      NCT06186700 Active not recruiting
      Breast Cancer Female
      Mansoura University
      December 25 2023 Phase 2
      NCT06085742 Recruiting
      Breast Cancer
      University of Illinois at Chicago
      November 22 2023 Phase 2
      NCT05800041 Not yet recruiting
      Gout Tophus
      RenJi Hospital|Westlake Therapeutics
      April 10 2023 Early Phase 1
      • [1]https://pubmed.ncbi.nlm.nih.gov/15591121/
      • [2]https://pubmed.ncbi.nlm.nih.gov/9157990/
      • [3]https://pubmed.ncbi.nlm.nih.gov/7623863/
      • [4]https://pubmed.ncbi.nlm.nih.gov/11325840/
      • [5]https://pubmed.ncbi.nlm.nih.gov/35409194/
      • [6]https://pubmed.ncbi.nlm.nih.gov/34385713/
      • [7]https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7123643/
      • [8]https://pubmed.ncbi.nlm.nih.gov/21530682/

      化學(xué)信息&溶解度

      分子量 279.1 分子式

      C7H15Cl2N2O2P.H2O

      CAS號 6055-19-2 SDF Download Cyclophosphamide Monohydrate SDF
      Smiles C1CNP(=O)(OC1)N(CCCl)CCCl.O
      儲存條件(自收到貨起)

      體外溶解度
      批次:

      DMSO : 55 mg/mL ( (197.06 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO)

      Water : 55 mg/mL (197.06 mM)

      Ethanol : 55 mg/mL (197.06 mM)

      摩爾濃度計算器

      體內(nèi)溶解配方
      批次:

      現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑

      動物體內(nèi)配方計算器

      實驗計算

      摩爾濃度計算器

      質(zhì)量 濃度 體積 分子量

      動物體內(nèi)配方計算器(澄清溶液)

      第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)

      mg/kg g μL

      第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)

      % DMSO % % Tween 80 % ddH2O
      %DMSO %

      計算結(jié)果:

      工作液濃度: mg/ml;

      DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);

      體內(nèi)配方配制方法:μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。

      體內(nèi)配方配制方法:μL DMSO母液,加入μL Corn oil,混勻澄清。

      注意:1. 首先保證母液是澄清的;
      2.一定要按照順序依次將溶劑加入,進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。

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      常見問題及建議解決方法

      問題 1:
      Why does it show no activity in vitro assays?

      回答:
      The activity of this compound in vitro is controversial and has not been fully determined. It is a prodrug and may need Cytochrome P450 to convert it to the active form: 4-hydroxy cyclophosphamide. It is widely used in vivo, if you are going to use it in vitro, you may need to supplement Cytochrome P450 exogenously.

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