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    • Mercaptopurine (6-MP)

      別名: 6-MP 中文名稱:巰嘌呤

      Mercaptopurine (6-MP)是一種廣泛應(yīng)用于治療白血病的藥物,也是一種免疫抑制藥,通過整合巰基嘌呤的甲基轉(zhuǎn)移酶代謝產(chǎn)物進(jìn)入DNA和RNA抑制新創(chuàng)嘌呤合成。

      Mercaptopurine (6-MP) Chemical Structure

      Mercaptopurine (6-MP) Chemical Structure

      CAS: 50-44-2

      規(guī)格 價格 庫存 購買數(shù)量
      10mM (1mL in DMSO) 818.52 現(xiàn)貨
      50mg 784.59 現(xiàn)貨
      1g 5487.3 現(xiàn)貨
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      細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

      細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息(PMID)
      mouse J774.A1 cells Proliferation assay 3 days Antiproliferative activity against mouse J774.A1 cells after 3 days by MTT conversion assay, IC50=0.003 μM
      HEK293 cells Proliferation assay 3 days Antiproliferative activity against HEK293 cells after 3 days by MTT conversion assay, IC50=0.007 μM
      mouse J774 cells Proliferation assay 72 h Antiproliferative activity against mouse J774 cells assessed as reduction of cell growth after 72 hrs by MTT method, IC50=0.003 μM
      human PBMC Function assay 4 days Inhibition of T cell mitogen-induced blastogenesis in human PBMC after 4 days, IC50=0.1495 μM
      HeLa cells Cytotoxicity assay 48 h Cytotoxicity against human HeLa cells at lag phase of growth after 48 hrs by MTT assay, IC50=2.9 μM
      A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells at lag phase of growth after 48 hrs by MTT assay, IC50=47 μM
      MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells at lag phase of growth after 48 hrs by MTT assay, IC50=1.4 μM
      MT4 cells Cytotoxicity assay 96 h Cytotoxicity against human MT4 cells infected with HTLV-1 after 96 hrs by MTT assay, CC50=0.1 μM
      CCRF-CEM cells Proliferation assay 96 h Antiproliferative activity against human CCRF-CEM cells after 96 hrs by MTT assay, CC50=1 μM
      WIL2-NS cells Proliferation assay 96 h Antiproliferative activity against human WIL2-NS cells after 96 hrs by MTT assay, CC50=3 μM
      CCRF-SB cells Proliferation assay 96 h Antiproliferative activity against human CCRF-SB cells after 96 hrs by MTT assay, CC50=1.1 μM
      human DU145 cells Proliferation assay 96 h Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay, CC50=2 μM
      human HepG2 cells Proliferation assay 96 h Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay, CC50=8 μM
      MCF7 cells Proliferation assay 96 h Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay, CC50=3.2 μM
      SK-MEL-28 cells Proliferation assay 96 h Antiproliferative activity against human SK-MEL-28 cells after 96 hrs by MTT assay, CC50=15 μM
      mouse S49 cells Cytotoxicity assay 72 h Cytotoxicity against wild type mouse S49 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay, EC50=8 μM
      A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50=47 μM
      MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay, IC50=1.4 μM
      HeLa cells Cytotoxicity assay 48 h Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay, IC50=2.9 μM
      WEHI164 cells Proliferation assay 3 days Antiproliferative activity against mouse WEHI164 cells after 3 days by MTT conversion assay, IC50=0.015 μM
      WEHI164 cells Proliferation assay 72 h Antiproliferative activity against mouse WEHI164 cells assessed as reduction of cell growth after 72 hrs by MTT method, IC50=0.017 μM
      L1210 leukemia cells Function assay Inhibitory concentration on multidrug-resistant L1210 leukemia cells, IC50=0.024 μM
      MT4 cells Proliferation assay Antiproliferative activity against human MT4 cells by MTT assay, IC50=0.1 μM
      human CCRF-CEM cells Proliferation assay Antiproliferative activity against human CCRF-CEM cells by MTT assay, IC50=1 μM
      human CCRF-SB cells Proliferation assay Antiproliferative activity against human CCRF-SB cells by MTT assay, IC50=1 μM
      human SK-MEL-28 cells Proliferation assay Antiproliferative activity against human SK-MEL-28 cells by MTT assay, IC50=15 μM
      human MCF7 cells Proliferation assay Antiproliferative activity against human MCF7 cells by MTT assay, IC50=3 μM
      human HepG2 cells Proliferation assay Antiproliferative activity against human HepG2 cells by MTT assay, IC50=8 μM
      human DU145 cells Proliferation assay Antiproliferative activity against human DU145 cells by MTT assay, IC50=2 μM
      MCF7 cells Cytotoxicity assay Cytotoxicity against human MCF7 cells, IC50=2.79 μM
      Colo-357 cells Cytotoxicity assay Cytotoxicity against human Colo-357 cells by crystal violet staining, IC50=6.12 μM
      Aspc-1 cells Cytotoxicity assay Cytotoxicity against human Aspc-1 cells by crystal violet staining, IC50=2.45 μM
      Patu-02 cells Cytotoxicity assay Cytotoxicity against human Patu-02 cells by crystal violet staining, IC50=9.69 μM
      Patu-T cells Cytotoxicity assay Cytotoxicity against human Patu-T cells by crystal violet staining, IC50=4.09 μM
      Patu-S cells Cytotoxicity assay Cytotoxicity against human Patu-S cells by crystal violet staining, IC50=11.07 μM
      T3M4 cells Cytotoxicity assay Cytotoxicity against human T3M4 cells by crystal violet staining, IC50=2.63 μM
      human PANC1 cells Cytotoxicity assay Cytotoxicity against human PANC1 cells by crystal violet staining, IC50=6.39 μM
      human DAN-G cells Cytotoxicity assay Cytotoxicity against human DAN-G cells by crystal violet staining, IC50=4.06 μM
      WIL-2NS cells Proliferation assay Antiproliferative activity against human WIL-2NS cells by MTT assay, IC50=3 μM
      點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

      生物活性

      產(chǎn)品描述 Mercaptopurine (6-MP)是一種廣泛應(yīng)用于治療白血病的藥物,也是一種免疫抑制藥,通過整合巰基嘌呤的甲基轉(zhuǎn)移酶代謝產(chǎn)物進(jìn)入DNA和RNA抑制新創(chuàng)嘌呤合成。
      靶點(diǎn)
      PRPP Amidotransferase [2]
      體外研究(In Vitro)
      體外研究活性

      Mercaptopurine被廣泛用于治療惡性腫瘤,風(fēng)濕性疾病,皮膚病,炎癥性腸道疾病,以及實(shí)體器官移植排斥。[1] Mercaptopurine通過抑制磷酸核糖焦磷酸酰胺轉(zhuǎn)移酶(PRPP酰胺轉(zhuǎn)移酶)而抑制嘌呤核苷和代謝。PRPP酰胺轉(zhuǎn)移酶是嘌呤合成的限速酶。它會改變RNA和DNA的合成和功能。Mercaptopurine干擾核苷酸的互變和糖蛋白的合成。[2]

      NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
      NCT04770922 Completed
      Acute Lymphoblastic Leukemia Pediatric|Adverse Drug Event
      Cipherome Inc.|Stanford University
      February 23 2021 --
      NCT03022747 Unknown status
      Lymphoblastic Leukemia Acute Childhood
      Vastra Gotaland Region
      January 2017 Phase 2
      • https://pubmed.ncbi.nlm.nih.gov/18506437/
      • https://pubmed.ncbi.nlm.nih.gov/7191632/

      化學(xué)信息&溶解度

      分子量 152.18 分子式

      C5H4N4S

      CAS號 50-44-2 SDF Download Mercaptopurine (6-MP) SDF
      Smiles C1=NC2=C(N1)C(=S)N=CN2
      儲存條件(自收到貨起)

      體外溶解度
      批次:

      DMSO : 30 mg/mL ( (197.13 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO)

      Water : Insoluble

      Ethanol : Insoluble

      摩爾濃度計(jì)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(jì)算器

      實(shí)驗(yàn)計(jì)算

      摩爾濃度計(jì)算器

      質(zhì)量 濃度 體積 分子量

      動物體內(nèi)配方計(jì)算器(澄清溶液)

      第一步:請輸入基本實(shí)驗(yàn)信息(考慮到實(shí)驗(yàn)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(jì)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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