• <dfn id="q240u"></dfn>
    • Floxuridine (FUDR)

      別名: NSC 27640, Deoxyfluorouridine 中文名稱:氟尿苷

      Floxuridine (FUDR)是一種前體藥物,在體內(nèi)可迅速分解為5-fluorouracil。Floxuridine 可用于治療各種癌癥,特別是轉(zhuǎn)移到肝臟的癌癥。Floxuridine 可抑制 Poly(ADP-Ribose) polymerase、誘導(dǎo)DNA損傷和凋亡。Floxuridine 對HSV和CMV具有抗病毒作用。

      Floxuridine (FUDR) Chemical Structure

      Floxuridine (FUDR) Chemical Structure

      CAS: 50-91-9

      規(guī)格 價(jià)格 庫存 購買數(shù)量
      10mM (1mL in DMSO) 1270 現(xiàn)貨
      50mg 782.46 現(xiàn)貨
      200mg 2439.19 現(xiàn)貨
      更大包裝 有超大折扣

      400-668-6834

      [email protected]

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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(shí)間 活性描述 文獻(xiàn)信息(PMID)
      Colo-357 cells Function assay 100 μM 15 mins Activity at MRP5 in human Colo-357 cells assessed as 5-FdUMP accumulation at 100 uM after 15 mins
      L1210 mouse leukemia cells Growth inhibition assay 24 h Growth inhibition in L1210 mouse leukemia cells after 24 h treatment, IC50=0.0041 μM
      L1210 mouse leukemia cells Growth inhibition assay 48 h Growth inhibition in L1210 mouse leukemia cells after 48 hr treatment, IC50=0.00064 μM
      L1210 mouse leukemia cells Function assay 2 h Thymidylate synthase inhibition in L1210 mouse leukemia cells after 2 hr treatment, IC50=0.0079 μM
      LM cells Function assay 2 h Thymidylate synthase inhibition in thymidine kinase deficient LM cells after 2 hr treatment, IC50=5.4 μM
      L1210 cells Growth inhibition assay 72 h Cytostatic activity against mouse L1210 cells ATCC CCL219 assessed as growth reduction after 72 hrs, IC50=0.012 μM
      HL60 cells Growth inhibition assay 72 h Cytostatic activity against human HL60 cells ATCC CCL 240 assessed as growth reduction after 72 hrs, IC50=0.012 μM
      CCRF-CEM cells Growth inhibition assay 72 h Cytostatic activity against human CCRF-CEM cells ATCC CCL 119 assessed as growth reduction after 72 hrs, IC50=0.017 μM
      L1210 cells Growth inhibition assay 72 h Cytostatic activity in mouse L1210 cells assessed as inhibition of cell growth after 72 hrs, IC50=0.012 μM
      HL60 cells Growth inhibition assay 72 h Cytostatic activity in human HL60 cells assessed as inhibition of cell growth after 72 hrs, IC50=0.012 μM
      CCRF-CEM cells Growth inhibition assay 72 h Cytostatic activity in human CCRF-CEM cells assessed as inhibition of cell growth after 72 hrs, IC50=0.017 μM
      CCRF-CEM cells Function assay 48 h Anticancer activity against human CCRF-CEM cells after 48 hrs by sulforhodamine B assay, GI50=0.00631 μM
      K562 cells Function assay 48 h Anticancer activity against human K562 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM
      MOLT4 cells Function assay 48 h Anticancer activity against human MOLT4 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM
      RPMI8266 cells Function assay 48 h Anticancer activity against human RPMI8266 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM
      human SR cells Function assay 48 h Anticancer activity against human SR cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM
      A549 cells Function assay 48 h Anticancer activity against human A549 cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM
      EKVX cells Function assay 48 h Anticancer activity against human EKVX cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
      HOP62 cells Function assay 48 h Anticancer activity against human HOP62 cells after 48 hrs by sulforhodamine B assay, GI50=0.02512 μM
      HOP92 cells Function assay 48 h Anticancer activity against human HOP92 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM
      NCI-H226 cells Function assay 48 h Anticancer activity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay
      NCI-H23 Function assay 48 h Anticancer activity against human NCI-H23 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
      NCI-H322 Function assay 48 h Anticancer activity against human NCI-H322M cells after 48 hrs by sulforhodamine B assay, GI50=0.50119 μM
      NCI-H460 Function assay 48 h Anticancer activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay, GI50=0.50119 μM
      NCI-H522 Function assay 48 h Anticancer activity against human NCI-H522 cells after 48 hrs by sulforhodamine B assay, GI50=0.002 μM
      COLO205 cells Function assay 48 h Anticancer activity against human COLO205 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
      HCC2998 cells Function assay 48 h Anticancer activity against human HCC2998 cells after 48 hrs by sulforhodamine B assay, GI50=1.58489 μM
      HCT116 cells Function assay 48 h Anticancer activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.001 μM
      HCT15 cells Function assay 48 h Anticancer activity against human HCT15 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
      HT-29 cells Function assay 48 h Anticancer activity against human HT-29 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM
      KM12 cells Function assay 48 h Anticancer activity against human KM12 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
      SW620 cells Function assay 48 h Anticancer activity against human SW620 cells after 48 hrs by sulforhodamine B assay, GI50=6.30957 μM
      SF268 cells Function assay 48 h Anticancer activity against human SF268 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
      SF295 cells Function assay 48 h Anticancer activity against human SF295 cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM
      SF539 cells Function assay 48 h Anticancer activity against human SF539 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM
      SNB19 cells Function assay 48 h Anticancer activity against human SNB19 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM
      SNB75 cells Function assay 48 h Anticancer activity against human SNB75 cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM
      U251 cells Function assay 48 h Anticancer activity against human U251 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
      LOXIMVI cells Function assay 48 h Anticancer activity against human LOXIMVI cells after 48 hrs by sulforhodamine B assay, GI50=0.02512 μM
      MALME-3M cells Function assay 48 h Anticancer activity against human MALME-3M cells after 48 hrs by sulforhodamine B assay, GI50=7.94328 μM
      M14 cells Function assay 48 h Anticancer activity against human M14 cells after 48 hrs by sulforhodamine B assay, GI50=0.15849 μM
      SK-MEL-2 cells Function assay 48 h Anticancer activity against human SK-MEL-2 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
      SK-MEL-28 cells Function assay 48 h Anticancer activity against human SK-MEL-28 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM
      SK-MEL-5 cells Function assay 48 h Anticancer activity against human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM
      UACC257 cells Function assay 48 h Anticancer activity against human UACC257 cells after 48 hrs by sulforhodamine B assay, GI50=3.16228 μM
      UACC62 cells Function assay 48 h Anticancer activity against human UACC62 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM
      IGROV1 cells Function assay 48 h Anticancer activity against human IGROV1 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
      OVCAR-3 cells Function assay 48 h Anticancer activity against human OVCAR-3 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
      OVCAR4 cells Function assay 48 h Anticancer activity against human OVCAR4 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
      OVCAR5 cells Function assay 48 h Anticancer activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=6.30957 Μm
      OVCAR8 cells Function assay 48 h Anticancer activity against human OVCAR8 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
      SKOV3 cells Function assay 48 h Anticancer activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM
      786-0 cells Function assay 48 h Anticancer activity against human 786-0 cells after 48 hrs by sulforhodamine B assay, GI50=0.1 μM
      A498 cells Function assay 48 h Anticancer activity against human A498 cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM
      ACHN cells Function assay 48 h Anticancer activity against human ACHN cells after 48 hrs by sulforhodamine B assay, GI50=0.03162 μM
      Caki1 cells Function assay 48 h Anticancer activity against human Caki1 cells after 48 hrs by sulforhodamine B assay, GI50=0.03162 μM
      SN12C cells Function assay 48 h Anticancer activity against human SN12C cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM
      TK10 cells Function assay 48 h Anticancer activity against human TK10 cells after 48 hrs by sulforhodamine B assay, GI50=5.01187 μM
      UO31 cells Function assay 48 h Anticancer activity against human UO31 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
      PC3 cells Function assay 48 h Anticancer activity against human PC3 cells after 48 hrs by sulforhodamine B assay, GI50=0.31623 μM
      DU145 cells Function assay 48 h Anticancer activity against human DU145 cells after 48 hrs by sulforhodamine B assay, GI50=0.25119 μM
      MCF7 cells Function assay 48 h Anticancer activity against human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.00631 μM
      NCI/ADR-RES cells Function assay 48 h Anticancer activity against human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM
      MDA-MB-231 cells Function assay 48 h Anticancer activity against human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM
      Hs 578T cells Function assay 48 h Anticancer activity against human Hs 578T cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM
      MDA-MB-435 cells Function assay 48 h Anticancer activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=3.16228 μM
      MDA-N cells Function assay 48 h Anticancer activity against human MDA-N cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM
      BT549 cells Function assay 48 h Anticancer activity against human BT549 cells after 48 hrs by sulforhodamine B assay, GI50=1 μM
      T47D cells Function assay 48 h Anticancer activity against human T47D cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM
      HepG2 cells Cytotoxicity assay 72 h Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, EC50=18.84 μM
      A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay, EC50=9.74 μM
      LAC cells Cytotoxicity assay 72 h Cytotoxicity against human LAC cells after 72 hrs by MTT assay, EC50=32.09 μM
      HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, EC50=10.26 μM
      FM3A cells Function assay 2 days Cytostatic activity against mouse FM3A cells after 2 days by coulter counting analysis, IC50=0.0094 μM
      LLC cells Cytotoxicity assay 24 h Cytotoxicity against mouse LLC cells after 24 hrs by resazurin assay, IC50=14.2 μM
      LLC cells Cytotoxicity assay 72 h Cytotoxicity against mouse LLC cells after 72 hrs by resazurin assay, IC50=2 μM
      RAW264.7 cells Cytotoxicity assay 72 h Cytotoxicity against mouse RAW264.7 cells after 72 hrs by resazurin assay, IC50=30 μM
      A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by WST-8 assay, IC50=0.047 μM
      A2780 cells Cytotoxicity assay 5 days Cytotoxicity against human A2780 cells after 5 days by MTT assay, IC50=0.026 μM
      LMTK cells Cytotoxicity assay 5 days Cytotoxicity against thymidine kinase-deficient mouse LMTK cells after 5 days by MTT assay, IC50=4.5 μM
      A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells after 72 hrs by microplate reader method, IC50=0.0124 μM
      CEM cells Function assay 72 h Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting in presence of NBMPR, IC50=0.8 μM
      Hela cells Function assay 72 h Cytostatic activity against human HeLa cells after 72 hrs by cell counting, IC50=0.05 μM
      CEM/0 cells Function assay 72 h Cytostatic activity against human CEM/0 cells after 72 hrs by cell counting, IC50=0.022 μM
      L1210/0 cells Function assay 48 h Cytostatic activity against mouse L1210/0 cells after 48 hrs by cell counting, IC50=0.0009 μM
      MCF7 cells Cytotoxicity assay 72 h Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50=12.19 μM
      HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by SRB assay, IC50=6.5 μM
      HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.24 μM
      SW707 cells Proliferation assay 72 h Antiproliferative activity against human SW707 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=23.86 μM
      LoVo cells Proliferation assay 72 h Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by SRB method, IC50=19.07 μM
      BALB/3T3 cell Proliferation assay 72 h Antiproliferative activity against mouse BALB/3T3 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=23.9 μM
      HFF cells Function assay 72 h Antiparasitic activity against Toxoplasma gondii ATCC 50839 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.91 μM
      RXF393 cells Function assay 48 h Anticancer activity against human RXF393 cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM
      HL-60(TB) cells Function assay 48 h Anticancer activity against human HL-60(TB) cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM
      L1210 cells Function assay 15 mins Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 15 mins by liquid scintillation counting, IC50=0.0006 μM
      KB cells Cytotoxicity assay 72 h Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50=8.69 μM
      CCRF-CEM cell Growth inhibition assay Tested in vitro for the inhibition of cell growth of human T lymphoblastoid CCRF-CEM cell line (ATCC CCL 119), IC50=0.5 μM
      CCRF-CEM Growth inhibition assay In vitro concentration required for 50% inhibition of growth of human leukemia cell line CCRF-CEM with hPAP (0.2 unit/mL), GI50=0.0006 μM
      LNCaP cells Cytotoxicity assay Cytotoxic concentration in prostate specific antigen (PSA) producing human LNCaP cells, IC50=0.0692 μM
      TSU cells Cytotoxicity assay Cytotoxic concentration in non prostate specific antigen (PSA) producing human TSU cells, IC50=0.058 μM
      KBALB cell Cytotoxicity assay In vitro cell cytotoxicity against KBALB cell line (transformed fibroblast sarcoma cell line), CC50=6.00E-05 μM
      KBALB-STK cell Cytotoxicity assay In vitro cell cytotoxicity against KBALB-STK cell lines expressed in HSV-1 TK, IC50=8.80E-05 μM
      L5178Y cell Growth inhibition assay Comparative inhibition of L5178Y cell growth in vitro (concentration required for 50% inhibition), IC50=0.00076 μM
      L5178Y cells Function assay Inhibitory concentration of compound was calculated on L5178Y cells by [14C]Leu incorporation, IC50=2 μM
      HT1080 cells Function assay Cytostatic activity against human HT1080 cells by MTT assay, IC50=0.18 μM
      MDA-MB-231 cells Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells overexpressing urokinase plasminogen activator, IC50=0.21 μM
      human ACHN cells Function assay Anticancer activity against human ACHN cells by SRB assay, GI50=2.1 μM
      PC3 cells Function assay Anticancer activity against human PC3 cells by SRB assay, GI50=4.97 μM
      MDA-MB-231 cells Function assay Anticancer activity against human MDA-MB-231 cells by SRB assay, GI50=0.16 μM
      HeLa cells Function assay Cytostatic activity against human HeLa cells in presence of 20 uM thymidine, IC50=8.5 μM
      CCRFCEM cells Function assay Cytostatic activity against human CCRFCEM cells by MTT assay, IC50=0.29 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 Floxuridine (FUDR)是一種前體藥物,在體內(nèi)可迅速分解為5-fluorouracil。Floxuridine 可用于治療各種癌癥,特別是轉(zhuǎn)移到肝臟的癌癥。Floxuridine 可抑制 Poly(ADP-Ribose) polymerase、誘導(dǎo)DNA損傷和凋亡。Floxuridine 對HSV和CMV具有抗病毒作用。
      體外研究(In Vitro)
      體外研究活性 Floxuridine呈現(xiàn)對PEPT1比相應(yīng)的5'-O-單氨基酸酯前藥更高的親和力。[1] Floxuridine和Leucovorin聯(lián)用導(dǎo)致人T淋巴細(xì)胞白血病細(xì)胞生長的協(xié)同抑制作用。[2] Floxuridine顯著抑制[(3)H]-inosine和[(3)H]腺苷的的攝取(對照的60-70%),而它的氨基酸酯前體,包括纈氨酸,苯丙氨酸,Asp和賴氨酸酯,顯著下降抑制效力(對照的10-30%)。[3] Floxuridine在36天抑制細(xì)胞增值超過對照細(xì)胞的50%,細(xì)胞數(shù)量和初始細(xì)胞密度相比增加了4倍。Floxuridine導(dǎo)致對體外培養(yǎng)的人眼球筋膜囊成纖維細(xì)胞增殖長時(shí)間延長。[4] Floxuridine是一種理想的肝動(dòng)脈灌注(HAI)藥物,由于其半衰期短,陡峭的劑量反應(yīng)曲線,高總清除率和高肝提取。[5]
      NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
      NCT01042691 Completed
      Unresectable Colorectal Liver Metastases
      David Bartlett|The Pittsburgh Foundation|Sanofi|University of Pittsburgh
      May 2003 Phase 1
      NCT00695201 Completed
      Colon Cancer|Rectal Cancer
      Memorial Sloan Kettering Cancer Center|University of Medicine and Dentistry of New Jersey|Rutgers The State University of New Jersey|Sanofi
      August 2000 Phase 1
      • https://pubmed.ncbi.nlm.nih.gov/18652477/
      • https://pubmed.ncbi.nlm.nih.gov/2950995/
      • https://pubmed.ncbi.nlm.nih.gov/16462026/
      • https://pubmed.ncbi.nlm.nih.gov/1386726/
      • https://pubmed.ncbi.nlm.nih.gov/19383854/

      化學(xué)信息&溶解度

      分子量 246.19 分子式

      C9H11FN2O5

      CAS號 50-91-9 SDF Download Floxuridine (FUDR) SDF
      Smiles C1C(C(OC1N2C=C(C(=O)NC2=O)F)CO)O
      儲存條件(自收到貨起)

      體外溶解度
      批次:

      DMSO : 49 mg/mL ( (199.03 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO)

      Water : 49 mg/mL (199.03 mM)

      Ethanol : 10 mg/mL (40.61 mM)

      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(dòng)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(dòng)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(dòng)物的藥量)

      mg/kg g μL

      第二步:請輸入動(dòng)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。

      技術(shù)支持

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