Floxuridine (FUDR)

别名: NSC 27640, Deoxyfluorouridine 中文名称:氟尿苷

Floxuridine (FUDR)是一种前体药物,在体内可迅速分解为5-fluorouracil。Floxuridine 可用于治疗各种癌症,特别是转移到肝脏的癌症。Floxuridine 可抑制 Poly(ADP-Ribose) polymerase、诱导DNA损伤和凋亡。Floxuridine 对HSV和CMV具有抗病毒作用。

Floxuridine (FUDR) Chemical Structure

Floxuridine (FUDR) Chemical Structure

CAS: 50-91-9

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 647.01 现货
50mg RMB 782.46 现货
200mg RMB 2439.19 现货
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批次: 纯度: 99.99%
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Floxuridine (FUDR)相关产品

DNA/RNA Synthesis抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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 20930123
L1210 mouse leukemia cells Growth inhibition assay 24 h Growth inhibition in L1210 mouse leukemia cells after 24 h treatment, IC50=0.0041 μM 11728193
L1210 mouse leukemia cells Growth inhibition assay 48 h Growth inhibition in L1210 mouse leukemia cells after 48 hr treatment, IC50=0.00064 μM 11728193
L1210 mouse leukemia cells Function assay 2 h Thymidylate synthase inhibition in L1210 mouse leukemia cells after 2 hr treatment, IC50=0.0079 μM 11728193
LM cells Function assay 2 h Thymidylate synthase inhibition in thymidine kinase deficient LM cells after 2 hr treatment, IC50=5.4 μM 11728193
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 17997319
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 17997319
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 17997319
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 18078757
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 18078757
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 18078757
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 19744858
K562 cells Function assay 48 h Anticancer activity against human K562 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM 19744858
MOLT4 cells Function assay 48 h Anticancer activity against human MOLT4 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM 19744858
RPMI8266 cells Function assay 48 h Anticancer activity against human RPMI8266 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM 19744858
human SR cells Function assay 48 h Anticancer activity against human SR cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM 19744858
A549 cells Function assay 48 h Anticancer activity against human A549 cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM 19744858
EKVX cells Function assay 48 h Anticancer activity against human EKVX cells after 48 hrs by sulforhodamine B assay, GI50=10 μM 19744858
HOP62 cells Function assay 48 h Anticancer activity against human HOP62 cells after 48 hrs by sulforhodamine B assay, GI50=0.02512 μM 19744858
HOP92 cells Function assay 48 h Anticancer activity against human HOP92 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM 19744858
NCI-H226 cells Function assay 48 h Anticancer activity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay 19744858
NCI-H23 Function assay 48 h Anticancer activity against human NCI-H23 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM 19744858
NCI-H322 Function assay 48 h Anticancer activity against human NCI-H322M cells after 48 hrs by sulforhodamine B assay, GI50=0.50119 μM 19744858
NCI-H460 Function assay 48 h Anticancer activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay, GI50=0.50119 μM 19744858
NCI-H522 Function assay 48 h Anticancer activity against human NCI-H522 cells after 48 hrs by sulforhodamine B assay, GI50=0.002 μM 19744858
COLO205 cells Function assay 48 h Anticancer activity against human COLO205 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM 19744858
HCC2998 cells Function assay 48 h Anticancer activity against human HCC2998 cells after 48 hrs by sulforhodamine B assay, GI50=1.58489 μM 19744858
HCT116 cells Function assay 48 h Anticancer activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.001 μM 19744858
HCT15 cells Function assay 48 h Anticancer activity against human HCT15 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM 19744858
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 19744858
KM12 cells Function assay 48 h Anticancer activity against human KM12 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM 19744858
SW620 cells Function assay 48 h Anticancer activity against human SW620 cells after 48 hrs by sulforhodamine B assay, GI50=6.30957 μM 19744858
SF268 cells Function assay 48 h Anticancer activity against human SF268 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM 19744858
SF295 cells Function assay 48 h Anticancer activity against human SF295 cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM 19744858
SF539 cells Function assay 48 h Anticancer activity against human SF539 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM 19744858
SNB19 cells Function assay 48 h Anticancer activity against human SNB19 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM 19744858
SNB75 cells Function assay 48 h Anticancer activity against human SNB75 cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM 19744858
U251 cells Function assay 48 h Anticancer activity against human U251 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM 19744858
LOXIMVI cells Function assay 48 h Anticancer activity against human LOXIMVI cells after 48 hrs by sulforhodamine B assay, GI50=0.02512 μM 19744858
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 19744858
M14 cells Function assay 48 h Anticancer activity against human M14 cells after 48 hrs by sulforhodamine B assay, GI50=0.15849 μM 19744858
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 19744858
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 19744858
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 19744858
UACC257 cells Function assay 48 h Anticancer activity against human UACC257 cells after 48 hrs by sulforhodamine B assay, GI50=3.16228 μM 19744858
UACC62 cells Function assay 48 h Anticancer activity against human UACC62 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM 19744858
IGROV1 cells Function assay 48 h Anticancer activity against human IGROV1 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM 19744858
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 19744858
OVCAR4 cells Function assay 48 h Anticancer activity against human OVCAR4 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM 19744858
OVCAR5 cells Function assay 48 h Anticancer activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=6.30957 Μm 19744858
OVCAR8 cells Function assay 48 h Anticancer activity against human OVCAR8 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM 19744858
SKOV3 cells Function assay 48 h Anticancer activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM 19744858
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 19744858
A498 cells Function assay 48 h Anticancer activity against human A498 cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM 19744858
ACHN cells Function assay 48 h Anticancer activity against human ACHN cells after 48 hrs by sulforhodamine B assay, GI50=0.03162 μM 19744858
Caki1 cells Function assay 48 h Anticancer activity against human Caki1 cells after 48 hrs by sulforhodamine B assay, GI50=0.03162 μM 19744858
SN12C cells Function assay 48 h Anticancer activity against human SN12C cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM 19744858
TK10 cells Function assay 48 h Anticancer activity against human TK10 cells after 48 hrs by sulforhodamine B assay, GI50=5.01187 μM 19744858
UO31 cells Function assay 48 h Anticancer activity against human UO31 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM 19744858
PC3 cells Function assay 48 h Anticancer activity against human PC3 cells after 48 hrs by sulforhodamine B assay, GI50=0.31623 μM 19744858
DU145 cells Function assay 48 h Anticancer activity against human DU145 cells after 48 hrs by sulforhodamine B assay, GI50=0.25119 μM 19744858
MCF7 cells Function assay 48 h Anticancer activity against human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.00631 μM 19744858
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 19744858
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 19744858
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 19744858
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 19744858
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 19744858
BT549 cells Function assay 48 h Anticancer activity against human BT549 cells after 48 hrs by sulforhodamine B assay, GI50=1 μM 19744858
T47D cells Function assay 48 h Anticancer activity against human T47D cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM 19744858
HepG2 cells Cytotoxicity assay 72 h Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, EC50=18.84 μM 19917528
A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay, EC50=9.74 μM 19917528
LAC cells Cytotoxicity assay 72 h Cytotoxicity against human LAC cells after 72 hrs by MTT assay, EC50=32.09 μM 19917528
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, EC50=10.26 μM 19917528
FM3A cells Function assay 2 days Cytostatic activity against mouse FM3A cells after 2 days by coulter counting analysis, IC50=0.0094 μM 21330014
LLC cells Cytotoxicity assay 24 h Cytotoxicity against mouse LLC cells after 24 hrs by resazurin assay, IC50=14.2 μM 21536448
LLC cells Cytotoxicity assay 72 h Cytotoxicity against mouse LLC cells after 72 hrs by resazurin assay, IC50=2 μM 21536448
RAW264.7 cells Cytotoxicity assay 72 h Cytotoxicity against mouse RAW264.7 cells after 72 hrs by resazurin assay, IC50=30 μM 21536448
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 22248856
A2780 cells Cytotoxicity assay 5 days Cytotoxicity against human A2780 cells after 5 days by MTT assay, IC50=0.026 μM 22738636
LMTK cells Cytotoxicity assay 5 days Cytotoxicity against thymidine kinase-deficient mouse LMTK cells after 5 days by MTT assay, IC50=4.5 μM 22738636
A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells after 72 hrs by microplate reader method, IC50=0.0124 μM 22847019
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 21892829
Hela cells Function assay 72 h Cytostatic activity against human HeLa cells after 72 hrs by cell counting, IC50=0.05 μM 21892829
CEM/0 cells Function assay 72 h Cytostatic activity against human CEM/0 cells after 72 hrs by cell counting, IC50=0.022 μM 21892829
L1210/0 cells Function assay 48 h Cytostatic activity against mouse L1210/0 cells after 48 hrs by cell counting, IC50=0.0009 μM 21892829
MCF7 cells Cytotoxicity assay 72 h Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50=12.19 μM 23867603
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by SRB assay, IC50=6.5 μM 23867603
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 25644674
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 25644674
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 25644674
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 25644674
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 17698618
RXF393 cells Function assay 48 h Anticancer activity against human RXF393 cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM 19744858
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 19744858
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 21330014
KB cells Cytotoxicity assay 72 h Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50=8.69 μM 23867603
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 11909716
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 11597404
LNCaP cells Cytotoxicity assay Cytotoxic concentration in prostate specific antigen (PSA) producing human LNCaP cells, IC50=0.0692 μM 12161157
TSU cells Cytotoxicity assay Cytotoxic concentration in non prostate specific antigen (PSA) producing human TSU cells, IC50=0.058 μM 12161157
KBALB cell Cytotoxicity assay In vitro cell cytotoxicity against KBALB cell line (transformed fibroblast sarcoma cell line), CC50=6.00E-05 μM 12620076
KBALB-STK cell Cytotoxicity assay In vitro cell cytotoxicity against KBALB-STK cell lines expressed in HSV-1 TK, IC50=8.80E-05 μM 12620076
L5178Y cell Growth inhibition assay Comparative inhibition of L5178Y cell growth in vitro (concentration required for 50% inhibition), IC50=0.00076 μM 6779007
L5178Y cells Function assay Inhibitory concentration of compound was calculated on L5178Y cells by [14C]Leu incorporation, IC50=2 μM 8246229
HT1080 cells Function assay Cytostatic activity against human HT1080 cells by MTT assay, IC50=0.18 μM 17804231
MDA-MB-231 cells Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells overexpressing urokinase plasminogen activator, IC50=0.21 μM 20363130
human ACHN cells Function assay Anticancer activity against human ACHN cells by SRB assay, GI50=2.1 μM 20732810
PC3 cells Function assay Anticancer activity against human PC3 cells by SRB assay, GI50=4.97 μM 20732810
MDA-MB-231 cells Function assay Anticancer activity against human MDA-MB-231 cells by SRB assay, GI50=0.16 μM 20732810
HeLa cells Function assay Cytostatic activity against human HeLa cells in presence of 20 uM thymidine, IC50=8.5 μM 21330014
CCRFCEM cells Function assay Cytostatic activity against human CCRFCEM cells by MTT assay, IC50=0.29 μM 17804231
点击查看更多细胞系数据

生物活性

产品描述 Floxuridine (FUDR)是一种前体药物,在体内可迅速分解为5-fluorouracil。Floxuridine 可用于治疗各种癌症,特别是转移到肝脏的癌症。Floxuridine 可抑制 Poly(ADP-Ribose) polymerase、诱导DNA损伤和凋亡。Floxuridine 对HSV和CMV具有抗病毒作用。
体外研究(In Vitro)
体外研究活性 Floxuridine呈现对PEPT1比相应的5'-O-单氨基酸酯前药更高的亲和力。[1] Floxuridine和Leucovorin联用导致人T淋巴细胞白血病细胞生长的协同抑制作用。[2] Floxuridine显著抑制[(3)H]-inosine和[(3)H]腺苷的的摄取(对照的60-70%),而它的氨基酸酯前体,包括缬氨酸,苯丙氨酸,Asp和赖氨酸酯,显著下降抑制效力(对照的10-30%)。[3] Floxuridine在36天抑制细胞增值超过对照细胞的50%,细胞数量和初始细胞密度相比增加了4倍。Floxuridine导致对体外培养的人眼球筋膜囊成纤维细胞增殖长时间延长。[4] Floxuridine是一种理想的肝动脉灌注(HAI)药物,由于其半衰期短,陡峭的剂量反应曲线,高总清除率和高肝提取。[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

化学信息&溶解度

分子量 246.19 分子式

C9H11FN2O5

CAS号 50-91-9 SDF Download Floxuridine (FUDR) SDF
Smiles C1C(C(OC1N2C=C(C(=O)NC2=O)F)CO)O
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 49 mg/mL ( 199.03 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : 49 mg/mL

Ethanol : 10 mg/mL

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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