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Floxuridine

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Chemical Structure| 50-91-9 同义名 : 氟尿苷 ;5-Fluorouracil 2'-deoxyriboside;5-FDU;FUdR. WR138720.;FDUR;fluoruridine deoxyribose. FUDF. 5FUDR;fluorouridine deoxyribose;fluorodeoxyuridine;floxuridin;NSC 26740;5-FUDR;5-Fluorodeoxyuridine;FdUrd;NSC 27640
CAS号 : 50-91-9
货号 : A230277
分子式 : C9H11FN2O5
纯度 : 98%
分子量 : 246.192
MDL号 : MFCD00006530
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 120 mg/mL(487.42 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(203.09 mM)

动物实验配方:
生物活性
描述 Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine (0-25 μM; 4-24 hours) is affectd by inhibitors of PARP and its sensitivity of ovarian cancer cells is enhanced. Co-exposed to FdUrd and the PARP inhibitor markedly increases killing cell numbers when its compare to treatment alone in ovarian cancer cells. Floxuridine (300 μM; 4-24 hours) increases p-Chk1 and p-Chk2 in ovarian cancer cell lines. It may induce DNA damage and activate the ATM and ATR checkpoint signaling pathways. Floxuridine (0-2.5 μM; 24 hours) causes a G1/S-phase arrest and following removal of the FdUrd, the G1/S-phase-arrested cells moved synchronously through S phase and into G2/M[3]. Floxuridine (FUDR) is an ideal drug for hepatic arterial infusion (HAI) due to its short half life, steep dose response curve, high total body clearance, and high hepatic extraction[4]. Floxuridine is against Mueller Hinton Broth and Tryptic Soy Broth with MIC values of 0.25 μM and 0.81 μM, respectively. It also reported to be a very potent inhibitor of staphylococcal growth (MIC, 0.025–0.00313 μM)[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
A2780 cells Cytotoxicity assay 5 days Cytotoxicity against human A2780 cells after 5 days by MTT assay, IC50=0.026 μM 22738636
A498 cells Function assay 48 h Anticancer activity against human A498 cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM 19744858
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.06mL

0.81mL

0.41mL

20.31mL

4.06mL

2.03mL

40.62mL

8.12mL

4.06mL

参考文献

[1]Tsume Y, Hilfinger JM, Amidon GL. Enhanced cancer cell growth inhibition by dipeptide prodrugs of floxuridine: increased transporter affinity and metabolic stability. Mol Pharm. 2008 Sep-Oct;5(5):717-27.

[2]Mini E, Moroson BA, Bertino JR. Cytotoxicity of floxuridine and 5-fluorouracil in human T-lymphoblast leukemia cells: enhancement by leucovorin. Cancer Treat Rep. 1987 Apr;71(4):381-9.

[3]Huehls AM, Wagner JM, Huntoon CJ, Geng L, Erlichman C, Patel AG, Kaufmann SH, Karnitz LM. Poly(ADP-Ribose) polymerase inhibition synergizes with 5-fluorodeoxyuridine but not 5-fluorouracil in ovarian cancer cells. Cancer Res. 2011 Jul 15;71(14):4944-54

[4]Power DG, Kemeny NE. The role of floxuridine in metastatic liver disease. Mol Cancer Ther. 2009 May;8(5):1015-25

[5]Yeo WS, Arya R, Kim KK, Jeong H, Cho KH, Bae T. The FDA-approved anti-cancer drugs, streptozotocin and floxuridine, reduce the virulence of Staphylococcus aureus. Sci Rep. 2018 Feb 6;8(1):2521