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Catalog: | HY-B0097 |
Brand: | MCE |
CAS: | 50-91-9 |
MDL | MFCD00006530 |
---|---|
Molecular Weight | 246.19 |
Molecular Formula | C9H11FN2O5 |
SMILES | O=C(N1)N([C@H]2C[C@H](O)[C@@H](CO)O2)C=C(F)C1=O |
Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite . Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis [1] [2] . Floxuridine has antiviral effects against HSV and CMV [3] .
DNA synthesis
|
Bacterial
|
HSV
|
CMV
|
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
[1]
.
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
[1]
.
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
[1]
.
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)
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
Cell Line: | Ovarian cancer cells |
Concentration: | 0-25 μM |
Incubation Time: | 4, 8, 24 hours |
Result: | Was potentiated the sensitivity by PARP inhibitors. |
Western Blot Analysis [1]
Cell Line: | OVCAR-8 and SKOV3ip cells |
Concentration: | 300 μM |
Incubation Time: | 4, 8, 24 hours |
Result: | Induced phosphorylation of Chk1 and Chk2 in two ovarian cancer cell lines |
Cell Cycle Analysis [1]
Cell Line: | A2780, SKOV3ip, OVCAR-5, and OVCAR-3 ovarian cancer cells |
Concentration: | 0.5, 1.0, 1.5, 2.0, and 2.5 μM |
Incubation Time: | 24 hours |
Result: | Induced cell arrest at G1/S-phase period. |
Floxuridine (intraperitoneal injection; 0.5-1.25 mg/kg; once per day for 7 days or single dose) is sufficient to show statistically significant protection against S. aureus infection at 0.5 mg/kg for 7 days. In addition, 1.25 mg/kg single administration of the compound shows statistically significant protection against S. aureus infection [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | C57BL/6 mice injected with S. aureus [2] |
Dosage: | 0.5-1.25 mg/kg |
Administration: | once per day for 7 days or single dose |
Result: | Was a very potent inhibitor for S. aureus infection in vivo. |
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT03876574 | Xiangya Hospital of Central South University |
Nasopharyngeal Carcinoma|Neoplasm Metastasis|Liver
|
January 1, 2011 | Phase 1 |
NCT00002783 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Gastric Cancer
|
May 1996 | Phase 2 |
NCT00408551 | Goshen Health System|National Cancer Institute (NCI) |
Colorectal Cancer|Metastatic Cancer
|
November 2005 | Phase 2 |
NCT00492999 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Colorectal Cancer|Metastatic Cancer
|
May 2007 | Phase 2 |
NCT03693807 | Memorial Sloan Kettering Cancer Center |
Colorectal Cancer|Cholangiocarcinoma
|
October 18, 2018 | Phase 2 |
NCT00004142 | M.D. Anderson Cancer Center|National Cancer Institute (NCI) |
Colorectal Cancer|Metastatic Cancer
|
August 5, 1998 | Phase 2 |
NCT00002842 | City of Hope Medical Center|National Cancer Institute (NCI) |
Colorectal Cancer|Metastatic Cancer
|
September 1994 | Phase 2 |
NCT03493061 | Sun Yat-sen University |
Colo-rectal Cancer|Liver Metastases
|
February 1, 2018 | Phase 2 |
NCT00449163 | University of Miami |
Colorectal Cancer
|
March 1, 2006 | Phase 2 |
NCT02529774 | Ye Xu|Fudan University |
Resected Liver Metastases From Colorectal Cancer
|
September 2015 | Phase 2|Phase 3 |
NCT01525069 | Washington University School of Medicine |
Cholangiocarcinoma|Liver Neoplasms
|
April 3, 2012 | Phase 1 |
NCT00020501 | National Institutes of Health Clinical Center (CC)|National Cancer Institute (NCI) |
Colorectal Cancer|Metastatic Cancer
|
March 2001 | Phase 3 |
NCT00008294 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Colorectal Cancer|Metastatic Cancer
|
August 2000 | Phase 1 |
NCT00001576 | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
Colorectal Neoplasm|Liver Neoplasm|Neoplasm Metastasis
|
July 1997 | Phase 1 |
NCT05286814 | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
Metastatic Colorectal Cancer (Mcrc)|Intrahepatic Cholangiocarcinoma (Icc)|Colorectal Cancer|Colorectal Neoplasms|Cholangiocarcinoma|Intrahepatic Bile Duct Cancer|Bile Duct Cancer|Bile Duct Neoplasms
|
October 24, 2022 | Phase 2 |
NCT00026234 | National Cancer Institute (NCI)|NSABP Foundation Inc |
Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum|Liver Metastases|Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IV Colon Cancer|Stage IV Rectal Cancer
|
February 2002 | Phase 2 |
NCT00522509 | IRCCS San Raffaele |
Colorectal Liver Metastases
|
December 1995 | |
NCT01692704 | University of Zurich |
Cholangiocellular Carcinoma
|
April 2012 | Phase 1|Phase 2 |
NCT01938729 | Memorial Sloan Kettering Cancer Center|Ohio State University|University of Texas Southwestern Medical Center|Washington University School of Medicine |
Intrahepatic Cholangiocarcinoma|Peripheral Cholangiocarcinoma|Cholangiolar Carcinoma|Cholangiocellular Carcinoma) (ICC)
|
September 5, 2013 | Phase 1 |
NCT01749397 | National Cancer Institute (NCI) |
Stage IV Fallopian Tube Cancer AJCC v6 and v7|Stage IV Ovarian Cancer AJCC v6 and v7|Stage IV Primary Peritoneal Cancer AJCC v7
|
December 7, 2012 | Phase 1 |
NCT00003753 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Colorectal Cancer|Metastatic Cancer
|
September 1998 | Phase 2 |
NCT04552093 | The Netherlands Cancer Institute|Erasmus Medical Center |
Colorectal Neoplasms
|
September 9, 2020 | Phase 2|Phase 3 |
NCT00006038 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Esophageal Cancer|Gastric Cancer
|
February 2000 | Phase 2 |
NCT00848783 | NYU Langone Health |
Gastric Cancer|Gastric Adenocarcinoma|Esophageal Cancer
|
May 2008 | Phase 2 |
NCT00004103 | NYU Langone Health|National Cancer Institute (NCI) |
Gastric Cancer
|
July 1998 | Phase 2 |
NCT00448682 | University of Miami |
Gastric Cancer
|
June 2005 | Phase 2 |
NCT00858338 | NYU Langone Health|Food and Drug Administration (FDA) |
Gastric Cancer|Stomach Cancer
|
December 2002 | Phase 2 |
NCT00019760 | National Institutes of Health Clinical Center (CC) |
Recurrent Colon Cancer|Liver Metastases|Stage IV Rectal Cancer|Recurrent Rectal Cancer|Stage IV Colon Cancer
|
April 1999 | Phase 2 |
NCT00059930 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI)|University of Medicine and Dentistry of New Jersey |
Colorectal Cancer|Metastatic Cancer
|
January 2003 | Phase 1 |
NCT00268463 | NSABP Foundation Inc|National Cancer Institute (NCI) |
Colorectal Cancer|Metastatic Cancer
|
January 2006 | Phase 3 |
NCT03856658 | Spectrum Health Hospitals |
Pancreatic Adenocarcinoma|Liver Metastases
|
February 5, 2019 | Phase 2 |
NCT04668976 | Benaroya Research Institute|Virginia Mason Hospital+Medical Center |
Colorectal Cancer|Cholangiocarcinoma
|
November 25, 2020 | Phase 2 |
NCT00410956 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Liver Cancer
|
May 2007 | Phase 2 |
NCT00063960 | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) |
Colorectal Cancer|Metastatic Cancer
|
August 2003 | Phase 2 |
NCT00448760 | University of Miami |
Esophageal Cancer
|
October 2004 | Phase 2 |
NCT03678428 | Sun Yat-sen University |
Metastatic Colorectal Cancer|Liver Metastases
|
December 31, 2021 | Phase 3 |
NCT00587067 | Memorial Sloan Kettering Cancer Center|Wake Forest University |
Hepatic Cancer
|
June 2003 | Phase 2 |
NCT00005049 | NYU Langone Health|National Cancer Institute (NCI) |
Colorectal Cancer|Gastric Cancer|Gastrointestinal Carcinoid Tumor|Gastrointestinal Stromal Tumor|Ovarian Cancer|Peritoneal Cavity Cancer|Small Intestine Cancer
|
May 1997 | Phase 2 |
NCT00645710 | City of Hope Medical Center |
Liver Metastases|Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IV Colon Cancer|Stage IV Rectal Cancer
|
February 11, 2005 | Phase 1|Phase 2 |
NCT04251715 | OHSU Knight Cancer Institute|Oregon Health and Science University |
Liver and Intrahepatic Bile Duct Carcinoma|Stage III Intrahepatic Cholangiocarcinoma AJCC v8|Stage IIIA Intrahepatic Cholangiocarcinoma AJCC v8|Stage IIIB Intrahepatic Cholangiocarcinoma AJCC v8|Stage IV Intrahepatic Cholangiocarcinoma AJCC v8|Unresectable Intrahepatic Cholangiocarcinoma
|
April 28, 2021 | Phase 2 |
NCT04898504 | Oslo University Hospital |
Colorectal Cancer|Liver Metastases|Chemotherapy Effect
|
August 2021 | Phase 2 |
NCT00005860 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Cancer
|
April 2000 | Phase 1 |
NCT03069950 | Memorial Sloan Kettering Cancer Center|The Cleveland Clinic|Oregon Health and Science University|Queens Cancer Center of Queens Hospital|Washington University School of Medicine |
Colorectal Adenocarcinoma Metastatic to the Liver
|
February 28, 2017 | Phase 2 |
NCT01862315 | Memorial Sloan Kettering Cancer Center |
Intrahepatic Cholangiocarcinoma|Peripheral Cholangiocarcinoma|Cholangiolar Carcinoma|Cholangiocellular Carcinoma
|
May 2013 | Phase 2 |
NCT04276090 | Michael J Cavnar, MD|University of Kentucky |
Bile Duct Neoplasms|Colorectal Neoplasms
|
May 1, 2020 | Not Applicable |
NCT00002716 | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) |
Colorectal Cancer|Metastatic Cancer
|
January 1996 | Phase 3 |
NCT04891289 | Memorial Sloan Kettering Cancer Center |
Intrahepatic Cholangiocarcinoma
|
May 7, 2021 | Phase 2 |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 125 mg/mL ( 507.74 mM ; Need ultrasonic)
H 2 O : ≥ 50 mg/mL ( 203.10 mM )
* "≥" means soluble, but saturation unknown.
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 4.0619 mL | 20.3095 mL | 40.6190 mL |
5 mM | 0.8124 mL | 4.0619 mL | 8.1238 mL |
10 mM | 0.4062 mL | 2.0310 mL | 4.0619 mL |
Add each solvent one by one: PBS
Solubility: 100 mg/mL (406.19 mM); Clear solution; Need ultrasonic
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (8.45 mM); Clear solution
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (8.45 mM); Clear solution
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