Catalog No.S1778 Synonyms: NSC 529182, NSC 75520
Molecular Weight(MW): 296.2
Trifluridine is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye.
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|Description||Trifluridine is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye.|
Trifluridine inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently. Trifluridine inhibits colony formation of bone marrow cells in a concentration-dependent manner.  Trifluridine (FTD) and 2'-deoxy-5-fluorouridine (FdUrd) are incorporated into DNA with different efficiencies due to differences in the substrate specificities of TK1 and DUT, causing abundant FTD incorporation into DNA. FTD-treated cells shows differing nuclear morphologies compared to FdUrd-treated cells.  Trifluridine inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently. 
|In vivo||Trifluridine has significantly fewer swabs positive for HSV-1 than the untreated eyes in the infected rabbits.  Trifluridine has increased antitumor activity and is incorporated into DNA more effectively than continuously infused Trifluridine in mice. Trifluridine gradually accumulates in tumor cell DNA, in a TPI-independent manner, and significantly delays tumor growth and prolonged survival in mice, compared to treatment with 5-FU derivatives.  Trifluridine results in significantly lower viral titers, fewer HSV-1-positive eyes/total during the treatment period, lower keratitis scores, fewer eyes with keratitis/total, and a shorter time to resolution of keratitis in the New Zealand rabbit ocular model. |
-  Yamashita F, et al. Cancer Chemother Pharmacol,?015 Jun 18.
-  Sakamoto K, et al. Int J Oncol,?015, 46(6), 2327-2334.
-  Germano A, et al. Mol燙ell燛ndocrinol,?014, 382(1), 1-7.
|In vitro||DMSO||59 mg/mL (199.18 mM)|
|Water||59 mg/mL warmed (199.18 mM)|
|Ethanol||59 mg/mL (199.18 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||NSC 529182, NSC 75520|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03274882||Active not recruiting||Metastatic Colorectal Cancer||Institut de Recherches Internationales Servier|Servier||March 6 2017||Phase 2|Phase 3|
|NCT03368963||Recruiting||Colorectal Adenocarcinoma|Gastric Adenocarcinoma|Metastatic Pancreatic Adenocarcinoma|Non-Resectable Cholangiocarcinoma|Stage IV Colorectal Cancer|Stage IV Gastric Cancer|Stage IV Pancreatic Cancer|Stage IVA Colorectal Cancer|Stage IVB Colorectal Cancer|Unresectable Pancreatic Carcinoma||Emory University|Taiho Oncology Inc.|Ipsen||January 30 2018||Phase 1|Phase 2|
|NCT03031691||Completed||Metastatic Colorectal Cancer||OncoMed Pharmaceuticals Inc.||January 2017||Phase 1|
|NCT02848443||Recruiting||Metastatic Colorectal Cancer||Institut de Recherches Internationales Servier|Servier||May 2016||Phase 1|
|NCT02743221||Active not recruiting||Metastatic Colorectal Cancer||Institut de Recherches Internationales Servier|Servier||April 2016||Phase 2|
|NCT01867866||Completed||Advanced Solid Tumors||Taiho Oncology Inc.||May 2013||Phase 1|
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