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[CAS NO. 70-00-8] Trifluridine
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-A0061 |
| Brand: | MCE |
| CAS: | 70-00-8 |
Overview
| MDL | MFCD00006534 |
|---|---|
| Molecular Weight | 296.20 |
| Molecular Formula | C10H11F3N2O5 |
| SMILES | O[C@H]1C[C@H](N2C(NC(C(C(F)(F)F)=C2)=O)=O)O[C@@H]1CO |
For research use only. We do not sell to patients.
1 Publications Citing Use of MCE
Summary
Trifluridine (Trifluorothymidine; 5-Trifluorothymidine; TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis . Trifluridine is an antiviral drug for herpes simplex virus (HSV) infection . Trifluorothymidine also has anti- orthopoxvirus activity [3] .
IC50 & Target
|
Thymidylate Synthase
|
Nucleoside Antimetabolite/Analog
|
HSV-1
|
HSV-2
|
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04511039 | Roswell Park Cancer Institute|Pfizer |
Advanced Malignant Solid Neoplasm|Clinical Stage III Gastroesophageal Junction Adenocarcinoma|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma A|Locally Advanced Colorectal Carcinoma|Locally Advanced Gastroesophageal Junction Adenocarcinoma|Metastatic Colorectal Adenocarcinoma|Metastatic Gastroesophageal Junction Adenocarcinoma|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma|Postneoadjuvant Therapy Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8|Stage III Colorectal Cancer AJCC v8|Stage IIIA Colorectal Cancer AJCC v8|Stage IIIB Colorectal Cancer AJCC v8|Stage IIIC Colorectal Cancer AJCC v8|Stage IV Colorectal Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8
|
May 28, 2021 | Phase 1 |
| NCT04660760 | Academic and Community Cancer Research United|National Cancer Institute (NCI) |
Clinical Stage III Gastric Cancer AJCC v8|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IV Gastric Cancer AJCC v8|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IVA Gastric Cancer AJCC v8|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IVB Gastric Cancer AJCC v8|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8|Locally Advanced Unresectable Gastric Adenocarcinoma|Locally Advanced Unresectable Gastroesophageal Junction Adenocarcinoma|Metastatic Gastric Adenocarcinoma|Metastatic Gastroesophageal Junction Adenocarcinoma|Pathologic Stage III Gastric Cancer AJCC v8|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIA Gastric Cancer AJCC v8|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIB Gastric Cancer AJCC v8|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIC Gastric Cancer AJCC v8|Pathologic Stage IV Gastric Cancer AJCC v8|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage III Gastric Cancer AJCC v8|Postneoadjuvant Therapy Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IV Gastric Cancer AJCC v8|Postneoadjuvant Therapy Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8|Postneoadjuvant Therapy Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8
|
June 16, 2021 | Phase 2 |
| NCT04294264 | Rutgers, The State University of New Jersey|National Cancer Institute (NCI) |
Metastatic Colorectal Carcinoma|Recurrent Colon Carcinoma|Refractory Colorectal Carcinoma|Stage IV Colon Cancer AJCC v7|Stage IVA Colon Cancer AJCC v7|Stage IVB Colon Cancer AJCC v7
|
February 12, 2019 | Phase 2 |
| NCT05468892 | University of Campania Luigi Vanvitelli |
Metastatic Colon Cancer
|
October 29, 2019 | Phase 2 |
| NCT03844620 | M.D. Anderson Cancer Center|National Cancer Institute (NCI) |
Refractory Colorectal Carcinoma|Stage III Colorectal Cancer AJCC v8|Stage IIIA Colorectal Cancer AJCC v8|Stage IIIB Colorectal Cancer AJCC v8|Stage IIIC Colorectal Cancer AJCC v8|Stage IV Colorectal Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8
|
January 29, 2019 | Phase 2 |
| NCT05130060 | Mayo Clinic|National Cancer Institute (NCI) |
Metastatic Colon Adenocarcinoma|Metastatic Colorectal Adenocarcinoma|Metastatic Colorectal Carcinoma|Metastatic Microsatellite Stable Colon Carcinoma|Metastatic Microsatellite Stable Colorectal Carcinoma|Metastatic Rectal Adenocarcinoma|Microsatellite Stable Rectal Carcinoma|Stage IV Colorectal Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8
|
January 10, 2022 | Phase 1 |
| NCT00000635 | National Institute of Allergy and Infectious Diseases (NIAID)|Glaxo Wellcome |
Herpes Simplex|HIV Infections
|
Not Applicable | |
| NCT03981614 | Academic and Community Cancer Research United|National Cancer Institute (NCI) |
Metastatic Colorectal Carcinoma|Stage IV Colorectal Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8|Unresectable Carcinoma
|
October 29, 2019 | Phase 2 |
| NCT05198934 | Amgen |
Colorectal Cancer (CRC)
|
April 19, 2022 | Phase 3 |
| NCT04104139 | OHSU Knight Cancer Institute|Oregon Health and Science University|Taiho Pharmaceutical Co., Ltd. |
Rectal Adenocarcinoma|Stage IIA Rectal Cancer AJCC v8|Stage IIB Rectal Cancer AJCC v8|Stage III Rectal Cancer AJCC v8|Stage IIIA Rectal Cancer AJCC v8|Stage IIIB Rectal Cancer AJCC v8|Stage IIIC Rectal Cancer AJCC v8
|
December 11, 2019 | Phase 1 |
| NCT03992456 | Academic and Community Cancer Research United|National Cancer Institute (NCI) |
Metastatic Colon Adenocarcinoma|Metastatic Colorectal Carcinoma|Metastatic Rectal Adenocarcinoma|Stage III Colon Cancer AJCC v8|Stage III Colorectal Cancer AJCC v8|Stage III Rectal Cancer AJCC v8|Stage IIIA Colon Cancer AJCC v8|Stage IIIA Colorectal Cancer AJCC v8|Stage IIIA Rectal Cancer AJCC v8|Stage IIIB Colon Cancer AJCC v8|Stage IIIB Colorectal Cancer AJCC v8|Stage IIIB Rectal Cancer AJCC v8|Stage IIIC Colon Cancer AJCC v8|Stage IIIC Colorectal Cancer AJCC v8|Stage IIIC Rectal Cancer AJCC v8|Stage IV Colon Cancer AJCC v8|Stage IV Colorectal Cancer AJCC v8|Stage IV Rectal Cancer AJCC v8|Stage IVA Colon Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVA Rectal Cancer AJCC v8|Stage IVB Colon Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVB Rectal Cancer AJCC v8|Stage IVC Colon Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8|Stage IVC Rectal Cancer AJCC v8|Unresectable Colon Adenocarcinoma|Unresectable Colorectal Carcinoma|Unresectable Rectal Adenocarcinoma
|
April 24, 2020 | Phase 2 |
| NCT00002037 | Amgen|NIH AIDS Clinical Trials Information Service |
Mycobacterium Avium-Intracellulare Infection|HIV Infections
|
Not Applicable | |
| NCT04097028 | Roswell Park Cancer Institute|National Comprehensive Cancer Network |
Clinical Stage IIA Esophageal Adenocarcinoma AJCC v8|Clinical Stage IIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage III Esophageal Adenocarcinoma AJCC v8|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IVA Esophageal Adenocarcinoma AJCC v8|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIB Esophageal Adenocarcinoma AJCC v8|Pathologic Stage IIB Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage III Esophageal Adenocarcinoma AJCC v8|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIA Esophageal Adenocarcinoma AJCC v8|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIB Esophageal Adenocarcinoma AJCC v8|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IVA Esophageal Adenocarcinoma AJCC v8|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8
|
December 20, 2019 | Phase 2 |
| NCT05356897 | Academic and Community Cancer Research United|National Cancer Institute (NCI) |
Metastatic Colon Adenocarcinoma|Metastatic Colorectal Adenocarcinoma|Metastatic Rectal Adenocarcinoma|Stage IV Colon Cancer AJCC v8|Stage IV Colorectal Cancer AJCC v8|Stage IV Rectal Cancer AJCC v8
|
November 30, 2022 | Phase 2 |
| NCT01867866 | Taiho Oncology, Inc. |
Advanced Solid Tumors
|
May 2013 | Phase 1 |
| NCT04457297 | National Cancer Center Hospital East|Alpha-A, Inc. |
Colorectal Neoplasms|Trifluridine and Tipiracil|Circulating Tumor DNA
|
July 8, 2020 | Phase 3 |
| NCT03317119 | City of Hope Medical Center|National Cancer Institute (NCI) |
Metastatic Colon Carcinoma|Metastatic Colorectal Carcinoma|Metastatic Rectal Carcinoma|RAS Family Gene Mutation|Stage III Colon Cancer AJCC v7|Stage III Colorectal Cancer AJCC v7|Stage III Rectal Cancer AJCC v7|Stage IIIA Colon Cancer AJCC v7|Stage IIIA Colorectal Cancer AJCC v7|Stage IIIA Rectal Cancer AJCC v7|Stage IIIB Colon Cancer AJCC v7|Stage IIIB Colorectal Cancer AJCC v7|Stage IIIB Rectal Cancer AJCC v7|Stage IIIC Colon Cancer AJCC v7|Stage IIIC Colorectal Cancer AJCC v7|Stage IIIC Rectal Cancer AJCC v7|Stage IV Colon Cancer AJCC v7|Stage IV Colorectal Cancer AJCC v7|Stage IV Rectal Cancer AJCC v7|Stage IVA Colon Cancer AJCC v7|Stage IVA Colorectal Cancer AJCC v7|Stage IVA Rectal Cancer AJCC v7|Stage IVB Colon Cancer AJCC v7|Stage IVB Colorectal Cancer AJCC v7|Stage IVB Rectal Cancer AJCC v7
|
April 11, 2018 | Phase 1 |
| NCT04072445 | Mayo Clinic|National Cancer Institute (NCI)|National Comprehensive Cancer Network |
Advanced Bile Duct Carcinoma|Advanced Gallbladder Carcinoma|Refractory Bile Duct Carcinoma|Refractory Gallbladder Carcinoma|Stage III Distal Bile Duct Cancer AJCC v8|Stage III Gallbladder Cancer AJCC v8|Stage III Intrahepatic Bile Duct Cancer AJCC v8|Stage IIIA Distal Bile Duct Cancer AJCC v8|Stage IIIA Gallbladder Cancer AJCC v8|Stage IIIA Intrahepatic Bile Duct Cancer AJCC v8|Stage IIIB Distal Bile Duct Cancer AJCC v8|Stage IIIB Gallbladder Cancer AJCC v8|Stage IIIB Intrahepatic Bile Duct Cancer AJCC v8|Stage IV Distal Bile Duct Cancer AJCC v8|Stage IV Gallbladder Cancer AJCC v8|Stage IV Intrahepatic Bile Duct Cancer AJCC v8|Stage IVA Gallbladder Cancer AJCC v8|Stage IVB Gallbladder Cancer AJCC v8
|
October 18, 2019 | Phase 2 |
| NCT03368963 | Emory University|Taiho Oncology, Inc.|Ipsen |
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|Stage III Colorectal Cancer|Stage III Gastric Cancer|Stage III Pancreatic Cancer|Unresectable Digestive System Adenocarcinoma|Unresectable Pancreatic Carcinoma
|
January 30, 2018 | Phase 1|Phase 2 |
| NCT04109924 | Roswell Park Cancer Institute|National Comprehensive Cancer Network |
Advanced Colorectal Carcinoma|Metastatic Colon Adenocarcinoma|Metastatic Rectal Adenocarcinoma|Recurrent Colon Adenocarcinoma|Recurrent Colorectal Adenocarcinoma|Recurrent Rectal Adenocarcinoma|Stage III Colon Cancer AJCC v8|Stage III Colorectal Cancer AJCC v8|Stage III Rectal Cancer AJCC v8|Stage IIIA Colon Cancer AJCC v8|Stage IIIA Colorectal Cancer AJCC v8|Stage IIIB Colorectal Cancer AJCC v8|Stage IIIB Rectal Cancer AJCC v8|Stage IIIC Colon Cancer AJCC v8|Stage IIIC Colorectal Cancer AJCC v8|Stage IV Colon Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVA Rectal Cancer AJCC v8|Stage IVB Colon Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVB Rectal Cancer AJCC v8|Stage IVC Colon Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8|Stage IVC Rectal Cancer AJCC v8|Unresectable Colon Adenocarcinoma|Unresectable Colorectal Carcinoma|Unresectable Rectal Adenocarcinoma
|
December 27, 2019 | Phase 2 |
| NCT04854434 | Karyopharm Therapeutics Inc |
Metastatic Colorectal Cancer
|
June 29, 2021 | Phase 2 |
| NCT03974594 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. |
Colorectal Cancer
|
May 21, 2019 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL ( 337.61 mM )
H 2 O : 33.33 mg/mL ( 112.53 mM ; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
Preparing
Stock Solutions
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3761 mL | 16.8805 mL | 33.7610 mL |
| 5 mM | 0.6752 mL | 3.3761 mL | 6.7522 mL |
| 10 mM | 0.3376 mL | 1.6880 mL | 3.3761 mL |
*
Please refer to the solubility information to select the appropriate solvent.
In Vivo:
*
All of the co-solvents are available by MCE.
References
- [1] Suzuki N, et al. Mode of action of trifluorothymidine (TFT) against DNA replication and repair enzymes. Int J Oncol. 2011 Jul;39(1):263-70.
- [2] Suzuki N, et al. Trifluorothymidine exhibits potent antitumor activity via the induction of DNA double-strand breaks. Exp Ther Med. 2011 May;2(3):393-397.
- [3] Temmink OH, et al. Irinotecan-induced cytotoxicity to colon cancer cells in vitro is stimulated by pre-incubation withtrifluorothymidine. Eur J Cancer. 2007 Jan;43(1):175-83.
- [4] Okayama T, et al. Involvement of concentrative nucleoside transporter 1 in intestinal absorption of trifluorothymidine, a novel antitumor nucleoside, in rats. J Pharmacol Exp Ther. 2012 Feb;340(2):457-62.
- [5] Novel trifluridine crystal form and preparation method thereof. CN105198946A.
- [6] Donald F Smee, et al. A review of compounds exhibiting anti-orthopoxvirus activity in animal models. Antiviral Res. 2003 Jan;57(1-2):41-52.
Synonyms
Thymidine, α,α,α-trifluoro-
Uridine, 2′-deoxy-5-(trifluoromethyl)-
α,α,α-Trifluorothymidine
5-(Trifluoromethyl)-2′-deoxyuridine
Trifluorothymidine
2′-Deoxy-5-(trifluoromethyl)uridine
5-(Trifluoromethyl)deoxyuridine
Trifluridine
Viroptic
5-Trifluoromethyl-2′-deoxy-β-uridine
5-Trifluorothymidine
NSC 529182
NSC 75520
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