Art. -Nr.: HY-17400

Tegafur

(Synonyms: FT 207; NSC 148958)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Tegafur (FT 207; NSC 148958) is a chemotherapeutic 5-FU proagent used in the treatment of cancers; is a component of tegafur-uracil.

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Reinheit: 99.50%
CAS. Nr.: 17902-23-7
Formel: C₈H₉FN₂O₃
Molecular Weight:200.17

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Tegafur Chemical Structure

CAS. Nr.: 17902-23-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Tegafur (FT 207; NSC 148958) is a chemotherapeutic 5-FU proagent used in the treatment of cancers; is a component of tegafur-uracil.

IC₅₀ & Target

Nucleoside antimetabolite/analog

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	>50 μM Compound: 9	Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay	[PMID: 32683166]
Astrocyte	IC₅₀	4294 μM Compound: 1, tegafur	Anticancer activity against human astrocytes cells after 72 hrs by Hoechst test Anticancer activity against human astrocytes cells after 72 hrs by Hoechst test	[PMID: 18163551]
BXPC-3	IC₅₀	145 μM Compound: 1, tegafur	Anticancer activity against human BXPC3 cells after 72 hrs in the presence of HMTA by Hoechst test Anticancer activity against human BXPC3 cells after 72 hrs in the presence of HMTA by Hoechst test	[PMID: 18163551]
BXPC-3	IC₅₀	154 μM Compound: 1, tegafur	Anticancer activity against human BXPC3 cells after 72 hrs in the presence of succinate by Hoechst test Anticancer activity against human BXPC3 cells after 72 hrs in the presence of succinate by Hoechst test	[PMID: 18163551]
BXPC-3	IC₅₀	172 μM Compound: 1, tegafur	Anticancer activity against human BXPC3 cells after 72 hrs by Hoechst test Anticancer activity against human BXPC3 cells after 72 hrs by Hoechst test	[PMID: 18163551]
CT26	IC₅₀	107 μM Compound: 1, tegafur	Anticancer activity against mouse CT26 cells after 72 hrs in the presence of HMTA by Hoechst test Anticancer activity against mouse CT26 cells after 72 hrs in the presence of HMTA by Hoechst test	[PMID: 18163551]
CT26	IC₅₀	136 μM Compound: 1, tegafur	Anticancer activity against mouse CT26 cells after 72 hrs by Hoechst test Anticancer activity against mouse CT26 cells after 72 hrs by Hoechst test	[PMID: 18163551]
CT26	IC₅₀	90 μM Compound: 1, tegafur	Anticancer activity against mouse CT26 cells after 72 hrs in the presence of succinate by Hoechst test Anticancer activity against mouse CT26 cells after 72 hrs in the presence of succinate by Hoechst test	[PMID: 18163551]
HCT-116	GI₅₀	>10 μM Compound: 9	Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay	[PMID: 32683166]
HT-29	IC₅₀	158 μM Compound: 1, tegafur	Anticancer activity against human HT29 cells after 72 hrs in the presence of HMTA by Hoechst test Anticancer activity against human HT29 cells after 72 hrs in the presence of HMTA by Hoechst test	[PMID: 18163551]
HT-29	IC₅₀	158 μM Compound: 1, tegafur	Anticancer activity against human HT29 cells after 72 hrs in the presence of succinate by Hoechst test Anticancer activity against human HT29 cells after 72 hrs in the presence of succinate by Hoechst test	[PMID: 18163551]
HT-29	IC₅₀	201 μM Compound: 1, tegafur	Anticancer activity against human HT29 cells after 72 hrs by Hoechst test Anticancer activity against human HT29 cells after 72 hrs by Hoechst test	[PMID: 18163551]
HUVEC	IC₅₀	1 μM Compound: 1, tegafur	Effect on cell viability of HUVEC cells after 48 hrs Effect on cell viability of HUVEC cells after 48 hrs	[PMID: 18163551]
LS-1034	IC₅₀	172 μM Compound: 1, tegafur	Anticancer activity against human LS1034 cells after 72 hrs in the presence of succinate by Hoechst test Anticancer activity against human LS1034 cells after 72 hrs in the presence of succinate by Hoechst test	[PMID: 18163551]
LS-1034	IC₅₀	193 μM Compound: 1, tegafur	Anticancer activity against human LS1034 cells after 72 hrs in the presence of HMTA by Hoechst test Anticancer activity against human LS1034 cells after 72 hrs in the presence of HMTA by Hoechst test	[PMID: 18163551]
LS-1034	IC₅₀	519 μM Compound: 1, tegafur	Anticancer activity against human LS1034 cells after 72 hrs by Hoechst test Anticancer activity against human LS1034 cells after 72 hrs by Hoechst test	[PMID: 18163551]
U-251	IC₅₀	384 μM Compound: 1, tegafur	Anticancer activity against human U251 cells after 72 hrs by Hoechst test Anticancer activity against human U251 cells after 72 hrs by Hoechst test	[PMID: 18163551]

In Vitro

Tegafur is bioactivated to 5-FU by liver microsomal cytochrome P450 enzymes. 5-FU is subsequently converted into its active metabolites 5-fluoro-deoxyuridine-monophosphate (FdUMP) and 5-fluorouridine-triphosphate (FUTP) intracellularly; these metabolites inhibit the enzyme thymidylate synthase and intercalate into RNA, resulting in decreased thymidine synthesis, reduced DNA synthesis, disrupted RNA function, and tumor cell cytotoxicity.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 17902-23-7
Appearance Solid
Molecular Weight 200.17
Formel C₈H₉FN₂O₃
Color White to off-white
SMILES

O=C1NC(C(F)=CN1C2OCCC2)=O
Synonyms

FT 207; NSC 148958
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (2)

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Journal Impact Factor

J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Toxicol Lett

Discovery of non-steroidal aldo-keto reductase 1D1 inhibitors through automated screening and in vitro evaluation. [Abstract]

2025 Apr:406:31-37. PMID: 39988211

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 48 mg/mL (239.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 20 mg/mL (99.92 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.9958 mL

24.9788 mL

49.9575 mL

5 mM

0.9992 mL

4.9958 mL

9.9915 mL

10 mM

0.4996 mL

2.4979 mL

4.9958 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (12.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (12.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (12.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Sotaro Sadahiro, Toshiyuki Suzuki, Akira Tanaka, et al. Association of right-sided tumors with high thymidine phosphorylase gene expression levels and the response to oral uracil and tegafur/leucovorin chemotherapy among patients with colorectal cancer. Cancer Chemotherapy and Pharmacology. 2012, 70 (2): 285-291.

[2]. José L. Ariasa, et al. Engineering of an antitumor (core/shell) magnetic nanoformulation based on the chemotherapy agent ftorafur. Colloids and Surfaces A: Physicochemical and Engineering Aspects. 2011,384(1-3): 157-163.

[3]. Gabriel N. Hortobagyi, William Heim, Laura Hutchins, et al. A phase 2 study of a fixed combination of uracil and ftorafur (UFT) and leucovorin given orally in a 3-times-daily regimen to treat patients with recurrent metastatic breast cancer. Cancer. 2010, 116(6): 1440-1445. [Content Brief]

[4]. K. Fujita, H. Nakayama, W. Ichikawa, et al. Pharmacokinetics of 5-Fluorouracil in Elderly Japanese Patients with Cancer Treated with S-1 (a Combination of Tegafur and Dihydropyrimidine Dehydrogenase Inhibitor 5-Chloro-2,4-dihydroxypyridine). Drug Metab Dispos. 2009 Jul;37(7):1375-7. doi: 10.1124/dmd.109.027052. Epub 2009 Apr 23.

[5]. Tegafur-uracil

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	4.9958 mL	24.9788 mL	49.9575 mL	124.8938 mL
	5 mM	0.9992 mL	4.9958 mL	9.9915 mL	24.9788 mL
	10 mM	0.4996 mL	2.4979 mL	4.9958 mL	12.4894 mL
	15 mM	0.3331 mL	1.6653 mL	3.3305 mL	8.3263 mL
	20 mM	0.2498 mL	1.2489 mL	2.4979 mL	6.2447 mL
	25 mM	0.1998 mL	0.9992 mL	1.9983 mL	4.9958 mL
	30 mM	0.1665 mL	0.8326 mL	1.6653 mL	4.1631 mL
	40 mM	0.1249 mL	0.6245 mL	1.2489 mL	3.1223 mL
	50 mM	0.0999 mL	0.4996 mL	0.9992 mL	2.4979 mL
	60 mM	0.0833 mL	0.4163 mL	0.8326 mL	2.0816 mL
	80 mM	0.0624 mL	0.3122 mL	0.6245 mL	1.5612 mL
DMSO	100 mM	0.0500 mL	0.2498 mL	0.4996 mL	1.2489 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Tegafur

2 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Tegafur

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tegafur Related Classifications

HY-17400 Related Classifications