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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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T649333-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $70.90 | |
T649333-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $210.90 | |
T649333-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $350.90 | |
T649333-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,050.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | TAS-114 is an orally active dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine. |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Product Description | TAS-114 is an orally active dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine In Vitro TAS-114 (1-10 μM; 72 hours) increases the cytotoxicity of 5-Fluorouracil (5-FU) and 5-FU,2′-deoxy-5-fluorouridine (FdUrd) against various cancer cell lines in dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cytotoxicity AssayCell Line: HeLa, NUGC-4, NCI-H441, HT-29, CFPAC-1, and MCF-7 cell lines Concentration: 72 hours Incubation Time: 1 μM, 3 μM, and 10 μM Result: Clearly increased the cytotoxicity of FdUrd and 5-FU against various cancer cell lines in dose-dependent manner. In Vivo TAS-114 (37.5-1,200 mg/kg/day; orally; 1-14 days) increases the antitumor activity of 5-FU when co-administers with Capecitabine (539 mg/kg/day) in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c nude mice with MX-1 human breast cancer xenografts Dosage: 37.5 to 1,200 mg/kg/day Administration: Orally; daily; 1-14 days Result: Decreased the tolerable doses of Capecitabine (539 mg/kg/day) in a dose-dependent manner in mice. Form:Solid IC50& Target:dUTPase, DPD |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N-[(1R)-1-(3-cyclopentyloxyphenyl)ethyl]-3-[(2,4-dioxopyrimidin-1-yl)methoxy]propane-1-sulfonamide |
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INCHI | InChI=1S/C21H29N3O6S/c1-16(17-6-4-9-19(14-17)30-18-7-2-3-8-18)23-31(27,28)13-5-12-29-15-24-11-10-20(25)22-21(24)26/h4,6,9-11,14,16,18,23H,2-3,5,7-8,12-13,15H2,1H3,(H,22,25,26)/t16-/m1/s1 |
InChi Key | AMCGLRWKUQPNKD-MRXNPFEDSA-N |
Canonical SMILES | CC(C1=CC(=CC=C1)OC2CCCC2)NS(=O)(=O)CCCOCN3C=CC(=O)NC3=O |
Isomeric SMILES | C[C@H](C1=CC(=CC=C1)OC2CCCC2)NS(=O)(=O)CCCOCN3C=CC(=O)NC3=O |
PubChem CID | 53630253 |
MeSH Entry Terms | N-((1R)-1-(3-(Cyclopentyloxy)-phenyl)-ethyl)-3-((3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)methoxy)-1-propanesulfonamide;TAS-114 |
Molecular Weight | 451.54 |
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Solubility | DMSO : 100 mg/mL (221.46 mM; Need ultrasonic) |
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