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Chemical Structure : TAS-114
Catalog No.: PC-63498Not For Human Use, Lab Use Only.
TAS-114 is a first-in-class, potent, dual dUTPase/DPD inhibitor with Ki of 0.13/2.14 uM, respectively.
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TAS-114 is a first-in-class, potent, dual dUTPase/DPD inhibitor with Ki of 0.13/2.14 uM, respectively; competitively inhibits dUTPase in the dUTP binding step, selectively inhibits the hydrolysis of dUTP to dUMP in cancer cells, significantly enhances cytotoxicity of fluoropyrimidines; TAS-114 has moderate and reversible inhibitory activity on dihydropyrimidine dehydrogenase (DPD), a catabolizing enzyme of 5-FU; increases the bioavailability of 5-FU when co-administered with capecitabine in mice, significantly improves the therapeutic efficacy of capecitabine in vivo.
Gastric Cancer
Phase 2 Clinical
| M.Wt | 451.538 | |
| Formula | C21H29N3O6S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Yano W, et al. Mol Cancer Ther. 2018 May 10. pii: molcanther.0911.2017.
2. Saito K, et al. Cancer Chemother Pharmacol. 2014 Mar;73(3):577-83.
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