| Name | Tipiracil hydrochloride |
| Description | Tipiracil hydrochloride (MA-1 hydrochloride) is a thymidine phosphorylase inhibitor (TPI). Tipiracil hydrochloride is one of the active components in TAS-102, which is an anticancer drug candidate currently in clinical trials. |
| Kinase Assay | In vitro kinase inhibition assays: Kinase activity for PI3K isoforms is measured as the percentage of ATP consumed following the kinase reaction using luciferase–luciferin-coupled chemiluminescence, with ATP concentrations approximately equal to the Km for each respective kinase. Kinase reactions are initiated by combining test compounds, ATP and kinase in a 20 μL volume. PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ final enzyme concentrations are 0.5, 8, 20, and 2 nM, respectively. Of note, 0.5 μL dimethyl sulfoxide (DMSO) containing varying concentrations of the test compound is mixed with 10 μL enzyme solution (2×concentration). Kinase reactions are initiated by the addition of 10 μL of liver phosphatidylinositol and ATP solution (2×concentration). Assay concentrations for VPS34, ATP, and phosphatidylinositol are 40 nM, 1 μM, and 5 μM, respectively |
| In vitro | Tipiracil has an antiangiogenic effect that also inhibits proliferation of endothelial cells[1]. Tipiracil is a potent inhibitor of thymidine phosphorylase, which is the enzyme that degrades FTD[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : 50 mg/mL (179.13 mM)
DMSO : 50 mg/mL (179.13 mM)
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| Keywords | Inhibitor | Tipiracil | inhibit | Nucleoside Antimetabolite/Analog | MA 1 Hydrochloride | Tipiracil hydrochloride | MA-1 Hydrochloride | MA1 Hydrochloride | Tipiracil Hydrochloride |
| Inhibitors Related | Stavudine | 5-Fluorouracil |
| Related Compound Libraries | Bioactive Compound Library | EMA Approved Drug Library | Anti-Viral Compound Library | Inhibitor Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
United States
