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Tipiracil hydrochloride

Catalog No. T2366 CAS 183204-72-0

Synonyms: MA-1 hydrochloride

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.

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Tipiracil hydrochloride Chemical Structure

Tipiracil hydrochloride, CAS 183204-72-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 52.00
10 mg	In stock	$ 76.00
25 mg	In stock	$ 119.00
50 mg	In stock	$ 162.00
100 mg	In stock	$ 216.00
200 mg	In stock	$ 279.00
500 mg	In stock	$ 468.00

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Purity: 100%

Purity: 99.45%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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.
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].
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

Synonyms	MA-1 hydrochloride
Molecular Weight	279.12
Formula	C9H12Cl2N4O2
CAS No.	183204-72-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 50 mg/mL(179.13 mM)

DMSO: 50 mg/mL (179.13 mM)

References and Literature

1. Peters GJ, et al. TAS-102: more than an antimetabolite. Lancet Oncol. 2012 Dec;13(12):e518-9. 2. Yoshino T, et al. TAS-102 monotherapy for pretreated metastatic colorectal cancer: a double-blind, randomised, placebo-controlled phase 2 trial. Lancet Oncol. 2012 Oct;13(10):1993-12001. 3. Belcher A, Zulfiker A H M, Li O Q, et al. Targeting Thymidine Phosphorylase With Tipiracil Hydrochloride Attenuates Thrombosis Without Increasing Risk of Bleeding in Mice[J]. Arteriosclerosis, Thrombosis, and Vascular Biology. 2020: ATVBAHA. 120.315109.

Citations

1. Belcher A, Zulfiker A H M, Li O Q, et al. Targeting Thymidine Phosphorylase With Tipiracil Hydrochloride Attenuates Thrombosis Without Increasing Risk of Bleeding in Mice. Arteriosclerosis, Thrombosis, and Vascular Biology. 2020: ATVBAHA. 120.315109.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Drug Library EMA Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Inhibitor Library FDA-Approved Drug Library Anti-Colorectal Cancer Compound Library Approved Drug Library

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Keywords

Tipiracil hydrochloride 183204-72-0 Cell Cycle/Checkpoint DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog Inhibitor Tipiracil inhibit MA-1 hydrochloride MA 1 Hydrochloride MA-1 Hydrochloride MA1 Hydrochloride Tipiracil Hydrochloride inhibitor

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