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MedChemExpressModel Sparfosic acid trisodium -70962-66-2

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Sparfosic acid trisodium is a DNA antimetabolite agent and a potent inhibitor of aspartate transcarbamoyl transferase. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis. Sparfosic acid trisodium synergistically enhances the cytotoxicity of a combination of 5-fluorouracil (5-FU) and interferon-alpha (IFN) against human colon cancer cell lines[1][2][3].
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Sparfosic acid trisodium

MCE China:Sparfosic acid trisodium

Brand:MedChemExpress (MCE)

Cat. No.HY-112732B

CAS:70962-66-2

Purity:98.0%

Storage:-80°C, protect from light, stored under nitrogen

Shipping:Shipping with dry ice.

Description:Sparfosic acid trisodium is a DNA antimetabolite agent and a potent inhibitor of aspartate transcarbamoyl transferase. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis. Sparfosic acid trisodium synergistically enhances the cytotoxicity of a combination of 5-fluorouracil (5-FU) and interferon-alpha (IFN) against human colon cancer cell lines.

In Vitro:Sparfosic acid trisodium (N-(Phosphonacetyl)-L-aspartate, PALA) treatment causes apoptosis in the resistant Br1 cells[1].?Sparfosic acid trisodium (PALA, 300 μM) shows progressive accumulation of cells in S phase and activation of an apoptotic pathway leading to cell death[1].

In Vivo:Sparfosic acid trisodium (490 mg/kg; i.p.; on days 1, 5, and 9; mice bearing B16 melanoma) shows the life-span is increased survives 77 to 86% longer than controls. Lewis lung carcinoma is highly sensitive to Sparfosic acid trisodium. Treatment on days 1, 5, and 9 following s.c. implantation of Lewis lung carcinoma is curative to 50% of the mice[4].

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References:

[1]. Wang J, et al. Elevated cyclin A associated kinase activity promotes sensitivity of metastatic human cancer cells to DNA antimetabolite drug. Int J Oncol. 2015 Aug;47(2):782-90.  [Content Brief]

[2]. Angela D. Morris, et al. A New, Efficient, Two Step Procedure for the Preparation of the Antineoplastic Agent Sparfosic Acid

[3]. Wadler S, et al. Phase II trial of N-(phosphonacetyl)-L-aspartate (PALA), 5-fluorouracil and recombinant interferon-alpha-2b in patients with advanced gastric carcinoma. Eur J Cancer. 1996;32A(7):1254-1256.  [Content Brief]

[4]. Johnson RK, et al. Antitumor activity of N-(phosphonacetyl)-L-aspartic acid, a transition-state inhibitor of aspartate transcarbamylase. Cancer Res. 1976;36(8):2720-2725.  [Content Brief]

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