Sparfosic acid

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Sparfosic acid 

Sparfosic acid 是 DNA 抗代谢剂和天门冬氨酸氨甲酰转移酶 (aspartate transcarbamoyl transferase) 的有效抑制剂。Sparfosic acid 具有抗肿瘤活性。天冬氨酸氨甲酰转移酶催化第二步 de novo 嘧啶生物合成。Sparfosic acid 协同增强 5-氟尿嘧啶 (5-FU) 和干扰素-α (IFN) 对人结肠癌细胞系的细胞毒性。

Sparfosic acid

Sparfosic acid Chemical Structure

CAS No. : 51321-79-0

规格 价格 是否有货
5 mg ￥3800 询问价格 & 货期
10 mg ￥6000 询问价格 & 货期
50 mg ￥19800 询问价格 & 货期
100 mg ￥29500 询问价格 & 货期

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Sparfosic acid 的其他形式现货产品:

Sparfosic acid trisodium

生物活性

Sparfosic acid, a DNA antimetabolite agent, is a potent inhibitor of aspartate transcarbamoyl transferase, the enzyme catalyzing the second step of de novo pyrimidine biosynthesis. Sparfosic acid 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].

体外研究
(In Vitro)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Br-l and L-2 cell lines established from metastasis in nude mouse injected with the human tumor cell line MDA-MB-435
Concentration: 300 µM
Incubation Time: 12, 24 and 48 hours
Result: Cells were predominantly in S phase in both the cell lines, although slightly higher proportion of cells in S phase were noted in L-2 than Brl-3prl cells.

Western Blot Analysis[1]

Cell Line: Br-l and L-2 cell lines
Concentration: 300 µM
Incubation Time: 4, 10 and 24 hours
Result: There was moderate difference in the level of phosphorylated Rb proteins seen in the two cell types. Marked increase in the amount of cyclin A protein was detected in the L-2 cells undergoing apoptosis with the highest level detected at 10 h post-drug treatment. In contrast, there was no increase in the level of cyclin A seen in the Brl-3prl cells. Cyclin E protein was found elevated in the L-2 cells and Brl-3prl cells compared to their respective controls.

体内研究
(In Vivo)

Sparfosic acid (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. Treatment on days 1, 5, and 9 following s.c. implantation of Lewis lung carcinoma is curative to 50% of the mice[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

255.12

Formula

C6H10NO8P
CAS 号

51321-79-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vitro: 

H2O : 125 mg/mL (489.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9197 mL 19.5986 mL 39.1972 mL
5 mM 0.7839 mL 3.9197 mL 7.8394 mL
10 mM 0.3920 mL 1.9599 mL 3.9197 mL

参考文献

  • [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.

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

    [3]. 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.

    [4]. 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.

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