Sparfosic Acid

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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, 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.

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

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.

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Apoptosis

Apoptosis

Apoptosis

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51321-79-0

255.12

C6H10NO8P

>98% (HPLC)

In Vitro:?H2O 中的溶解度 : 125 mg/mL (489.97 mM; 超声助溶)

[C@H](NC(CP(=O)(O)O)=O)(CC(O)=O)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years