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70962-66-2

中文名称 Sparfosic acid trisodium
英文名称 Sparfosic acid trisodium
CAS 70962-66-2
分子式 C6H11NNaO8P
分子量 279.12
MOL 文件 70962-66-2.mol
70962-66-2 结构式 70962-66-2 结构式

基本信息

中文别名
N-(膦酰基乙酰基)-L-天门冬氨酸三钠盐
英文别名
Sparfosic acid trisodium

物理化学性质

储存条件-20°C储存
形态Solid-Liquid Mixture
颜色Colorless to off-white
水溶解性Water: 250 mg/mL (778.67 mM)

常见问题列表

生物活性
Sparfosic acid trisodium 是天门冬氨酸氨甲酰转移酶 (aspartate transcarbamoyl transferase) 的有效抑制剂,具有抗肿瘤和抗代谢物活性。天冬氨酸氨甲酰转移酶催化第二步 de novo 嘧啶生物合成。
体外研究

Sparfosic acid (PALA) treatment causes apoptosis in the resistant Br1 cells.
Sparfosic acid (PALA, 300 µM) shows progressive accumulation of cells in S phase and activation of an apoptotic pathway leading to cell death.

Cell Cycle Analysis

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 h.
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 h.
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.
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