Sparfosic acid

产品编号:Bellancom-112732| CAS NO:51321-79-0| 分子式:C6H10NO8P| 分子量:255.12

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-112732
3800.00 杭州 北京(现货)
Bellancom-112732
6000.00 杭州 北京(现货)
Bellancom-112732
19800.00 杭州 北京(现货)
Bellancom-112732
29500.00 杭州 北京(现货)

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Sparfosic acid

产品介绍 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。
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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状Liquid
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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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