Sparfosic acid trisodium
目录号 : KM3979 CAS No. : 70962-66-2 纯度 : 98%

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。

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生物活性

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. Anti-tumor activity.

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.
分子式
C6H7NNa3O8P
分子量
321.06
CAS号
70962-66-2
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据
In Vitro: 

H2O : 250 mg/mL (778.67 mM; Need ultrasonic)

DMSO : 180 mg/mL (560.64 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1147 mL 15.5734 mL 31.1468 mL
5 mM 0.6229 mL 3.1147 mL 6.2294 mL
10 mM 0.3115 mL 1.5573 mL 3.1147 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 (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 4.5 mg/mL (14.02 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (14.02 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 4.5 mg/mL (14.02 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (14.02 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 4.5 mg/mL (14.02 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (14.02 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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