Sparfosic acid

Cat. No.: HY-112732: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Sparfosic acid trisodium) usually boasts enhanced water solubility and stability.

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Sparfosic acid Chemical Structure

CAS No. : 51321-79-0

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Other Forms of Sparfosic acid:

Sparfosic acid trisodium Get quote

2 Publications Citing Use of MCE Sparfosic acid

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

MedChemExpress (MCE) 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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

255.12

Formula

C₆H₁₀NO₈P

CAS No.

51321-79-0

Appearance

Liquid (Density: 1.792±0.06 g/cm³)

Color

Colorless to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (246 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	3.9197 mL	19.5986 mL	39.1972 mL	97.9931 mL
	5 mM	0.7839 mL	3.9197 mL	7.8394 mL	19.5986 mL
	10 mM	0.3920 mL	1.9599 mL	3.9197 mL	9.7993 mL
	15 mM	0.2613 mL	1.3066 mL	2.6131 mL	6.5329 mL
	20 mM	0.1960 mL	0.9799 mL	1.9599 mL	4.8997 mL
	25 mM	0.1568 mL	0.7839 mL	1.5679 mL	3.9197 mL
	30 mM	0.1307 mL	0.6533 mL	1.3066 mL	3.2664 mL
	40 mM	0.0980 mL	0.4900 mL	0.9799 mL	2.4498 mL
	50 mM	0.0784 mL	0.3920 mL	0.7839 mL	1.9599 mL
	60 mM	0.0653 mL	0.3266 mL	0.6533 mL	1.6332 mL
	80 mM	0.0490 mL	0.2450 mL	0.4900 mL	1.2249 mL
	100 mM	0.0392 mL	0.1960 mL	0.3920 mL	0.9799 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Sparfosic acid Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sparfosic acid51321-79-0ApoptosisDNAantimetaboliteaspartatetranscarbamoyltransferasetumorpyrimidine biosynthesisInhibitorinhibitorinhibit

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