Sparfosic acid trisodium

Name: Sparfosic acid trisodium
Brand: MedChemExpress
SKU: HY-112732B
Rating: 4.5 (2 reviews)

Cat. No.: HY-112732B Purity: 99.65%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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. Sparfosic acid trisodium synergistically enhances the cytotoxicity of a combination of 5-fluorouracil (5-FU) and interferon-alpha (IFN) against human colon cancer cell lines.

For research use only. We do not sell to patients.

Sparfosic acid trisodium Chemical Structure

CAS No. : 70962-66-2

Size	Price	Stock	Quantity
Solid or liquid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 352	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 352	In-stock	Estimated Time of Arrival: December 31
Solid or liquid
5 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1050	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1680	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Sparfosic acid trisodium:

Sparfosic acid Get quote

2 Publications Citing Use of MCE Sparfosic acid trisodium

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

Sparfosic acid trisodium (N-(Phosphonacetyl)-L-aspartate, PALA) treatment causes apoptosis in the resistant Br1 cells^[1].
? Sparfosic acid trisodium (PALA, 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 Cycle Analysis^[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 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^[1]

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.

In Vivo

Sparfosic acid trisodium (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 trisodium. 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

321.06

Formula

C₆H₇NNa₃O₈P

CAS No.

70962-66-2

Appearance

Solid-Liquid Mixture

Color

Colorless to off-white

SMILES

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

Shipping

Shipping with dry ice.

Storage

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

Solvent & Solubility

In Vitro:

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

DMSO : 180 mg/mL (560.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months.

* 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.

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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

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 4.5 mg/mL (14.02 mM); Clear solution

This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 4.5 mg/mL (14.02 mM); Clear solution

This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 4.5 mg/mL (14.02 mM); Clear solution

This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (311.47 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(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: 99.65%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (248 KB) HNMR (429 KB) LCMS (92 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]. 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]

[4]. 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]

Complete Stock Solution Preparation Table

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

DMSO / H₂O	1 mM	3.1147 mL	15.5734 mL	31.1468 mL	77.8671 mL
	5 mM	0.6229 mL	3.1147 mL	6.2294 mL	15.5734 mL
	10 mM	0.3115 mL	1.5573 mL	3.1147 mL	7.7867 mL
	15 mM	0.2076 mL	1.0382 mL	2.0765 mL	5.1911 mL
	20 mM	0.1557 mL	0.7787 mL	1.5573 mL	3.8934 mL
	25 mM	0.1246 mL	0.6229 mL	1.2459 mL	3.1147 mL
	30 mM	0.1038 mL	0.5191 mL	1.0382 mL	2.5956 mL
	40 mM	0.0779 mL	0.3893 mL	0.7787 mL	1.9467 mL
	50 mM	0.0623 mL	0.3115 mL	0.6229 mL	1.5573 mL
	60 mM	0.0519 mL	0.2596 mL	0.5191 mL	1.2978 mL
	80 mM	0.0389 mL	0.1947 mL	0.3893 mL	0.9733 mL
	100 mM	0.0311 mL	0.1557 mL	0.3115 mL	0.7787 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.