| Identification | Back Directory | [Name]
Sparfosic | [CAS]
51321-79-0 | [Synonyms]
PALA
Sparfosic
NSC 224131
Sparfosate
Acide sparfosique
N-phosphonacetyl-L-aspartate
N-(Phosphonoacetyl)-L-aspartic acid
L-Aspartic acid, N-(2-phosphonoacetyl)- | [Molecular Formula]
C6H10NO8P | [MDL Number]
MFCD01664797 | [MOL File]
51321-79-0.mol | [Molecular Weight]
255.118 |
| Chemical Properties | Back Directory | [Boiling point ]
96.8°C | [density ]
1.792±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Liquid | [pka]
1.73±0.10(Predicted) | [color ]
Colorless to light yellow | [Water Solubility ]
Water : 125 mg/mL (489.97 mM; Need ultrasonic) |
| Hazard Information | Back Directory | [Uses]
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[1][2][3]. | [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]. | [storage]
Store at -20°C | [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. DOI:10.3892/ijo.2015.3037
[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. PMID:1064466
[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. DOI:10.1016/0959-8049(96)00035-4 |
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| Company Name: |
LGM Pharma
|
| Tel: |
1-(800)-881-8210 |
| Website: |
www.lgmpharma.com |
|