| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In drug-resistant Br1 cells, spadrin (N-(phosphonacetyl)-L-aspartic acid, PALA) induces apoptosis [1]. At 300 µM, spafosic acid causes apoptotic pathways to be activated, which results in cell death, and a gradual buildup of S phase cells [1].
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| ln Vivo |
Mice with B16 melanoma given 490 mg/kg of spafosic acid intraperitoneally on days 1, 5, and 9 demonstrated higher lifespans—between 77% and 86% longer than controls. Sparfosic acid sensitivity in Lewis lung carcinoma is high. Half of the mice who received treatment for Lewis lung carcinoma on days 1, 5, and 9 following subcutaneous implantation recovered [4].
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| Cell Assay |
Cell viability assay [1]
Cell Types: Br-1 and L-2 cell lines established by nude mouse transfer injected with the human tumor cell line MDA-MB-435 Tested Concentrations: 300 µM Incubation Duration: 12, 24 and 48 hrs (hours) Experimental Results: Two Cells in the seed cell line are mainly in S phase, but the proportion of S phase cells in L-2 is slightly higher than that in Brl-3prl cells. Western Blot Analysis[1] Cell Types: Br-1 and L-2 Cell lines Tested Concentrations: 300 µM Incubation Duration: 4, 10 and 24 hrs (hours) Experimental Results: There was a moderate difference in the levels of phosphorylated Rb protein in the two cell types. A significant increase in the amount of cyclin A protein was detected in apoptotic L-2 cells, with the highest levels detected 10 hrs (hours) after drug treatment. In contrast, cyclin A levels were not increased in Brl-3prl cells. Cyclin E protein was increased in L-2 cells and Brl-3prl cells compared with respective controls. |
| References |
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| Additional Infomation |
Sparfosic acid is a solid. This compound belongs to the n-acyl-alpha amino acids. These are compounds containing an alpha amino acid which bears an acyl group at the terminal nitrogen atom. This substance is known to target aspartate carbamoyltransferase catalytic chain and CAD protein.
Sparfosic Acid is a stable transition state analogue for an aspartate transcarbamylase-catalyzed reaction with antineoplastic activity. Sparfosic acid is a stable transition analogue of the activated complex for the reaction catalyzed by aspartate transcarbamylase, the first step in the pyrimidine biosynthetic pathway. This agent inhibits de novo pyrimidine biosynthesis and increases the extent to which fluorouracil metabolites are incorporated into RNA. |
| Molecular Formula |
C6H10NO8P
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|---|---|
| Molecular Weight |
255.11
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| Exact Mass |
255.014
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| CAS # |
51321-79-0
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| Related CAS # |
Sparfosic acid trisodium;70962-66-2
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| PubChem CID |
39981
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| Appearance |
Colorless to light yellow liquid
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| LogP |
-3.1
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
16
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| Complexity |
346
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(C(C(=O)O)NC(=O)CP(=O)(O)O)C(=O)O
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| InChi Key |
ZZKNRXZVGOYGJT-VKHMYHEASA-N
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| InChi Code |
InChI=1S/C6H10NO8P/c8-4(2-16(13,14)15)7-3(6(11)12)1-5(9)10/h3H,1-2H2,(H,7,8)(H,9,10)(H,11,12)(H2,13,14,15)/t3-/m0/s1
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| Chemical Name |
(2S)-2-[(2-phosphonoacetyl)amino]butanedioic acid
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| Synonyms |
NSC-224131; Acide sparfosique; Sparfosic Acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~125 mg/mL (~489.97 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9199 mL | 19.5994 mL | 39.1988 mL | |
| 5 mM | 0.7840 mL | 3.9199 mL | 7.8398 mL | |
| 10 mM | 0.3920 mL | 1.9599 mL | 3.9199 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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