| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
The molecular target of Rasburicase is uric acid. It functions by catalyzing the oxidation of uric acid (urate) to allantoin, a metabolite that is 5 to 10 times more soluble than uric acid. This enzymatic action dramatically reduces plasma uric acid levels. By breaking down the insoluble uric acid, it prevents the formation of uric acid crystals, which can cause acute kidney injury, a hallmark of Tumor Lysis Syndrome.
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| ln Vitro |
Rasburicase is highly active in vitro. In plasma samples, its activity can be measured directly. A single dose can rapidly reduce uric acid levels by degrading the target molecule. The enzyme is also used in research settings as a tool to deplete uric acid from biological samples, allowing researchers to study the effects of hyperuricemia on cell function or to isolate other components of the sample by removing the interfering uric acid.
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| ln Vivo |
In vivo, Rasburicase is extremely effective at rapidly lowering plasma uric acid levels. Clinical studies have shown that a single intravenous dose (0.15 or 0.20 mg/kg) can reduce uric acid to sub-normal levels within 4 hours of administration, maintaining this effect for 24 hours or longer. By preventing the accumulation of uric acid and its crystals in the kidneys, it effectively prevents the acute renal failure associated with Tumor Lysis Syndrome (TLS) and refractory gout.
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| Enzyme Assay |
Rasburicase is a parenteral drug, and its in vitro activity can be measured enzymatically. In a typical assay, the enzyme is incubated with a sample containing uric acid. The reaction proceeds, and the decrease in uric acid concentration is monitored over time using a spectrophotometer (e.g., at 293 nm). The enzyme's unit definition is based on its ability to degrade a specific amount of uric acid under defined conditions of pH, temperature, and substrate concentration.
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| Cell Assay |
Rasburicase is not typically used in standard in vitro cell culture experiments due to its high molecular weight and specific action. However, in a research setting, it could be added to cell culture media to study the effects of uric acid removal on cell phenotype or function. For example, a researcher could treat a culture of kidney cells with uric acid, then co-treat with Rasburicase to see if it reverses any uric acid-induced cellular damage.
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| Animal Protocol |
The clinical and preclinical efficacy of Rasburicase is demonstrated in vivo. In animal models, intravenous administration of Rasburicase leads to a precipitous and dose-dependent drop in plasma uric acid levels. In human clinical trials, it has been administered as a 30-minute intravenous infusion. The efficacy is measured by the percentage of patients achieving a specific, low target plasma uric acid level (e.g., ≤ 7.5 mg/dL) within a few hours of the first dose.
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| ADME/Pharmacokinetics |
Rasburicase is an exogenous protein with complex pharmacokinetics. After an IV infusion, it has a relatively short elimination half-life of about 16 to 24 hours in adults. It has a limited volume of distribution, meaning it does not extensively penetrate tissues and remains primarily in the plasma. It is a large protein and is likely to be cleared through proteolytic degradation, like other enzymes. Its effects, however, far outlast its presence due to the rapid initial depletion of uric acid.
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| Toxicity/Toxicokinetics |
Rasburicase is generally well-tolerated, but as a foreign protein, the most significant adverse reactions are immune-mediated. These include allergic reactions, bronchospasm, and rash. The development of neutralizing antibodies is common, which can reduce the drug's efficacy and increase the risk of infusion reactions. As an enzyme that breaks down uric acid, it is not directly cytotoxic, but it is contraindicated in individuals with G6PD deficiency because the breakdown of uric acid produces hydrogen peroxide, which can lead to hemolytic anemia in this population.
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| References | |
| Additional Infomation |
See also: Rasburicase (note moved to).
Rasburicase (brand names Elitek and Fasturtec) is an approved and marketed pharmaceutical drug. It is indicated for the initial management of plasma uric acid levels in adult and pediatric patients with leukemia, lymphoma, and solid tumors who are receiving chemotherapy expected to cause Tumor Lysis Syndrome (TLS). It is administered intravenously. It is also used off-label for the management of severe, refractory gout. Its use revolutionized the prevention of chemotherapy-related acute kidney injury. |
| Molecular Formula |
C1523H2383N417O462S7
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|---|---|
| Molecular Weight |
34151.61
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| Exact Mass |
261.973
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| CAS # |
134774-45-1
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| PubChem CID |
1211947
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| Appearance |
White to off-white Lyophilized powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
15
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| Complexity |
263
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WNKDYIHLNSAHRF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H8Cl2N2OS/c1-5(14)12-9(15)13-8-3-2-6(10)4-7(8)11/h2-4H,1H3,(H2,12,13,14,15)
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| Chemical Name |
N-[(2,4-dichlorophenyl)carbamothioyl]acetamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.0293 mL | 0.1464 mL | 0.2928 mL | |
| 5 mM | 0.0059 mL | 0.0293 mL | 0.0586 mL | |
| 10 mM | 0.0029 mL | 0.0146 mL | 0.0293 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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