| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg |
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| Targets |
The primary target of NSC 247030 is interleukin-2 (IL-2) production. It acts as an inhibitor of IL-2 production, thereby modulating T cell activation and proliferation. IL-2 is a key cytokine that plays a critical role in the immune response, and its inhibition has potential applications in immunosuppression and the treatment of autoimmune diseases. NSC 247030 has also been reported to inhibit the growth of certain cancer cells, suggesting that it may have additional targets involved in cell proliferation and survival. The compound is a 3-heteroaryl-2-indolinone and a cyclooxygenase-2 inhibitor for the treatment of neoplasia.
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| ln Vitro |
In vitro, NSC 247030 inhibits IL-2 production. It has been shown to inhibit the growth of certain cancer cells by interfering with cellular processes critical for proliferation and survival. The compound's activity is typically measured using cell-based assays that assess IL-2 production in stimulated T cells, such as ELISA or flow cytometry. In cancer cell lines, the compound's anti-proliferative effects are assessed using MTT, CellTiter-Glo, or colony formation assays. These assays confirm that NSC 247030 engages its targets and produces the expected inhibition of IL-2 production and cancer cell growth.
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| ln Vivo |
In vivo, NSC 247030 has been studied for its potential therapeutic applications in immunology, inflammation, and cancer. By inhibiting IL-2 production, the compound modulates T cell function and has potential applications in immunosuppression and the treatment of autoimmune diseases. The compound's anti-cancer activity suggests that it may also have potential as an anti-tumor agent. While specific in vivo efficacy data for NSC 247030 are not extensively detailed in the available literature, its mechanism of action suggests that it would be effective in modulating immune responses and inhibiting tumor growth.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for NSC 247030 are not extensively described. As an inhibitor of IL-2 production, the compound's activity is primarily assessed in cell-based assays that measure IL-2 production rather than direct enzyme inhibition. However, the compound's reported activity as a cyclooxygenase-2 (COX-2) inhibitor suggests that enzyme inhibition assays using purified COX-2 enzyme could be performed to assess its activity against this target. In these assays, the compound's inhibitory activity is measured by monitoring the conversion of arachidonic acid to prostaglandins.
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| Cell Assay |
In vitro cellular assays for NSC 247030 are conducted in T cells or cancer cell lines. In T cells, the compound's ability to inhibit IL-2 production is assessed by stimulating cells with a T cell activator (e.g., anti-CD3/anti-CD28 antibodies) in the presence of varying concentrations of NSC 247030, and measuring IL-2 levels in the culture supernatant using ELISA. In cancer cell lines, the compound's anti-proliferative effects are assessed using MTT, CellTiter-Glo, or colony formation assays. These assays confirm that NSC 247030 engages its targets in a cellular context and produces the expected inhibition of IL-2 production and cancer cell growth.
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| Animal Protocol |
In vivo animal studies for NSC 247030 would typically be conducted in animal models of autoimmune diseases, inflammation, or cancer. Animals would be administered the compound, and outcomes would be assessed based on the specific disease model. For example, in models of autoimmune diseases, the compound's effects on T cell activation and disease severity could be assessed. In cancer models, the compound's effects on tumor growth could be assessed in xenograft studies. These studies would confirm that NSC 247030 is effective in vivo and provide information about its therapeutic potential.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NSC 247030 indicate that it has a molecular weight of 290.14 and a molecular formula of C15H9Cl2NO. The compound is soluble in DMSO at a concentration of 20 mg/mL, facilitating its use in in vitro assays and formulation for in vivo administration. It is also soluble in DMF and DMF:PBS mixtures. For storage, the powder should be kept under appropriate conditions to maintain stability. The compound's purity is typically high, ensuring quality and reproducibility in experimental studies.
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| Toxicity/Toxicokinetics |
The toxicological profile of NSC 247030 is primarily derived from its use as a research compound in preclinical studies. As an inhibitor of IL-2 production, potential on-target effects could include immunosuppression and increased susceptibility to infections, given the role of IL-2 in the immune response. The compound's reported activity as a COX-2 inhibitor could also affect inflammation and pain pathways. Comprehensive toxicology studies would be required for therapeutic development, including assessments of immune function, gastrointestinal, and renal function.
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| References | |
| Additional Infomation |
NSC 247030 (SU5201) is an inhibitor of interleukin-2 (IL-2) production. It inhibits the growth of certain cancer cells. The compound is a 3-heteroaryl-2-indolinone and a cyclooxygenase-2 inhibitor for the treatment of neoplasia. NSC 247030 is not approved for clinical use and is available from research chemical suppliers for preclinical studies.
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| Molecular Formula |
C15H9CL2NO
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| Molecular Weight |
290.143
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| Exact Mass |
289.006
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| CAS # |
114727-43-4
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| Related CAS # |
114727-43-4
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| PubChem CID |
5476623
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| Appearance |
Yellow to orange solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
505.7±50.0 °C at 760 mmHg
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| Flash Point |
259.6±30.1 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.693
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| LogP |
4.42
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
396
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)/C(=C/C3=CC(=C(C=C3)Cl)Cl)/C(=O)N2
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| InChi Key |
RCJZXLNWNCVIMJ-XFFZJAGNSA-N
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| InChi Code |
InChI=1S/C15H9Cl2NO/c16-12-6-5-9(8-13(12)17)7-11-10-3-1-2-4-14(10)18-15(11)19/h1-8H,(H,18,19)/b11-7-
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| Chemical Name |
(3,4-Dichlorobenzylidene)-1,3-dihydroindol-2-one
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| Synonyms |
NSC 247030 NSC-247030 NSC247030.
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~25 mg/mL (~86.17 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 | 3.4466 mL | 17.2331 mL | 34.4661 mL | |
| 5 mM | 0.6893 mL | 3.4466 mL | 6.8932 mL | |
| 10 mM | 0.3447 mL | 1.7233 mL | 3.4466 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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