| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
SI-2 selectively targets steroid receptor coactivator-3 (SRC-3). It inhibits the intrinsic transcriptional activities of SRC-3 and also inhibits SRC-1 and SRC-2.
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| ln Vitro |
In vitro, SI-2 selectively reduces the transcriptional activity and protein concentrations of SRC-3 in cells. It selectively induces breast cancer cell death with IC50 values in the low nanomolar range (3-20 nM). It exhibits cytotoxicity in cancer cells and inhibits the migration of MDA-MB-468 cells.
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| ln Vivo |
In vivo, SI-2 inhibits tumor growth in mouse models without significant toxicity to the heart and other major organs at 20 mg/kg. It induces apoptosis in MDA-MB-468 cells.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for SI-2 involve measuring its binding to SRC-3. This can be done using techniques like surface plasmon resonance (SPR) or fluorescence polarization to determine the binding affinity (Kd). The compound's ability to inhibit the interaction between SRC-3 and its coactivator binding partners can be assessed in pull-down assays.
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| Cell Assay |
In vitro cellular assays for SI-2 are performed using breast cancer cell lines, such as MDA-MB-468 or other SRC-3-dependent cancer cell lines. Cells are treated with the compound for 48-72 hours, and cell viability is measured using MTT or CellTiter-Glo assays. The compound's effect on SRC-3 protein levels and transcriptional activity is assessed by Western blot and reporter gene assays. Apoptosis is measured by annexin V staining.
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| Animal Protocol |
In vivo animal studies for SI-2 are conducted in mouse xenograft models using breast cancer cell lines. Tumor-bearing mice are treated with the compound (e.g., 20 mg/kg), and tumor volume is measured over time. The compound's effect on tumor growth, SRC-3 levels, and apoptosis in tumor tissue is assessed. Toxicity to major organs is evaluated histologically.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for SI-2 are not detailed in publicly available sources. As an orally active compound, its PK properties would be characterized in preclinical species. Its ability to inhibit tumor growth in vivo suggests adequate bioavailability and tissue distribution.
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| Toxicity/Toxicokinetics |
Toxicological data for SI-2 are limited. In mouse models, it has been shown to inhibit tumor growth without significant toxicity to the heart and other major organs at 20 mg/kg. No significant toxicity has been reported in the available literature.
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| References | |
| Additional Infomation |
SI-2 is a research compound also known as EPH 116. It is a first-in-class small-molecule inhibitor of SRC-3, a nuclear protein frequently amplified in hormone-dependent cancers. It is not an approved drug and is used as a research tool to study SRC-3 biology and as a potential therapeutic lead.
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| Molecular Formula |
C15H15N5
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|---|---|
| Molecular Weight |
265.313102006912
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| Exact Mass |
265.1327
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| CAS # |
223788-33-8
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| Related CAS # |
SI-2 hydrochloride; 1992052-49-9; (E)-SI-2
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| Appearance |
Typically exists as solid at room temperature
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| SMILES |
N1(C)C(N/N=C(\C)/C2C=CC=CN=2)=NC2C=CC=CC1=2
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| Synonyms |
SI2; SI 2; SI-2
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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 | 3.7692 mL | 18.8459 mL | 37.6918 mL | |
| 5 mM | 0.7538 mL | 3.7692 mL | 7.5384 mL | |
| 10 mM | 0.3769 mL | 1.8846 mL | 3.7692 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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