| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg | |||
| Other Sizes |
| Targets |
A4B17 selectively targets the Androgen Receptor (AR) N-terminal domain. Unlike conventional antagonists that bind the ligand-binding pocket, it disrupts the AR's transcriptional activation function, providing a novel approach to inhibit AR signaling in prostate cancer research.
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| ln Vitro |
In vitro, A4B17 selectively targets the androgen receptor N-terminal domain to interfere with its transcriptional activity. In cell-based assays using androgen-responsive prostate cancer cell lines, A4B17 effectively reduces AR-driven gene expression and cell proliferation, demonstrating its utility as a tool for studying AR signaling blockade.
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| ln Vivo |
A4B17 has been studied in animal models of androgen-responsive prostate cancer. It demonstrates the ability to inhibit tumor growth by effectively blocking androgen receptor signaling, supporting its use as a research tool for exploring therapeutic strategies and resistance mechanisms.
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| Enzyme Assay |
A standardized protocol for AR N-terminal inhibition assay is performed using a purified GST-fused AR N-terminal domain (NTD) and a fluorescein-labeled coactivator peptide. The test compound is incubated with the protein in a buffer containing dithiothreitol (DTT) at room temperature for 30 minutes. The IC50 is determined by measuring the change in fluorescence polarization as the compound disrupts the NTD-coactivator interaction, indicating successful N-terminal inhibition.
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| Cell Assay |
Androgen-responsive prostate cancer cells are seeded in 96-well plates and treated with a dilution series of A4B17 for 48-72 hours. Cell viability is measured using a CCK-8 or MTT assay. To directly assess transcriptional activity, cells are transiently transfected with an androgen-response element (ARE) luciferase reporter. After 24 hours of treatment, luciferase activity is measured to quantify inhibition of AR-driven transcription.
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| Animal Protocol |
The in vivo efficacy of A4B17 is evaluated in a xenograft mouse model. Male athymic nude mice bearing subcutaneous LNCaP or C4-2B tumors are randomized into treatment groups when tumors reach ~100-150 mm3. A4B17 is administered via oral gavage (p.o.) or intraperitoneal (i.p.) injection. Tumor dimensions are measured bi-weekly with calipers, and tumor volume is calculated using the formula: V = 0.5 × (L × W2). At study termination, tumors are harvested for immunohistochemistry (IHC) to assess AR target gene (e.g., PSA, FKBP5) expression and Ki67 proliferation index.
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| ADME/Pharmacokinetics |
The pharmacokinetic (PK) profile of A4B17 has been characterized in rodent models. The compound exhibits good oral bioavailability with a moderate half-life suitable for once-daily dosing in preclinical studies. The PK properties support its use in xenograft mouse models for evaluating in vivo efficacy.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies indicate that A4B17 is well-tolerated at efficacious doses. Standard safety evaluations have demonstrated no significant off-target toxicity or adverse effects on major organ systems in animal models at therapeutic exposure levels. These toxicity profiles support the compound's utility as a pharmacological tool for in vivo studies.
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| References | |
| Additional Infomation |
A4B17 is a first-in-class tool compound specifically targeting the androgen receptor N-terminal domain, an intrinsically disordered region of the AR protein that has been historically difficult to drug. Its development represents a significant advance in prostate cancer research, offering a unique mechanism to block AR signaling independent of the ligand-binding domain. It is intended for research use only and is not approved for human consumption.
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| Molecular Formula |
C14H7F4NS
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|---|---|
| Molecular Weight |
297.27
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| CAS # |
2759918-91-5
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| Appearance |
White to off-white solid powder
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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 | 3.3639 mL | 16.8197 mL | 33.6395 mL | |
| 5 mM | 0.6728 mL | 3.3639 mL | 6.7279 mL | |
| 10 mM | 0.3364 mL | 1.6820 mL | 3.3639 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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