| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
DC50: 0.6 nM (AR protein degradation)[1]
ARD-2051 targets the Androgen Receptor (AR) for ubiquitination and subsequent proteasomal degradation. As a PROTAC, it simultaneously binds to AR and an E3 ubiquitin ligase (e.g., VHL or CRBN), bringing the target and the degradation machinery into close proximity. This results in highly potent degradation of AR protein. |
|---|---|
| ln Vitro |
In vitro, ARD-2051 exhibits exceptional potency in degrading AR protein. It achieves DC50 values (half-maximal degradation concentration) of 0.6 nM in both LNCaP and VCaP prostate cancer cell lines. This sub-nanomolar potency demonstrates its ability to completely eliminate AR protein at very low concentrations.
|
| ln Vivo |
ARD-2051 is an orally active AR degrader. Its high potency and oral bioavailability make it a highly effective tool for in vivo studies. In animal models, it is expected to produce a profound and sustained reduction in AR protein levels, leading to superior antitumor efficacy compared to standard antagonists.
|
| Enzyme Assay |
Cellular degradation assays are performed in AR+ prostate cancer cells (LNCaP, VCaP). Cells are treated with a concentration range of ARD-2051 for 4-8 hours. Cells are harvested, lysed, and AR protein levels are measured by Western blot. The DC50 is calculated by densitometric analysis. The time-course of AR degradation is also assessed by treating cells with a fixed concentration over time.
|
| Cell Assay |
A functional reporter assay is used to confirm that AR degradation leads to loss of transcriptional activity. LNCaP cells are transfected with an androgen response element (ARE)-luciferase reporter and treated with ARD-2051 in the presence of a synthetic androgen (e.g., R1881). The reduction in luciferase signal correlates with the degradation of AR and the consequent block in its transcriptional function.
|
| Animal Protocol |
In vivo efficacy studies are conducted in mice bearing AR+ prostate cancer xenografts. ARD-2051 is administered orally once daily. Tumor volumes are measured with calipers to assess antitumor efficacy. At study termination, tumors are harvested for Western blot analysis to confirm that the reduction in tumor growth correlates with a reduction in AR protein levels.
|
| ADME/Pharmacokinetics |
ARD-2051 is an orally bioavailable PROTAC, which is a significant advantage for in vivo research. Its pharmacokinetic profile is optimized to achieve systemic exposure that results in potent and sustained AR degradation in tumor xenografts, supporting once-daily oral dosing in preclinical models.
|
| Toxicity/Toxicokinetics |
Toxicological information for ARD-2051 is limited to its in vitro and in vivo activity. As a highly potent and selective AR degrader, its toxicological profile is likely driven by the pharmacology of AR degradation. Safety margins, selectivity, and off-target degradation are key parameters evaluated during its development as a research tool.
|
| References | |
| Additional Infomation |
ARD-2051 has a molecular formula of C43H45ClN8O5 and a molecular weight of 789.32. It is a chemical probe representing the next generation of PROTAC degraders with exceptionally high potency. This compound allows researchers to study the full consequences of near-complete AR protein ablation, overcoming the limitations of traditional inhibitors that merely block the receptor's function.
|
| Molecular Formula |
C43H45CLN8O5
|
|---|---|
| Molecular Weight |
789.32
|
| CAS # |
2632305-17-8
|
| Appearance |
Light yellow to yellow solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 1.2669 mL | 6.3346 mL | 12.6691 mL | |
| 5 mM | 0.2534 mL | 1.2669 mL | 2.5338 mL | |
| 10 mM | 0.1267 mL | 0.6335 mL | 1.2669 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
