Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 208.8 nM (AR(T877A)), 246.6 nM (wt-AR), 268.2 nM (AR (F876L)), 490.2 nM (AR(W741L))[1] DC50: 2.84 μM (AR)[1]
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ln Vitro |
AR antagonist 4 (Compound 67-b) (0-10 μM; 6 days) suppresses the growth of LNCaP and 22RV1 cells[1]. CYP17A1 is inhibited by AR antagonist 4 at an IC50 of 2.59 μM[1]. With antagonist IC50s of 490.2, 208.8, and 268.2 nM against AR(W741L), AR(T877A), and AR (F876L), respectively, AR antagonist 4 exhibits antagonistic activities[1].
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ln Vivo |
When testosterone propionate (TP) is given to rats, AR antagonist 4 (Compound 67-b) (20 mg/kg; po; daily for 10 days) suppresses the growth of androgen-sensitive organs (ASOs)[1]. 4 (30 mg/kg; po; daily for 4 weeks) has antitumor activity in a mouse xenograft model resistant to enzalutamide (c4-2b−ENZ)[1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: LNCaP and 22RV1 cells Tested Concentrations: 0-10 μM Incubation Duration: 6 days Experimental Results: demonstrated antiproliferative activity with IC50s of 246.6 nM and 590 nM against LNCaP and 22RV1 cells, respectively. Western Blot Analysis[1] Cell Types: LNCaP and 22RV1 cells Tested Concentrations: 0, 1, 5, 10 and 20 μM Incubation Duration: 0, 2, 4, 8, 16 and 24 h Experimental Results: Degraded androgen receptor in a dose- and time-dependent manner. |
Animal Protocol |
Animal/Disease Models: Castrated male Sprague−Dawley rats[1]
Doses: 20 mg /kg Route of Administration: Oral administration, daily for 10 days Experimental Results: Resulted in statistically significant weight reductions in seminal vesicles (62%, p < 0.01) and ventral prostate (66%, p < 0.01) versus the testosterone propionate control. Animal/Disease Models: SPF grade male Babl/c nude male mice, enzalutamide-resistant c4-2b−ENZ xenograft model[1] Doses: 30 mg/kg Route of Administration: Oral administration, daily for 4 weeks Experimental Results: demonstrated a remarkable tumor regression with ΔT/ΔC% = −14% after 4 weeks of treatment. Animal/Disease Models: Male Sprague−Dawley rats[1] Doses: 10 mg/kg Route of Administration: Oral administration (pharmacokinetic/PK Analysis) Experimental Results: PK Parameters for AR antagonist 4 (Compound 67-b) in Male SD Ratsa[1] Compound T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AR antagonist 4 2.80 2.17 2670 24 800 aCompounds were PO-dosed at 10 mg/ kg in a solution of 5% DMSO + 30% PEG400 + 65% water (0.5% MC) in male SD rats. Abbreviations |
References |
[1]. Wang A, et al. Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer. J Med Chem. 2022 Sep 7.
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Molecular Formula |
C29H36N4O
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Molecular Weight |
456.62
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CAS # |
2883447-45-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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 | 2.1900 mL | 10.9500 mL | 21.9000 mL | |
5 mM | 0.4380 mL | 2.1900 mL | 4.3800 mL | |
10 mM | 0.2190 mL | 1.0950 mL | 2.1900 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.