| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
Excellent AR antagonistic activity is demonstrated by AR antagonist 3 (compound T1-12) (0.01, 0.1, 1, 10, 100 µM; eGFP IC50= 0.47 µM; PSA IC50= 1.42 µM) [1]. The AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) prevents LNCaP cells from proliferating [1]. The AR antagonist 3 (0.1, 1, 10 µM; 48 hours) decreases c-Myc and KLK3 protein expression [1]. The FRET signal shows a dose-dependent reduction with AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) (IC50= 18.05 µM) [1]. In LNCaP cells, DHT-mediated AR translocation into the nucleus is inhibited by AR antagonist 3 (10 µM; 2 hours) [1].
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|---|---|
| ln Vivo |
AR antagonist 3 (intratumoral injection; 2.5 mg/kg; once a week for 25 days) suppressed tumor development, with a final tumor growth suppression rate of 65% [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: LNCaP-ARR2PB-eGFP Cell Tested Concentrations: 0.01, 0.1, 1, 10, 100 µM Incubation Duration: Experimental Results: demonstrated excellent AR antagonistic activity (eGFP IC50= 0.47 µM; PSA IC50= 1.42 µM). Cell proliferation experiment [1] Cell Types: LNCaP, 22Rv1, C4-2, PC3, DU145 Cell Tested Concentrations: 0.01, 0.1, 1, 10, 100 µM Incubation Duration: 3 days Experimental Results: Inhibition of LNCaP cell proliferation. |
| Animal Protocol |
Animal/Disease Models: 6weeks old male CB17 SCID (severe combined immunodeficient) mouse (specific? pathogen-free grade), 18-24 g[1]
Doses: 2.5 mg/kg Route of Administration: intratumoral injection; week; 25 days Experimental Results: Inhibition of tumor growth , the final tumor growth inhibition rate was 65%. |
| References |
| Molecular Formula |
C15H18N2O3S
|
|---|---|
| Molecular Weight |
306.38
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| Exact Mass |
306.103
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| CAS # |
349573-58-6
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| PubChem CID |
885229
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| Appearance |
Light brown to brown solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
21
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| Complexity |
392
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(S(NC1=CC=C(OCC2=CC=CC=C2)C=C1)(=O)=O)C
|
| InChi Key |
VOOWYFBNDLFQKS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H18N2O3S/c1-17(2)21(18,19)16-14-8-10-15(11-9-14)20-12-13-6-4-3-5-7-13/h3-11,16H,12H2,1-2H3
|
| Chemical Name |
1-(dimethylsulfamoylamino)-4-phenylmethoxybenzene
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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)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~326.4 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.16 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.16 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (8.16 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2639 mL | 16.3196 mL | 32.6392 mL | |
| 5 mM | 0.6528 mL | 3.2639 mL | 6.5278 mL | |
| 10 mM | 0.3264 mL | 1.6320 mL | 3.2639 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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