| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Androgen Receptor (AR) DNA-binding domain (AR-DBD).
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|---|---|
| ln Vitro |
VPC-14228 effectively inhibits the activity of both full-length androgen receptors and the constitutively active splice variant AR-V7 by disrupting AR binding to chromatin.
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| ln Vivo |
No detailed in vivo activity data is available for this compound. As an AR-DBD inhibitor, it is expected to exhibit antitumor activity in prostate cancer models by blocking AR-driven transcription, but specific in vivo efficacy studies have not been reported in the current literature.
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| Enzyme Assay |
The compound is evaluated in cell-free binding assays to assess its ability to disrupt the interaction between the AR DNA-binding domain and androgen response elements (AREs). These assays typically employ techniques such as electrophoretic mobility shift assays (EMSA) or fluorescence polarization using recombinant AR-DBD protein and labeled DNA probes to measure inhibition of AR-DNA complex formation.
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| Cell Assay |
VPC-14228 is tested in PC3 human prostate cancer cells transfected with wild-type or mutant AR constructs. The compound's ability to inhibit AR transcriptional activity is measured using luciferase reporter assays, with reported IC50 values of 2.36 µM for hAR-WT, 3.70 µM for hAR-Y594A, and 3.70 µM for hAR-Q592A.
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| Animal Protocol |
No detailed in vivo animal experimental protocol is available for this compound. Typically, for AR inhibitors, xenograft mouse models using AR-positive prostate cancer cell lines (e.g., LNCaP or VCaP) are employed to evaluate tumor growth inhibition, with compound administered via oral gavage or intraperitoneal injection.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is available for VPC-14228. As a small-molecule inhibitor with a molecular weight of 246.33, it is expected to have moderate oral bioavailability and tissue distribution, but specific parameters such as half-life, clearance, and volume of distribution have not been reported.
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| Toxicity/Toxicokinetics |
No detailed toxicological data is available for this compound. Standard preclinical toxicity studies including acute and sub-chronic toxicity assessments in rodent models would be required for further development, but such data has not been published in the current literature.
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| References | |
| Additional Infomation |
VPC-14228 demonstrates high selectivity for the androgen receptor over other nuclear receptors such as estrogen and progesterone receptors. It is a research-grade chemical probe intended for studying AR-DBD function and validating the AR DNA-binding domain as a therapeutic target in prostate cancer, particularly for castration-resistant prostate cancer driven by AR splice variants. The compound has not advanced to clinical trials and is not FDA-approved.
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| Molecular Formula |
C13H14N2OS
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|---|---|
| Molecular Weight |
246.32
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| Exact Mass |
246.083
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| CAS # |
19983-28-9
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| PubChem CID |
727584
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| Appearance |
White to light yellow solid powder
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| LogP |
2.711
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
240
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MRNNJVNMXOZEQC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H14N2OS/c1-2-4-11(5-3-1)12-10-17-13(14-12)15-6-8-16-9-7-15/h1-5,10H,6-9H2
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| Chemical Name |
4-(4-phenyl-1,3-thiazol-2-yl)morpholine
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| Synonyms |
VPC14228; VPC 14228; VPC-14228
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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) |
DMSO : ~100 mg/mL (~405.96 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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 (10.15 mM) (saturation unknown) 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0598 mL | 20.2988 mL | 40.5976 mL | |
| 5 mM | 0.8120 mL | 4.0598 mL | 8.1195 mL | |
| 10 mM | 0.4060 mL | 2.0299 mL | 4.0598 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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