| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Ralaniten's primary target is the androgen receptor (AR), specifically the N-terminal domain (NTD) of the receptor. By binding to the NTD, it inhibits the transcriptional activity of the AR, which is a key driver of prostate cancer growth. This makes it a potential therapeutic agent for castration-resistant prostate cancer.
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| ln Vitro |
While EPI-002 (5–35 μM; 2–3 days) does not affect the survivability of PC3 human truck cadavers that do not express functional AR, it does activate AR in LNCaP cells [1]. In LNCaP cells, forskolin-induced transactivation of the ARN termination domain (NTD) is inhibited by ralantiten (10–35 μM; 4 hours) [1].
In vitro, Ralaniten inhibits the transcriptional activity of the androgen receptor. Its activity is assessed in cell-based reporter assays using an androgen-responsive element (ARE)-driven luciferase reporter. It has been shown to inhibit AR-mediated transcription and to inhibit the proliferation of AR-positive prostate cancer cells. |
| ln Vivo |
In vitro, EPI-002 (100 mg/kg; administered twice daily for 28 days) suppresses and modifies the formation of VCaP tumors in mice [1].
Specific in vivo activity data for Ralaniten is not detailed in the provided search results. As an AR NTD inhibitor, it would be expected to have antitumor activity in animal models of prostate cancer. It would be administered to mice bearing human prostate cancer xenografts, and tumor growth inhibition would be assessed. |
| Enzyme Assay |
The in vitro activity of Ralaniten is assessed using cell-based reporter assays. Prostate cancer cells (e.g., LNCaP or VCaP cells) are transfected with a plasmid containing an androgen-responsive element (ARE) driving a luciferase reporter gene. Cells are treated with various concentrations of Ralaniten (typically ranging from 1 nM to 100 µM) in the presence of a synthetic androgen (e.g., R1881). Luciferase activity is measured to quantify the inhibition of AR-mediated transcription. The effect on cell proliferation is assessed using the MTT assay or by counting cell numbers.
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| Cell Assay |
For cellular assays, AR-positive prostate cancer cell lines (e.g., LNCaP, VCaP, 22Rv1) are cultured in appropriate media (e.g., RPMI-1640 with 10% fetal bovine serum). Cells are treated with various concentrations of Ralaniten (typically ranging from 1 nM to 100 µM) for different time periods (e.g., 24-72 hours). The expression of AR target genes (e.g., PSA, TMPRSS2) is analyzed by quantitative real-time PCR. Cell cycle progression and apoptosis are assessed by flow cytometry.
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| Animal Protocol |
Animal/Disease Models: Male subcutaneoustumor NOD-SCID (severe combined immunodeficient) mouse Castrate
Doses: 100 mg/kg Administration Doses: 100 mg/kg: PO twice (two times) daily for 28 days Experimental Results: Inhibition of expression of AR splice variants castration resistance Growth of prostate cancer (CRPC) xenografts [1]. In vivo, Ralaniten is typically administered orally to mice bearing human prostate cancer xenografts. The compound is formulated in a suitable vehicle and administered at various doses (e.g., 10-100 mg/kg) once or twice daily. Tumor growth is monitored by measuring tumor volume over time. Pharmacodynamic studies can be performed by measuring the expression of AR target genes in tumor tissue. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Ralaniten is not available in the provided search results. As a small molecule with a molecular weight of 404.52 g/mol, it is expected to have reasonable oral bioavailability. Its half-life and metabolism would require further investigation.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Ralaniten is not available in the provided search results. As an AR inhibitor, it may have effects on the reproductive system and other androgen-dependent tissues. Comprehensive toxicological studies are required to establish its full safety profile.
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| References |
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| Additional Infomation |
Ralaniten is a research compound used to study the role of the androgen receptor N-terminal domain in prostate cancer. It is a tool for investigating the therapeutic potential of AR NTD inhibitors for the treatment of castration-resistant prostate cancer. It is not approved for clinical use.
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| Molecular Formula |
C21H27CLO5
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|---|---|
| Molecular Weight |
394.889086008072
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| Exact Mass |
394.154
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| Elemental Analysis |
C, 63.87; H, 6.89; Cl, 8.98; O, 20.26
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| CAS # |
1203490-23-6
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| Related CAS # |
Ralaniten triacetate;1637573-04-6
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| PubChem CID |
45107537
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
601.0±55.0 °C at 760 mmHg
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| Flash Point |
317.2±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.571
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| LogP |
2.98
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
27
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| Complexity |
403
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| Defined Atom Stereocenter Count |
2
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| SMILES |
ClC[C@H](COC1C=CC(=CC=1)C(C)(C)C1C=CC(=CC=1)OC[C@@H](CO)O)O
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| InChi Key |
HDTYUHNZRYZEEB-QZTJIDSGSA-N
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| InChi Code |
InChI=1S/C21H27ClO5/c1-21(2,15-3-7-19(8-4-15)26-13-17(24)11-22)16-5-9-20(10-6-16)27-14-18(25)12-23/h3-10,17-18,23-25H,11-14H2,1-2H3/t17-,18-/m1/s1
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| Chemical Name |
(2R)-3-[4-[2-[4-[(2S)-3-chloro-2-hydroxypropoxy]phenyl]propan-2-yl]phenoxy]propane-1,2-diol
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| Synonyms |
EPI-002; EPI 002; EPI002; Ralaniten;
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~253.24 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.33 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5324 mL | 12.6618 mL | 25.3235 mL | |
| 5 mM | 0.5065 mL | 2.5324 mL | 5.0647 mL | |
| 10 mM | 0.2532 mL | 1.2662 mL | 2.5324 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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