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Ralaniten (EPI-002) is a potent, specific, and orally active antagonist of the androgen receptor N-terminal structural domain (AR-NTD), inhibiting AR transcriptional activity with an IC50 value of 7.4 μM. Ralaniten exhibits anticancer activity and is used to study desmoplasia-resistant prostate cancer (CRPC).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | - | In Stock | |
| 5 mg | $48 | - | In Stock | |
| 10 mg | $77 | - | In Stock | |
| 25 mg | $158 | - | In Stock | |
| 50 mg | $248 | - | In Stock | |
| 100 mg | $397 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $53 | - | In Stock |
| Description | Ralaniten (EPI-002) is a potent, specific, and orally active antagonist of the androgen receptor N-terminal structural domain (AR-NTD), inhibiting AR transcriptional activity with an IC50 value of 7.4 μM. Ralaniten exhibits anticancer activity and is used to study desmoplasia-resistant prostate cancer (CRPC). |
| Targets&IC50 | AR-NTD:7.4 μM (IC50) |
| In vitro | Ralaniten(5-35 μM; 2-3 days) reduces AR-dependent proliferation of LNCaP cells and has no effect on the viability of PC3 human prostate cancer cells that do not express functional AR.[1] Ralaniten (10-35 μM; 4 hours) inhibits forskolin-induced transactivation of the AR N-terminal domain (NTD) in LNCaP cells.[1] |
| In vivo | Ralaniten (100 mg/kg; taken orally twice daily for 28 days; Male NOD-SCID mice bearing subcutaneous tumors were castrated) inhibits VCaP tumor growth in castrated mice.[1] |
| Synonyms | EPI-002 |
| Molecular Weight | 394.89 |
| Formula | C21H27ClO5 |
| Cas No. | 1203490-23-6 |
| Smiles | CC(C)(c1ccc(OC[C@H](O)CO)cc1)c1ccc(OC[C@H](O)CCl)cc1 |
| Relative Density. | 1.228 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 90 mg/mL (227.91 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: 3.3 mg/mL (8.36 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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