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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 | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
5 mg | $80 | In Stock | |
10 mg | $128 | In Stock | |
25 mg | $263 | In Stock | |
50 mg | $413 | In Stock | |
100 mg | $662 | In Stock | |
200 mg | $926 | In Stock | |
1 mL x 10 mM (in DMSO) | $89 | 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] |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90 mg/mL (227.91 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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