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Ralaniten (EPI-002) 是一种具有有效性、特异性和口服活性的雄激素受体 N 端结构域 (AR-NTD) 拮抗剂。Ralaniten 对 AR 转录活性有抑制作用,IC50 值为 7.4 μM。Ralanites 具有抗癌活性,可用于研究去势抵抗性前列腺癌 (CRPC) 。
Ralaniten (EPI-002) 是一种具有有效性、特异性和口服活性的雄激素受体 N 端结构域 (AR-NTD) 拮抗剂。Ralaniten 对 AR 转录活性有抑制作用,IC50 值为 7.4 μM。Ralanites 具有抗癌活性,可用于研究去势抵抗性前列腺癌 (CRPC) 。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 347 | 现货 | |
5 mg | ¥ 828 | 现货 | |
10 mg | ¥ 1,320 | 现货 | |
25 mg | ¥ 2,650 | 现货 | |
50 mg | ¥ 4,130 | 现货 | |
100 mg | ¥ 5,880 | 现货 | |
200 mg | ¥ 7,950 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 892 | 现货 |
产品描述 | Ralaniten (EPI-002) is a potent, specific, and orally active antagonist of the androgen receptor N-terminal structural domain (AR-NTD).Ralaniten inhibits AR transcriptional activity with an IC50 value of 7.4 μM.Ralanites have anticancer activity and can be used to study desmoplasia-resistant prostate cancer (CRPC). |
靶点活性 | AR-NTD:7.4 μM (IC50) |
体外活性 | 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] |
体内活性 | 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] |
别名 | EPI-002 |
分子量 | 394.89 |
分子式 | C21H27ClO5 |
CAS No. | 1203490-23-6 |
Smiles | CC(C)(c1ccc(OC[C@H](O)CO)cc1)c1ccc(OC[C@H](O)CCl)cc1 |
密度 | 1.228 g/cm3 (Predicted) |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 90 mg/mL (227.91 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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