产品说明书

Ralaniten

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Chemical Structure| 1203490-23-6 同义名 : EPI-002
CAS号 : 1203490-23-6
货号 : A1167310
分子式 : C21H27ClO5
纯度 : 97%
分子量 : 394.889
MDL号 : MFCD30502912
存储条件:

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(265.9 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Ralaniten, also known as EPI-002, is a potent, orally active AR-NTD antagonist. Ralaniten inhibits the transcriptional activity of AR with an IC50 value of 7.4 μM. Ralaniten can be used to study castration-resistant prostate cancer (CRPC)[1][2].At concentrations of 5-35 μM for 2-3 days, Ralaniten reduced AR-dependent proliferation of LNCaP cells, but had no effect on the survival of PC3 human prostate cancer cells that do not express functional AR[1][2].Ralaniten inhibited forskolin-induced AR-NTD transcription in LNCaP cells at concentrations of 10-35 μM for 4 hours of action[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.66mL

2.53mL

1.27mL

25.32mL

5.06mL

2.53mL

参考文献

[1]Myung JK, et, al. An androgen receptor N-terminal domain antagonist for treating prostate cancer. J Clin Invest. 2013 Jul;123(7):2948-60.

[2]Yang YC, et, al. Targeting Androgen Receptor Activation Function-1 with EPI to Overcome Resistance Mechanisms in Castration-Resistant Prostate Cancer. Clin Cancer Res. 2016 Sep 1;22(17):4466-77.