Ralaniten triacetate是Ralaniten的前药,是一种首创的口服活性雄激素受体(AR)N端区域(NTD)抑制剂。Ralaniten triacetate 对全长AR及与耐药相关的AR变种(包括AR-v7)具有活性。
产品名称 | Androgen Receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Cyproterone acetate |
++++
Androgen Receptor, IC50: 7.1 nM | 98% | |||||||||||||||||
Apalutamide |
+++
Androgen Receptor, IC50: 16 nM | 98% | |||||||||||||||||
AZD3514 |
+
Androgen Receptor, Ki: 2.2 μM | 99% | |||||||||||||||||
Darolutamide |
++++
Androgen receptor, Ki: 11 nM | 98% | |||||||||||||||||
Flutamide |
+++
Androgen Receptor, Ki: 55 nM | 98% | |||||||||||||||||
Galeterone |
++
Androgen Receptor, IC50: 384 nM | 98% | |||||||||||||||||
Enzalutamide |
+++
Androgen Receptor, IC50: 36 nM | 98% | |||||||||||||||||
Megestrol | ✔ | 98% | |||||||||||||||||
Bicalutamide |
++
Androgen Receptor, IC50: 0.16 μM | 99% | |||||||||||||||||
EPI-001 |
+
Androgen Receptor, IC50: ~6 μM | 98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Ralaniten triacetate (EPI-506), a precursor of Ralaniten, is the first orally active inhibitor targeting the androgen receptor (AR) N-terminal domain (NTD). It is effective against both the full-length AR and variants associated with resistance, such as AR-v7[1][2]. |
体外研究 | Ralanidine triacetate (EPI-506) targets the N-terminal region of the androgen receptor (AR) and is being studied in metastatic castration-resistant prostate cancer (MCRPC). EPI-506 is a first-in-class, highly specific small molecule that binds to a new target on AR, the N-terminal domain (NTD), and directly inhibits AR by blocking the interaction between AR and transcription proteins transcriptional activity[2]. |
计算器 | ||||
存储液制备 | ![]() | 1mg | 5mg | 10mg |
1 mM 5 mM 10 mM | 1.92mL 0.38mL 0.19mL | 9.60mL 1.92mL 0.96mL | 19.19mL 3.84mL 1.92mL |
CAS号 | 1637573-04-6 |
分子式 | C27H33ClO8 |
分子量 | 520.999 |
别名 | EPI-506 |
运输 | 蓝冰 |
存储条件 | In solvent -20°C:3-6个月-80°C:12个月 |
溶解方案 | DMSO: 105 mg/mL(201.54 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |