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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-RAD140
RAD140

Chemical Structure : RAD140

CAS No.: 1182367-47-0

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RAD140 (RAD-140)

货号: PC-49722Not For Human Use, Lab Use Only.

Vosilasarm (RAD-140) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM), shows excellent affinity for the androgen receptor (Ki=7 nM).

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10 mg ￥780 In stock
50 mg ￥1480 In stock
100 mg ￥2380 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RAD140 (RAD-140, Vosilasarm) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM), shows excellent affinity for the androgen receptor (Ki=7 nM).
RAD140 displays good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor.
RAD140 exhibits in vitro functional androgen agonist activity with EC50 of 0.1 nM in the C2C12 osteoblast differentiation assays.
RAD140 stimulates muscle weight increases at a lower dose than that required to stimulate prostate weight increases in vivo.
Oral administration of RAD140 substantially inhibited the growth of AR/ER+ breast cancer patient-derived xenografts (PDX).
Coadministration of RAD140 and palbociclib showed improved efficacy in the AR/ER+ PDX models.

物理化学性质&存储条件

分子量 393.83
分子式 C20H16ClN5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-Chloro-4-[[(1R,2S)-1-[5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl]-2-hydroxypropyl]amino]-3-methylbenzonitrile

参考文献

1. Miller CP, et al. ACS Med Chem Lett. 2010 Dec 2;2(2):124-9.

2. Yu Z, et al. Clin Cancer Res. 2017 Dec 15;23(24):7608-7620.

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