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RAD140

Chemical Structure : RAD140

CAS No.: 1182367-47-0

RAD140 (RAD-140)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 393.83
Formula C20H16ClN5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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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