
Product Name:RAD140
Synonym:RAD140;1182367-47-0;RAD-140;Testolone;CS-2554;CS-2026;RADAROL
Molecular Formula:C20H16ClN5O2
Formula Weight:393.83
CAS No.:1182367-47-0
Description:RAD140 is an oral nonsteroidal selective androgen receptor modulator (SARM) that cannot be converted to estrogen by aromatase. It has been demonstrated that RAD140 has high AR affinity and target selectivity, showing marked tissue-selective AR agonist activity comparable to natural androgens in breast cancer cells, while lacking agonist activity in prostate cancer cells.
We have recently reported anti-tumor activity of RAD140 in multiple in vivo and in vitro models of AR/ER+ breast cancer as a single agent and in combination with inhibitors of CDK4/6 and mTOR.
Pharmacodynamic investigation indicates RAD140 acted as an AR agonist in breast cancer cells while suppressing ER signaling and reduced ESR1 mRNA expression.