Cl-4AS-1 

Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC₅₀ = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively)^[1][2].

IC50: 12 nM (androgen receptor); 6 nM (5α-reductase types I); 10 nM (5α-reductase types II)^[1][2]

Cl-4AS-1 suppresses MMP-1 promoter activity in 22Rv1 human prostate cancer cells^[1].
Cl-4AS-1 (10 μM) effectively promotes the AR N/C interaction, with an average maximal activity of 35.3%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cl-4AS-1 produces no significant reduction in prostate weight in intact animals and in castrates rats caused a significant increase of ventral prostate weight^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

441.01

C₂₆H₃₃ClN₂O₂

188589-66-4

Solid

White to off-white

O=C([C@H]1CC[C@]2([H])[C@]1(C)CC[C@]3([H])[C@@]4(C)C=CC(N(C)[C@]4([H])CC[C@]32[H])=O)NC5=CC=CC=C5Cl

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Schmidt A, et al. Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands. J Biol Chem. 2009 Dec 25;284(52):36367-36376.  [Content Brief]

  [2]. Tolman RL, et al. 4-Methyl-3-oxo-4-aza-5alpha-androst-1-ene-17beta-N-aryl-carboxamides: an approach to combined androgen blockade [5alpha-reductase inhibition with androgen receptor binding in vitro]. J Steroid Biochem Mol Biol. 1997 Mar;60(5-6):303-9.  [Content Brief]