Cl-4AS-1

Names

[ Name ]:
Cl-4AS-1

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Others >> Androgen Receptor

[Target]

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

[In Vitro]

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].

[In Vivo]

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]. Animal Model: ORX rats[1] Dosage: 10 mg/kg Administration: I.s.; 7 days Result: Effect of Cl-4AS-1 on prostate and seminal vesicle growth.

[References]

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₆H₃₃ClN₂O₂

[ Molecular Weight ]:
441.01

[ Exact Mass ]:
440.22300

[ PSA ]:
49.41000

[ LogP ]:
5.54500

Cl-4AS-1

Names

Biological Activity

Chemical & Physical Properties

Related Compounds