188589-66-4

188589-66-4 structure

Name: Cl-4AS-1
Chemical Name: N-(2-chlorophenyl)-3-oxo-4-methyl-4-aza-5α-androst-1-ene-17β-carboxamide
CAS Number: 188589-66-4
Molecular Formula: C₂₆H₃₃ClN₂O₂
Molecular Weight: 441.01
Catalog: Research Areas Cancer
Create Date: 2017-03-23 00:34:27
Modify Date: 2024-01-02 12:43:10
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].

Name	N-(2-chlorophenyl)-3-oxo-4-methyl-4-aza-5α-androst-1-ene-17β-carboxamide

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.