DC Chemicals Limited
China
Product Name: Androgen receptor antagonist 1
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Purity: 98.0%
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Contact: Tony Cao

1338812-36-4

1338812-36-4 structure

Name: Androgen receptor antagonist 1
Chemical Name: Androgen receptor antagonist 1
CAS Number: 1338812-36-4
Molecular Formula: C₂₁H₂₅ClN₄O₃
Molecular Weight: 416.90
Catalog: Signaling Pathways Others Androgen Receptor
Create Date: 2020-06-01 22:42:39
Modify Date: 2024-01-03 09:12:36
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM[1]. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively[2].

Name	Androgen receptor antagonist 1

Description	Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM[1]. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively[2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Others >> Androgen Receptor
Target	IC50: 59 nM (androgen receptor)[1]
In Vitro	Androgen receptor antagonist 1 (Compound 26; 1 nM-100 μM) shows significant cell growth inhibition effects for LNCaP and LNAR cells but not DU145 cells[1]. Cell Proliferation Assay[1] Cell Line: Prostate cancer (CaP) cells (LNCAP, LNAR, and DU145) Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM Incubation Time: 7 days Result: Antiproliferative effects of in LNCAP and LNAR cells.
In Vivo	Androgen receptor antagonist 1 (Compound 26; 100 mg/kg once a day for 5 weeks) demonstrates excellent in vivo tumor growth inhibition upon oral administration in a castration-resistant prostate cancer (CRPC) animal model[1]. Animal Model: Male athymic nude mice with LNCaP xenograft model of CRPC[1] Dosage: 100 mg/kg Administration: Orally once a day for 5 weeks Result: Demonstrated outstanding efficacy in inhibiting tumor growth. At the given doses (100 mg/kg once a day) nearly completely suppressed tumor growth (by 90 %) and the PSA levels (78%) after 5 weeks, with no detectable body weight loss for the period of time when animals were treated.
References	[1]. Guo C, et al. Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists. J Med Chem. 2011 Nov 10;54(21):7693-704. [2]. Han X, et al. Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. J Med Chem. 2019 Jan 24;62(2):941-964.

Molecular Formula	C₂₁H₂₅ClN₄O₃
Molecular Weight	416.90

Hazard Codes	Xi

1338812-36-4	2409791-89-3
353484-46-5	354815-43-3
2586195-28-8	1191908-24-3
1004312-94-0	2751609-45-5
443103-97-7	531506-36-2