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AZD3514

Catalog No. T6400 CAS 1240299-33-5

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.

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AZD3514, CAS 1240299-33-5

Pack Size	Availability	Price/USD	Quantity
5 mg	In stock	$ 65.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 96.6%

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Description	AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
Targets&IC50	Androgen receptor:2.2 μM(Ki)
In vitro	AZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors. In vitro AZD3514 inhibits cell growth in prostate cancer cells expressing wild-type (VCaP) and mutated (T877A) AR (LNCaP), but is inactive in AR-negative prostate cancer cells. AZD3514 causes a rapid reduction in PSA synthesis in vitro; with a significant decrease in PSA mRNA being evident in LNCaP cells within 2-3 h of compound treatment. AZD3514 inhibits an androgen-induced translocation of AR from the cytoplasm to the nucleus within a comparable time-frame in LNCaP cells and U2OS AR-transfected cells. AZD3514 treatment also reduces AR protein in LNCaP cells maintained in steroid-depleted conditions; an effect which is evident within 6-8 h, and maximal at 18-24 h. The ability to down-regulate AR under such conditions differentiates AZD3514 from the AR antagonists bicalutamide and Enzalutamide, which do not reduce AR protein levels. [2]
In vivo	Oral administration of AZD3514 (100 mg/kg once-daily for 7 days) significantly inhibits testosterone-induced growth of sexual accessory organs. The mode of action of AZD3514 is associated with loss of AR function. Administration of AZD3514 (100 mg/kg/day orally) for 3 days to Copenhagen rats bearing R3327H Dunning prostate tumours, indicates that AZD3514 treatment also reduces tumour AR in vivo. [2]

Molecular Weight	519.56
Formula	C25H32F3N7O2
CAS No.	1240299-33-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (179 mM)

Ethanol: 93 mg/mL (179 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Bradbury RH, et al. Bioorg Med Chem Lett, 2013, 23(7), 1945-1948. 2. Sarah A. Loddick, et al. Cancer Res, 2012, 72(8 Suppl), Abstract nr 3848.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Bioactive Compound Library Bioactive Compounds Library Max Nuclear Receptor Compound Library Anti-Prostate Cancer Compound Library Clinical Compound Library Transcription Factor-Targeted Compound Library

Related Products

Related compounds with same targets

Prochloraz ACP-105 Enzalutamide carboxylic acid Spironolactone JNJ-63576253 free base Nilutamide Androgen receptor antagonist 9 YK11

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Keywords

AZD3514 1240299-33-5 Endocrinology/Hormones Androgen Receptor selective anti proliferation LAPC4 Inhibitor oral AZD-3514 rat AR protein prostate cancer inhibit anti tumor AZD 3514 LNCaP inhibitor

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