[CAS NO. 1240299-33-5] AZD3514

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PRODUCTS SPECIFICATIONS [1240299-33-5]

Catalog

AS960482

Brand

Arctom Scientific

CAS

1240299-33-5

DESCRIPTION [1240299-33-5]

Overview

MDL	-
Molecular Weight	519.56
Molecular Formula	C25H32F3N7O2
SMILES	C(F)(F)(F)C=1N2C(=NN1)CCC(=N2)N3CCC(CC3)C4=CC=C(OCCN5CCN(C(C)=O)CC5)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.9247 mL	9.6235 mL	19.2471 mL
5 mM	0.3849 mL	1.9247 mL	3.8494 mL
10 mM	0.1925 mL	0.9624 mL	1.9247 mL
50 mM	0.0385 mL	0.1925 mL	0.3849 mL

Description

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

Targets

Androgen Receptor ^[1]

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.

References

[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.

Synonyms

Ethanone, 1-[4-[2-[4-[1-[7,8-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-b]pyridazin-6-yl]-4-piperidinyl]phenoxy]ethyl]-1-piperazinyl]-

1-[4-[2-[4-[1-[7,8-Dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-b]pyridazin-6-yl]-4-piperidinyl]phenoxy]ethyl]-1-piperazinyl]ethanone

AZD 3514

1-[4-[2-[4-[1-[3-(Trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazin-1-yl]ethanone

AZD3514

AZD-3514