AZD3514
AZD3514 Basic information
- Product Name:
- AZD3514
- Synonyms:
-
- AZD3514
- 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
- 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-(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;AZD 3514
- 1-(4-(2-(4-(1-(3-(Trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-
- AZD 3514; AZD-3514
- CS-795
- CAS:
- 1240299-33-5
- MF:
- C25H32F3N7O2
- MW:
- 519.56
- Product Categories:
-
- Inhibitors
- Mol File:
- 1240299-33-5.mol
AZD3514 Chemical Properties
- Boiling point:
- 669.5±65.0 °C(Predicted)
- Density
- 1.41±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- ≥24.45 mg/mL in DMSO; insoluble in H2O; ≥46.4 mg/mL in EtOH
- form
- solid
- pka
- 6.31±0.10(Predicted)
- color
- White to off-white
AZD3514 Usage And Synthesis
Uses
AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer[1][2][3].
in vivo
AZD3514 (10-100 mg/kg; p.o. once daily for 6 days) inhibits AR signaling in rats[2]. AZD3514 (50 mg/kg; p.o. once daily for 30 days) inhibits prostate tumor growth[2]. AZD3514 (50-100 mg/kg; p.o. once daily for 3 days) significantly reduces nuclear AR protein in vivo[2].
| Animal Model: | Intact or castrat 42- and 49-day-old Hans Wistar rats[2] |
| Dosage: | 10, 50 and 100 mg/kg |
| Administration: | Oral gavage; 10-100 mg/kg once daily; for 6 days |
| Result: | Inhibited AR signaling in rats, reduced seminal vesicle weight in intact rats, and inhibited the ability of exogenous testosterone proprionate to cause an increase in seminal vesicle weight in castrated rat. |
| Animal Model: | Male Copenhagen rats with Dunning R3327H prostate tumors[2] |
| Dosage: | 50 mg/kg |
| Administration: | Oral gavage; 50 mg/kg once daily; for 30 days |
| Result: | Significantly inhibited prostate tumor growth of rats. |
target
androgen receptor
References
[1] Bradbury RH, et al. Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer. Bioorg Med Chem Lett. 2013 Apr 1;23(7):1945-8. DOI:10.1016/j.bmcl.2013.02.056
[2] Loddick SA, et al. AZD3514: a small molecule that modulates androgen receptor signaling and function in vitro and in vivo. Mol Cancer Ther. 2013 Sep;12(9):1715-27. DOI:10.1158/1535-7163.MCT-12-1174
[3] Omlin A, et al. AZD3514, an oral selective androgen receptor down-regulator in patients with castration-resistant prostate cancer - results of two parallel first-in-human phase I studies. Invest New Drugs. 2015 Jun;33(3):679-90. DOI:10.1007/s10637-015-0235-5
AZD3514Supplier
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