AZD3514
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AZD3514是一个有效的口服雄激素受体（AR）抑制剂，Ki值为2.2 μM[1]。
AR属于类固醇激素受体家族，可作为配体依赖性的转录因子。AR信号参与抗雄激素治疗[2]。
在LNCaP和LAPC4前列腺癌细胞中，AZD3514以剂量依赖的方式抑制DHT驱动的LNCaP细胞增殖，并抑制配体驱动的AR调节基因PSA和TMPRSS2的表达。另外，AZD3514以剂量依赖的方式减少AR蛋白的表达[2]。
在患有前列腺癌的Copenhagen雄性大鼠中，口服给药AZD3514（50 mg/kg），每日一次，可抑制64％的肿瘤生长。另外，AZD3514减少核AR蛋白的表达。在Dunning R3327H肿瘤模型中，AZD3514的治疗显著降低肿瘤细胞核的AR染色，这是通过减少AR的合成速率引发的[2]。
参考文献：
[1]. Bradbury RH, Acton DG, Broadbent NL, et al. Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer. Bioorg Med Chem Lett, 2013, 23(7): 1945-1948.
[2]. Loddick SA, Ross SJ, Thomason AG, et al. AZD3514: a small molecule that modulates androgen receptor signaling and function in vitro and in vivo. Mol Cancer Ther, 2013, 12(9): 1715-1727.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 519.56 |
| Cas No. | 1240299-33-5 |
| Formula | C25H32F3N7O2 |
| Solubility | ≥24.45 mg/mL in DMSO; insoluble in H2O; ≥46.4 mg/mL in EtOH |
| Chemical Name | 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 |
| SDF | Download SDF |
| Canonical SMILES | CC(=O)N1CCN(CC1)CCOC2=CC=C(C=C2)C3CCN(CC3)C4=NN5C(=NN=C5C(F)(F)F)CC4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | AZD3514 is a small-molecule downregulator of androgen receptor with Ki value of 2.2 μM. | |||||
| Targets | androgen receptor | |||||
| IC50 | 2.2 μM (Ki) | |||||
化学结构
