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说明： Potent and selective AR and AR L702H Degrader, orally bioavailable
化学名： 4-[4-[4-[4-[[4-[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-7-methoxy-1-oxo-1H-isoindol-5-yl]-1-piperazinyl]methyl]-1-piperidinyl]phenyl]-1-piperidinyl]-3-fluoro-2-(trifluoromethyl)benzonitrile
纯度： ≥98% (HPLC)
生物活性 for AZ 3137
AZ 3137 is a potent and selective androgen receptor (AR) Degrader (PROTAC®)(DC50 = 22 nM in LNCaP cells). AZ 3137 can degrade L702H mutant AR (DC50 = 158 nM). AZ 3137 inhibits the proliferation of LNCaPs cells (GI50 = 74 nM). AZ 3137 inhibits AR signaling in vitro and tumor growth in vivo in a mouse prostate cancer xenograft model. AZ 3137 is orally bioavailable.
技术数据 for AZ 3137
| 分子量 | 801.89 |
| 公式 | C43H47F4N7O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2960179-55-7 |
| PubChem ID | 171922542 |
| InChI Key | IHSNQZPLVFVVMX-UHFFFAOYSA-N |
| Smiles | N#CC1=CC=C(N2CCC(CC2)C3=CC=C(N4CCC(CC4)CN5CCN(CC5)C6=CC(OC)=C7C(N(C8C(NC(CC8)=O)=O)CC7=C6)=O)C=C3)C(F)=C1C(F)(F)F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for AZ 3137
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 8.02 | 10 |
制备储备液 for AZ 3137
以下数据基于产品分子量 801.89。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 12.47 mL | 62.35 mL | 124.71 mL |
| 0.5 mM | 2.49 mL | 12.47 mL | 24.94 mL |
| 1 mM | 1.25 mL | 6.24 mL | 12.47 mL |
| 5 mM | 0.25 mL | 1.25 mL | 2.49 mL |
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产品说明书 for AZ 3137
参考文献 for AZ 3137
参考文献是支持产品生物活性的出版物。
Bagal et al (2024) Discovery of a series of orally bioavailable androgen receptor Degraders for the treatment of prostate cancer. J.Med.Chem. 67 11732 PMID: 38991141
If you know of a relevant reference for AZ 3137, please let us know.
关键词: AZ 3137, AZ 3137 supplier, AZ3137, Androgen, receptor, AR, degraders, degrader, degrades, PROTAC, proteolysis, targeting, Cereblon, CRBN, E3, ligase, potent, selective, orally, bioavailable, prostate, cancer, in, vivo, Other, Degraders, Receptor, 8833, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
TPD and Induced Proximity Research Product Guide
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia