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AZ 3137

Cat. No. 8833 Submit a Review Datasheet / COA / SDS
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Description: Potent and selective AR and AR L702H Degrader, orally bioavailable
Chemical Name: 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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity 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.

Technical Data for AZ 3137

M. Wt 801.89
Formula C43H47F4N7O4
Storage Store at -20°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AZ 3137

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 8.02 10

Preparing Stock Solutions for AZ 3137

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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References for AZ 3137

References are publications that support the biological activity of the product.

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.

View Related Products by Target

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Citations for AZ 3137

Citations are publications that use Tocris products.

Currently there are no citations for AZ 3137. Do you know of a great paper that uses AZ 3137 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

TPD and Induced Proximity Research Product Guide

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

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