AZ 3137

Name: AZ 3137
Brand: Tocris Bioscience
SKU: 8833

Tocris Bioscience, part of Bio-Techne | Catalog # 8833

COA / SDS

Potent and selective AR and AR L702H Degrader, orally bioavailable

Key Product Details

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)
Molecular Weight:	801.89

View Full Technical Details for AZ 3137

Technical Data
Citations

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 for AZ 3137

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

References for AZ 3137

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

Bagal Discovery of a series of orally bioavailable androgen receptor Degraders for the treatment of prostate cancer. J.Med.Chem. 2024 PMID: 38991141