AZ 3137
Tocris Bioscience, part of Bio-Techne | Catalog # 8833
Potent and selective AR and AR L702H Degrader, orally bioavailable
Key Product Details
Description
Potent and selective AR and AR L702H Degrader, orally bioavailable
Product Description
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.Product Specifications
Molecular Weight
801.89
Formula
C43H47F4N7O4
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for AZ 3137
For research use only
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