[CAS NO. 2168525-92-4] UT-34

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PRODUCTS SPECIFICATIONS [2168525-92-4]

Catalog

AS975172

Brand

Arctom Scientific

CAS

2168525-92-4

DESCRIPTION [2168525-92-4]

Overview

MDL	-
Molecular Weight	356.27
Molecular Formula	C15H12F4N4O2
SMILES	-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.8069 mL	14.0343 mL	28.0686 mL
5 mM	0.5614 mL	2.8069 mL	5.6137 mL
10 mM	0.2807 mL	1.4034 mL	2.8069 mL
50 mM	0.0561 mL	0.2807 mL	0.5614 mL

Description

UT-34 is a potent, selective and orally bioavailable second-generation pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer.

Targets

AR-T877A ^[1] (Cell-free assay)	AR-W741L ^[1] (Cell-free assay)	AR-WT ^[1] (Cell-free assay)
80.78 nM	94.17 nM	203.46 nM

In vitro

UT-34 inhibits the wild-type and LBD-mutant ARs comparably and inhibits the in vitro proliferation. UT-34 promotes a conformation that is distinct from the LBD-binding competitive antagonist enzalutamide and degrades the AR through the ubiquitin proteasome mechanism. UT-34 has a broad safety margin and exhibits no cross-reactivity with Gprotein-coupled receptor kinase and nuclear receptor family members.

References

[1] Suriyan Ponnusamy, et al. Clin Cancer Res. 2019 Nov 15;25(22):6764-6780.