UT-34

UT-34 UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) 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.TargetsAR-T877A (Cell-free assay); AR-W741L (Cell-free assay); AR-WT (Cell-free assay) 80.78 nM; 94.17 nM; 203.46 nMIn vitroUT-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.In vivoUT-34 inhibits the wild-type and LBD-mutant ARs comparably and inhibits the in vivo growth of enzalutamide-sensitive and -resistant prostate cancer xenografts. In preclinical models, UT-34 induces the regression of enzalutamide-resistant tumors at doses when the AR is degraded; but, at lower doses, when the AR is just antagonized, it inhibits, without shrinking, the tumors.Cell Research(from reference)Cell lines：LNCaP, PC-3, HEK-293, ZR-75-1, MDA-MB-453, VCaP, 22RV1, and COS7 cell lines Concentrations：0.1 μM, 1 μM, 10 μM Incubation Time：30 min, 24 h, 48 h

Androgen Receptor Antagonists

Specifications & Purity: UT-34 UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) 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.TargetsAR-T877A (Cell-free assay); AR-W741L (Cell-free assay); AR-WT (Cell-free assay) 80.78 nM; 94.17 nM; 203.46 nMIn vitroUT-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.In vivoUT-34 inhibits the wild-type and LBD-mutant ARs comparably and inhibits the in vivo growth of enzalutamide-sensitive and -resistant prostate cancer xenografts. In preclinical models, UT-34 induces the regression of enzalutamide-resistant tumors at doses when the AR is degraded; but, at lower doses, when the AR is just antagonized, it inhibits, without shrinking, the tumors.Cell Research(from reference)Cell lines：LNCaP, PC-3, HEK-293, ZR-75-1, MDA-MB-453, VCaP, 22RV1, and COS7 cell lines Concentrations：0.1 μM, 1 μM, 10 μM Incubation Time：30 min, 24 h, 48 h

Molecular Formula: C15H12F4N4O2

Molecular Weight: 356.27

PubChem CID: 132214622

Isomeric SMILES: C[C@](CN1C=C(C=N1)F)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O

Storage Temperature: Store at -20°C

Shipped in: Ice chest + Ice pads

UPC:

51442438

Weight:

1.06 Ounces

HazmatClass:

Yes

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

U414245-1mg

Country of Origin:

China

CAS:

2168525-92-4

Product Size:

1mg

Harmonized Tariff Code:

2931.90.90