UT-34

Catalog No.S8885 Batch:S888501

Technical Data

Formula	C₁₅H₁₂F₄N₄O₂
Molecular Weight	356.27	CAS No.	2168525-92-4
Solubility (25°C)*	In vitro	DMSO	71 mg/mL (199.28 mM)
		Ethanol	71 mg/mL (199.28 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

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 has a broad safety margin and exhibits no cross-reactivity with Gprotein-coupled receptor kinase and nuclear receptor family members.^[1]

In vivo

In preclinical models, UT-34 induces the regression of it tumors at doses when the AR is degraded; but, at lower doses, when the AR is just antagonized, it inhibits, without shrinking, the tumors.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	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 Method LNCaP cells are maintained in 1% charcoal-stripped serum-containing mediumfor two days. Cells are treated with the indicated doses of UT-34 in the presence of 0.1 nmol/L R1881 for 24 hours, protein is extracted, and Western blot analysis for AR and actin is performed.
Animal Study:^{^[1]}	Animal Models NSG mice with MR49F xenograft Dosages 20 mg/kg, 40 mg/kg Administration Oral gavage

Cell Assay:^{^[1]}

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
Method
LNCaP cells are maintained in 1% charcoal-stripped serum-containing mediumfor two days. Cells are treated with the indicated doses of UT-34 in the presence of 0.1 nmol/L R1881 for 24 hours, protein is extracted, and Western blot analysis for AR and actin is performed.

Animal Study:^{^[1]}

Animal Models
NSG mice with MR49F xenograft
Dosages
20 mg/kg, 40 mg/kg
Administration
Oral gavage

References

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

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