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UT-34

🥰Excellent
Catalog No. T13273Cas No. 2168525-92-4

UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.

UT-34

UT-34

🥰Excellent
Purity: 98.12%
Catalog No. T13273Cas No. 2168525-92-4
UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.
Pack SizePriceAvailabilityQuantity
1 mg$48In Stock
2 mg$74In Stock
5 mg$122In Stock
10 mg$196In Stock
25 mg$455In Stock
50 mg$669In Stock
100 mg$953In Stock
1 mL x 10 mM (in DMSO)$133In Stock
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Purity:98.12%
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Product Introduction

Bioactivity
Description
UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.
Targets&IC50
F876L AR:262.4 nM , AR (wild-type):211.7 nM , W741L AR:215.7 nM
In vitro
In LNCaP cells, UT-34 (3-10 μM; 24 hours) treatment inhibits the expression of PSA and FKBP5 and growth of LNCaP cells starting from 100 nM with maximum effect observed at 10 μM[1].In LNCaP cells UT-34 (0.1-10 μM; 24 hours; LNCaP cells) treatment results in a reduction of AR levels at 1000 nM [1]. Treatment of ZR-75-1 cells maintained in serum-containing growth medium with UT-34 results in downregulation of AR protein levels, but not estrogen receptor (ER) or progesterone receptor (PR) levels. Furthermore, in MDA-MB-453 breast cancer cells that express AR and glucocorticoid receptor (GR), UT-34 induces the downregulation of AR, but not GR[1]. UT-34 is an effective degrader of both AR and AR-V7.LNCaP-ARV7 cells were treated in the presence of 0.1 nM R1881 or 10 ng/mL doxycycline for 24 hours. Doxycycline induces the expression of EDN2, which is inhibited by UT-34, and UT-34 inhibits the expression of FKBP5 gene expression induced by R1881[1].
In vivo
In NSG mice, UT-34 (20-40 mg/kg; oral administration; daily; for 14 days ) at 20 and 40 mg/kg reduces the seminal vesicle weight by 10%-20% and 50%-60 %, respectively[1]. in rats,UT-34 inhibits androgen-dependent tissues such as prostate and seminal vesicles , and the growth of Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenografts. In intact immunocompromised rats, UT-34 also induces tumor regression [1].
Chemical Properties
Molecular Weight356.27
FormulaC15H12F4N4O2
Cas No.2168525-92-4
SmilesC[C@](O)(Cn1cc(F)cn1)C(=O)Nc1ccc(C#N)c(c1)C(F)(F)F
Relative Density.1.42 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 71 mg/mL (199.29 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.8069 mL14.0343 mL28.0686 mL140.3430 mL
5 mM0.5614 mL2.8069 mL5.6137 mL28.0686 mL
10 mM0.2807 mL1.4034 mL2.8069 mL14.0343 mL
20 mM0.1403 mL0.7017 mL1.4034 mL7.0171 mL
50 mM0.0561 mL0.2807 mL0.5614 mL2.8069 mL
100 mM0.0281 mL0.1403 mL0.2807 mL1.4034 mL

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