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UT-155 is a selective and potent antagonist of the androgen receptor (AR) with a binding affinity (Ki) of 267 nM for the AR ligand-binding domain (AR-LBD).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $56 | In Stock | |
5 mg | $137 | In Stock | |
10 mg | $218 | In Stock | |
25 mg | $350 | In Stock | |
50 mg | $476 | In Stock | |
100 mg | $678 | In Stock | |
200 mg | $917 | In Stock | |
1 mL x 10 mM (in DMSO) | $152 | In Stock |
Description | UT-155 is a selective and potent antagonist of the androgen receptor (AR) with a binding affinity (Ki) of 267 nM for the AR ligand-binding domain (AR-LBD). |
Targets&IC50 | AR-LBD:267 nM (Ki) |
In vitro | UT-155 binds to the AR-LBD (Ki: 267 nM) and potently inhibits R1881-induced wildtype AR transactivation with 6-10-fold higher potency than enzalutamide. While UT-155 antagonizes both wildtype and mutant ARs comparably, enzalutamide's efficacy is halved against the W742L mutant AR. In LNCaP cells, UT-155 inhibits PSA and FKBP5 gene expression induced by 0.1 nM R1881 at concentrations between 10 and 100 nM, demonstrating 5-10 times better efficacy than enzalutamide. |
In vivo | Consistent with its anti-proliferative effects in vitro, UT-155 significantly inhibits the growth of 22RV1 xenografts by 53%, while enzalutamide has no effect. In UT-155-treated animals, tumor weights, PSA levels, and expression of AR and AR-SV are significantly reduced. |
Molecular Weight | 405.35 |
Formula | C20H15F4N3O2 |
Cas No. | 2031161-35-8 |
Smiles | C[C@](O)(Cn1ccc2cc(F)ccc12)C(=O)Nc1ccc(C#N)c(c1)C(F)(F)F |
Relative Density. | 1.36 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 0.1 mg/mL (insoluble) DMSO: 130 mg/mL (320.71 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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