UT-155 是雄激素受体选择性拮抗剂，能够与 AR-LBD 结合(Ki:267 nM)。

UT-155 is a selective and potent antagonist of the androgen receptor (AR) (Ki: 267 nM for UT-155 binding to AR-LBD).

UT-155 binds to the AR-LBD (Ki: 267 nM). UT-155 potently inhibits the R1881-induced wildtype AR transactivation with 6-10-fold higher potency than enzalutamide. While UT-155 antagonizes both wildtype and mutant ARs comparably, Compared to wild-type AR, the W742L mutant AR makes enzalutamide twice as weak. Treatment of LNCaP cells with UT-155 can inhibit the expression of PSA and FKBP5 genes induced by 0.1 nM R1881 between 10 and 100 nM, and the efficacy is 5-10 times better than enzalutamide.

Consistent with the anti-proliferative effects in vitro, UT-155 significantly inhibits the growth of 22RV1 xenograft by 53%, while, enzalutamide has no effect on the growth of the 22RV1 tumors. In UT-155-treated animals, tumor weights and PSA and the expression of AR and AR-SV are significantly lower.

2031161-35-8

C20H15F4N3O2

405.35

DMSO:130 mg/mL (320.71 mM)
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years