Powder: -20°C for 3 years | In solvent: -80°C for 1 year
UT-155 is a selective and potent antagonist of the androgen receptor (AR) (Ki: 267 nM for UT-155 binding to AR-LBD).
説明 | UT-155 is a selective and potent antagonist of the androgen receptor (AR) (Ki: 267 nM for UT-155 binding to AR-LBD). |
ターゲット&IC50 | AR-LBD:267 nM (Ki) |
In vitro | 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. |
In vivo | 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. |
分子量 | 405.35 |
分子式 | C20H15F4N3O2 |
CAS No. | 2031161-35-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 0.1 mg/mL (insoluble)
DMSO: 130 mg/mL (320.71 mM)
You can also refer to dose conversion for different animals. 詳細
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UT-155 2031161-35-8 Endocrinology/Hormones Androgen Receptor Inhibitor UT155 inhibit UT 155 inhibitor