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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $93 | In Stock | |
2 mg | $137 | In Stock | |
5 mg | $228 | In Stock | |
10 mg | $363 | In Stock | |
25 mg | $583 | In Stock | |
50 mg | $793 | In Stock | |
100 mg | $1,130 | In Stock | |
500 mg | $2,280 | In Stock | |
1 mL x 10 mM (in DMSO) | $253 | In Stock |
Description | UT-155 is a selective and potent antagonist of the androgen receptor (AR) (Ki: 267 nM for UT-155 binding to AR-LBD). |
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. |
Molecular Weight | 405.35 |
Formula | C20H15F4N3O2 |
Cas No. | 2031161-35-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 0.1 mg/mL (insoluble) DMSO: 130 mg/mL (320.71 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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