UT-155

  Cat. No.:  DC12102   Featured
Chemical Structure
2031161-35-8
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More than 5000 active chemicals with high quality for research!
Field of application
UT-155 is a selective androgen receptor (AR) antagonist, with a Ki of 267 nM for AR-RBD.
Cas No.: 2031161-35-8
Synonyms: UT-155;UT 155;UT155
SMILES: O=C([C@@](C)(O)CN1C(C=CC(F)=C2)=C2C=C1)NC3=CC=C(C#N)C(C(F)(F)F)=C3
Formula: C20H15F4N3O2
M.Wt: 405.35
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Ponnusamy S, et al. Novel Selective Agents for the Degradation of Androgen Receptor Variants to Treat Castration-Resistant Prostate Cancer. Cancer Res. 2017 Nov 15;77(22):6282-6298.
Description: UT-155 is a selective androgen receptor (AR) antagonist, with a Ki of 267 nM for AR-RBD
Target: Ki: 267 nM (AR-LBD)[1].
In Vivo: Consistent with the anti-proliferative effects in vitro, UT-155 significantly inhibits the growth of 22RV1 xenograft by 53%, while, as expected, enzalutamide has no effect on the growth of the 22RV1 tumors. Tumor weights and PSA and the expression of AR and AR-SV are significantly lower in UT-155-treated animals[1].
In Vitro: UT-155 bounds to the AR-LBD at Ki of 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, enzalutamide is weaker by two fold with the W742L mutant AR relative to the wild type AR. Treatment of LNCaP cells with UT-155 inhibits 0.1 nM R1881-induced PSA and FKBP5 gene expression between 10 and 100 nM with 5-10-fold better potency than enzalutamide[1].
References: [1]. Ponnusamy S, et al. Novel Selective Agents for the Degradation of Androgen Receptor Variants to Treat Castration-Resistant Prostate Cancer. Cancer Res. 2017 Nov 15;77(22):6282-6298.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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