2031161-35-8

2031161-35-8 structure

Name: UT-155
Chemical Name: UT-155
CAS Number: 2031161-35-8
Molecular Formula: C₂₀H₁₅F₄N₃O₂
Molecular Weight: 405.35
Catalog: Research Areas Cancer
Create Date: 2019-01-20 09:03:33
Modify Date: 2024-02-17 18:12:15
UT-155 is a selective androgen receptor (AR) antagonist, with a Ki of 267 nM for AR-RBD.

Name	UT-155

Description	UT-155 is a selective androgen receptor (AR) antagonist, with a Ki of 267 nM for AR-RBD.
Related Catalog	Signaling Pathways >> Others >> Androgen Receptor Research Areas >> Cancer
Target	Ki: 267 nM (AR-LBD)[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].
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].
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.