UT-155-Androgen-Receptor-Antagonist-MedChemExpress

UT-155

体外研究UT-155 binds to the AR-LBD at K i 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].

体内研究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.

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Caution: Product has not been fully validated for medical applications. For research use only.

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