UT-155 free base · Synonyms: UT 155 · UT155

UT-155 is a selective and potent androgen receptor antagonist.

For research use only. Not for human or veterinary use.

Target Androgen Receptor

Research area Cancer

Purity 98+% Stock Inquire

Data Sheet SDS COA

UT-155 structure

CAS No.: 2031161-35-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 620.00	BP-01960-250mg	In stock	Get quote
500 mg	USD 980.00	BP-01960-500mg	In stock	Get quote
1 g	USD 1,580.00	BP-01960-1g	In stock	Get quote
5 g	Inquire	BP-01960-5g	Inquire	Inquire

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Description

UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.

Biological activity

In Vitro UT-155 binds 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. 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.

Identifiers

SMILES: C[C@](CN1C=CC2=C1C=CC(=C2)F)(C(=O)NC3=CC(=C(C=C3)C#N)C(F)(F)F)O
InChIKey: CFSAYQVTXBMPRF-IBGZPJMESA-N

Specifications

MW (average): 405.3456
Formula: C₂₀H₁₅F₄N₃O₂
CAS No.: 2031161-35-8
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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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