UT-34 free base · Synonyms: UT 34 · UT34

UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM…

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

Target Estrogen Receptor/ERR

Research area Endocrinology Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

UT-34 structure

CAS No.: 2168525-92-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 580.00	BP-01981-250mg	In stock	Get quote
500 mg	USD 820.00	BP-01981-500mg	In stock	Get quote
1 g	USD 1,160.00	BP-01981-1g	In stock	Get quote
5 g	Inquire	BP-01981-5g	Inquire	Inquire

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Description

UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy.

Biological activity

In Vitro UT-34 (3-10 μM; 24 hours; LNCaP cells) treatment inhibits the expression of PSA and FKBP5 and growth of LNCaP cells starting from 100 nM with maximum effect observed at 10 μM. UT-34 (0.1-10 μM; 24 hours; LNCaP cells) treatment results in a reduction of AR levels at 1000 nM in LNCaP cells. Treatment of ZR-75-1 cells maintained in serum-containing growth medium with UT-34 results in downregulation of AR protein levels, but not estrogen receptor (ER) or progesterone receptor (PR) levels. Furthermore, in MDA-MB-453 breast cancer cells that express AR and glucocorticoid receptor (GR), UT-34 induces the downregulation of AR, but not GR. UT-34 is an effective degrader of both AR and AR-V7. LNCaP-ARV7 cells are treated for 24 hours in the presence of 0.1 nM R1881 or 10 ng/mL Doxycycline. Doxycycline induces the expression of EDN2, which is inhibited by UT-34, while UT-34 inhibits the expression of R1881-induced FKBP5 gene expression. In Vivo UT-34 (20-40 mg/kg; oral administration; daily; for 14 days; NSG mice) at 20 and 40 mg/kg reduces the seminal vesicle weight by 10%-20% and 50%-60 %, respectively. UT-34 inhibits androgen-dependent tissues such as prostate and seminal vesicles in rats, and the growth of Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenografts. UT-34 also induces tumor regression in intact immunocompromised rats.

Identifiers

SMILES: O=C(NC1=CC=C(C#N)C(C(F)(F)F)=C1)[C@@](C)(O)CN2N=CC(F)=C2
InChIKey: YDRMSDHDYRAUBR-AWEZNQCLSA-N

Specifications

MW (average): 356.2750
Formula: C₁₅H₁₂F₄N₄O₂
CAS No.: 2168525-92-4
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. Orally Bioavailable Androgen Receptor Degrader, Potential Next-Generation Therapeutic for Enzalutamide-Resistant Prostate Cancer. Clin Cancer Res. 2019 Nov 15;25(22):6764-6780.

[2]. Stone L. UT-34: a promising new AR degrader. Nat Rev Urol. 2019 Nov;16(11):640.

Same target

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Same research area

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