UBX-390 | AR degrader | Probechem Biochemicals

Chemical Structure : UBX-390

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UBX-390 (UBX390)

货号: PC-22553Not For Human Use, Lab Use Only.

UBX-390 is a potent, selective cereblon (CRBN)-based androgen receptor (AR) degrader with DC50 of 2.41 nM in VCaP cells.

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生物&药学活性

UBX-390 is a potent, selective cereblon (CRBN)-based androgen receptor (AR) degrader with DC50 of 2.41 nM in VCaP cells.
UBX-390 degrades AR via proteasomal action in a prostate cancer cell line.
UBX-390 selectively degraded AR while sparing the degradation of other related nuclear receptors. UBX-390 exerted a more potent suppressive effect on mTOR pathway genes compared to ARV-110.
UBX-390 (10 mg/kg) exhibits therapeutic activity in xenograft models of prostate cancer.
UBX-390 shows broad activity against therapy-resistant AR mutations in the ligand-binding domain, has a stronger anti-proliferative effect than ARV-110 in VCaP, LNCaP cells (T878A mutation, no splice variant) and 22Rv1 (H875Y mutation, expresses AR variants such as AR-V7, ARV-12, and AR-V1).

物理化学性质&存储条件

分子量	909.03
分子式	C48H55F3N10O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(4-cyano-3-(trifluoromethyl)phenyl)-N-(5-(4-((4-((1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperidin-4-yl)methyl)piperazin-1-yl)methyl)piperidin-1-yl)pyridin-2-yl)piperidine-4-carboxamide

参考文献

1. Lee S, et al. Adv Sci (Weinh). 2024 Jul 3:e2400398.

UBX-390 (UBX390)

生物&药学活性

物理化学性质&存储条件

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UBX-390 (UBX390)

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