Chemical Structure : UBX-390
CAS No.:
2759144-75-5
UBX-390
(UBX390)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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).
Physicochemical Properties
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M.Wt
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909.03
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Formula
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C48H55F3N10O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Lee S, et al. Adv Sci (Weinh). 2024 Jul 3:e2400398.
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