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Chemical Structure : UT-105
Catalog No.: PC-21404Not For Human Use, Lab Use Only.
UT-105 is a small-molecule, irreversible, selective androgen receptor (AR) degrader (SARD) and irreversible inhibitor, binds to AR N-terminal domain (NTD) and inhibits both the AR and AR splice variants (AR-SVs).
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UT-105 is a small-molecule, irreversible, selective androgen receptor (AR) degrader (SARD) and irreversible inhibitor, binds to AR N-terminal domain (NTD) and inhibits both the AR and AR splice variants (AR-SVs).
UT-105 selectively inhibits wild-type and enzalutamide-resistant mutant AR transactivation with IC50 of 59.4 nM and 36.5 nM, respectively.
UT-105 is selective to AR and does not inhibit the transactivation of glucocorticoid (GR) or mineralocorticoid (MR) receptors in a panel of kinases (468) and 168 GPCRs.
UT-105 binds to AR NTD, but not ligand-binding domain (LBD).
UT-105 effectively degrades AR, irreversibly inhibits AR, inhibits AR-target genes, and significantly inhibits proliferation and colony formation in cells expressing AR and AR-V7.
UT-105 (60 mg/kg/day), but not enzalutamide and bicalutamide, inhibits TNBC tumor growth in orthotopic MDA-MB-453 TNBC model with a tumor growth inhibition (TGI) of >90%.
UT-105 inhibits STAT1 phosphorylation, effectively reduces IRF1, IRF7, and IRF9 expression in tumors, also inhibits the phosphorylation of STAT1, STAT3, and AKT in MDA-MB-453 tumors.
| M.Wt | 364.29 | |
| Formula | C15H11F3N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Asemota S, et al. Cell Rep. 2023 Nov 17;42(12):113461.
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